ST. JOHNS WORT – HYPERICUM PERFORATUM

Click to purchase St. Johns Wort – Hypericum Perforatum

Part Used:


buds of flowers

NOTE: These indications are only for use with embryonic plant stem cell tissues. Adult plants do not have the same constituents, actions or applications in most cases.

A plant of many faces, St. John’s Wort (Hypericum perforatum) is regarded as a wildflower, a weed, and herb. If I could I would renamed this plant to the Uplifter Worthiness. A perennial herb growing from 1-3 feet tall. Erect stems branch in upper parts with small pale green leaves. Flowers are bright yellow in terminal clusters with long hairy yellow stamens. St. John’s Wort is an aromatic perennial herb with an abundance of golden-yellow flowers. Tiny perforations filled with phytochemical-rich oils cover the aerial (above ground) portions of St. John’s Wort and yield an extract that give the plant its primary health benefits. About 400 species of the plant are in existence. The name Hypericum derives from the Greek name for the plant “hyperikon.” The word roots are hyper (meaning over) and eikon (meaning image). There are many ancient superstitions regarding this herb. Soldiers also knew the uses of St. John’s Wort. Often Crusaders and, later, Civil War soldiers would collect the plant to use on battle wounds. Many soldiers’ journals record the use of a wine made with St. John’s Wort that would steady the nerves. The next notable mention of St. John’s Wort was buy Dioscorides, a Roman army surgeon, recommended drinking the herb in special liquids, “For it expels choleric excrements.” in his medical text. He also recommended rubbing it on burns. Paracelsus, a medical authority of the Renaissance also wrote of using St. John’s Wort to treat wounds. He was also the first to mention using it for psychotic symptoms which he called “phatasmata”. The yellow flowers that seem to be particularly abundant on June 24, the day traditionally celebrated as the birthday of John de Baptist, the plant is commonly known as St. John’s Wort. Perhaps the most important writing on St. John’s Wort came in 1630AD when Agelo Sala stated that St. John’s Wort had an excellent reputation for treating illnesses of the imagination, melancholia, anxiety and disturbances of understanding. He wrote, “St. John’s Wort cures these disorders as quick as lightening.”

Each year, around the third week of June, the plants bloom on schedule and continue to flower sporadically through first frost. They may lapse into quiescence during droughts, only to liven up after the rains return. Their yellow petals are speckled with orange and reddish dots that ooze purplish oil when pinched. Some phytotherapists like the dots where the active ingredients reside–to the pores of St. John’s Wort skin. When the flowers are steeped in oil, the “blood” in the pores moves into the oil. The plants’ buds of flowers are so rich in phytochemicals compared to the blooming plants which lack many of the added phytohormones present in the embryonic stage of growth. One type of secretory glands consisting of black dots which are present even in early emerging leaves. In the fully expanded leaves the nodular structure appears to be composed by a cluster of cells. These become unfunctional and disassembled towards the end of their development, and are used only as reservoirs of secretion products. HPTLC analyses showed that flower buds and flowers are the plant parts richest in active compounds. However, the spectrum of active compounds accumulated by H. richeri was both quantitatively and qualitatively similar to those reported for the pharmaceutically utilized, H. perforatum, and thus could potentially represent a possible alternative to this species. Highest contents of 6-isobutyryl-5, 7-dimethoxy-2, 2-dimethylbenzopyran HP1 (1.56 ± 0.12 g % DW) and HP2 (0.19 ± 0.01 g % DW) were quantified in the green floral buds of the plants.

Blooms June to August, followed by numerous small round blackish seeds which have a resinous smell and are contained in a three-celled capsule; odor peculiar, terebenthic; taste bitter, astringent and balsamic. All St. John’s Wort seems to contain an aromatic phytochemical called cineole. In studies, large quantities of cineole enabled rats to zip through a maze more rapidly, whether the compound was inhaled, applied to their skins, or force-fed to them. The leaves are covered by translucent dots easily seen by holding the leaves up to a light; these are the perforations that give the plant its species designation “perforatum”. When the fresh flowers are crushed, they exude a blood-red juice, which stains the fingers blue-violet.

While St. John’s Wort is native to Europe, it is naturalized in waste places and along roadsides in Asia, Africa, North and South America and Australia. It is one of those European native plants that have followed European settlers wherever they have traveled in the world. The plant was introduced by early settlers to North America, and by 1793, the first recorded specimen, grown without cultivation, was collected in Pennsylvania.

With especially vigorous populations in western North America and Australia have made it a serious weed problem. It is particularly aggressive in rangelands with dry summers. Historically, the greatest economic importance of the herb focuses on St. John’s Wort as a serious weed of throughout the rangelands in Europe, Asia, North and South Africa, Australia, as well as in eastern and western parts of North America. Its economic impact is considered detrimental because it invaded pastures, leaving them a blaze of yellow flowers. I believe this is to cheer us up! Most North American scientific studies devoted to this plant ironically have focused on how to eradicate it. With the increased stress in today’s world it appears to me that this invasion of St John’s Wort is nature’s intelligence response and action towards our stress coming to the rescue! In Phytosociology this indicates the need for this plant as Nature tries cross talking to us. Telling us, “I am here!” Bright, cheerful, yellow, and in great quantities spreading the news. A more complete message from this plant would be, “I am here with a purpose has well as many other plants to relieve you from suffering, stress, and uplift depressive moods.”

Recommendation: this plant should only be taken orally by those who are not taking any kind of prescription drugs, due to the numerous reported contraindications, interactions and side effects listed below. This plant for topical use is safe for everyone.


Oligo-elements:


Al, Ba, Cr, Cu, K, Li, Mg, Mn, Na, Ni, Zn. Cadmium and lead being hypertensive, lithogenic, nephrotoxic was found in the adult leaf and roots again this is why I prefer always the embryonic plant.


Vitamins and Minerals:


Calcium, C, Choline


Phytochemical Constituents:


Naphthodianthrones 0.1% to 0.15%. The anthraquinone derivatives hypericin and pseudohypericin (also emodin-anthranol and cyclo-pseudohypericin). Isohypericin, protohypericin are also present. The reddish dianthrone pigment hypericin (hypericum red) is found in a concentration ranging from 0.02% to 2.5%, depending on harvesting stage of growth. Hypericin concentrations were found to be highest in the plant’s reproductive embryonic buds of flowers stage 3 of growth in the tissues just as the buds of flower are starting to open, followed by the leaf and in stem tissues, respectively. Liposoluble pigments from the plant, including hypericin, carotenoids, and chlorophylls. Flavonoid concentrations occur at n12% in the buds of flowers and approximately 7% in leaves/stalks and include kaempferol, quercetin, quercitrin, isoquercitrin, amentoflavone, luteolin, lutein, luteoxanthin, myricetin, hyperin, hyperoside, rutin, violaxanthin. Other flavonoids found are miquelianin and astilbin. The proanthocyanidins (approximately 12% of aerial parts) are certain forms of catechin/gallic acid and epicatechin. Hyperforin and adhyperforin are in the phloroglucinol class of compounds. Hyperforin appears in St. John’s Wort in concentrations of 2% to 4% in fully develop flowers, and the concentration in the opening embryonic buds of flowers were found to be the highest 3-5% hyperforin. The recovery of hyperforin in plasma has been measured. The related structure furohyperforin, an oxygenated analog of hyperforin, has been isolated from the plant, as have other hyperforin analogs.

The essential oil 0.05% and 0.9%. It consists of mono- and sesquiterpenes, mainly 2-methyl-octane (16% to more than 30%), n-nonane, alpha- and beta-pinene, alpha-terpineol, geraniol, and traces of myrcene, limonene, cadinene, caryophyllene.
Other compounds present include xanthones (1.28 mg/100 g) and tannins (3% to 16%). Phenol constituents include caffeic, chlorogenic, p-coumaric acids, and hyperfolin. Other plant constituents include acids (nicotinic, myristic, palmitic, stearic), carotenoids, choline, pectin, hydrocarbons, and long-chain alcohols. Amino acids include cysteine, gamma-amino butyric acid (GABA), glutamine, leucine, lysine, and others. Hyperinols A (1) and B (2) are new taraxastane type triterpenes, both showed significant inhibitory activity against chymotrypsin enzyme. (2006 August, Pharmaceutical Research Center, PCSIR Karachi Laboratories Complex, Karachi-75280, Pakistan). Two new xanthone derivatives, 1-hydroxy-5,6,7-trimethoxyxanthone and 3-O-methylpaxanthone were isolated from callus of Hypericum perforatum subsp. perforatum together with the known paxanthone, cadensin G, 1-hydroxy-6,7-dimethoxyxanthone, 1,3,6,7-tetrahydroxyxanthone, and 1,3,5,6-tetrahydroxyxanthone. (2005 Feb; 19(2):171-6. Istituto di Biochimica e Biochimica Clinica, Università Cattolica S Cuore e Centro per la Chimica del Riconoscimento Molecolare, CNR, Roma, Italy). Four new bisanthraquinone glycosides, S-(+)-skyrin-6-O-beta-glucopyranoside (1), R-(-)-skyrin-6-O-beta-glucopyranoside (2), S-(+)-skyrin-6-O-beta-xylopyranoside (3) and S-(+)-skyrin-6-O-beta-alpha-arabinofuranoside (4), have been isolated from an ethanol-water (1:1, v/v) dry extract of the aerial parts of Hypericum perforatum L. The structures were elucidated by spectroscopic methods, mainly NMR and mass spectrometry. Circular dichroism was used to determine their axial stereochemistry revealing 1 and 2 to be atropisomers. 1 and 2 inhibited sauvagine (a hypotensive and diuretic peptide) binding to corticotropin releasing hormone (CRH-1) receptors.

Melatonin and serotonin are indoleamine neurohormones that function as photoperiod signals in many species and have recently been found in St. John’s Wort, used in the treatment of depression. Higher concentrations of serotonin were found in the flower buds at the tetrad (prophase of meiosis) stage of microspore development and higher melatonin concentrations were detected during uninucleate mircosporogenesis. (References: Department of Plant Agriculture, Biotechnology Division, Edmund C. Bovey Complex, University of Guelph, Guelph, Ontario N1G 2W1, Canada. 2002 Dec;89(12):555-60. Epub 2002).


Also Contains the Hormones:


Auxins (IAA), Brassinosteroids (BR), Cytokinins (CK), Florigen, Gibberellins (GA), Jasmonic acid (JA), Meristems plant stem cells (PSC) and Salicylates (SA).
Pharmacological analysis illustrates that Hyperforin clearly exhibits a broad spectrum effect on the Serotonergic, Dopaminergic, Noradrenic and GABA-ergic systems, but its action on the brain’s 5-HIAA and 5-HT levels appears to be significantly different from the action of traditional 5-HT re-uptake blockers.

Until recently it was believed that Hyperforin was primarily responsible for the emotional health benefits of St. John’s Wort. However, further laboratory analysis has revealed that all phytochemical constituents of St. John’s Wort are required in order to maximize the effects of Natural Reuptake Inhibition in the Central Nervous System (CNS).

Research shows that Hypericin, Flavonoids and Adhyperforin, important constituents derived from St. John’s Wort, are also potent uptake inhibitors of Serotonin, Dopamine and Noradrenalin. Additionally, St. John’s Wort has been demonstrated to inhibit GABA and L-glutamate uptake. Together, these compounds are believed to promote a healthy neurotransmitter balance in the brain. This effect is thought to provide positive support for a depressed mood and mild to moderate mood changes caused by everyday stress, occasional nervousness, and nervous tension.

Plant Stem Cell Therapy Indications
For Nerve Regeneration Psychological – Physiological. If contraindicated for any reason it has none for its topical use. Do not miss out on its many topical benefits especially when combined with embryonic Arnica (buds).


Psychiatry:


Contains Lithium, Melatonin, and Serotonin. Till recently it remain elusive what phytochemicals in St John’s Worth was responsible for its antidepressant effects. Hypericin was speculated to be the antidepressant phytochemical, but knowing that it contains lithium, melatonin and serotonin I no longer wonder what it is that is responsible for its antidepressant biological activities (mild to moderate, onlydepression. Moderate monoamine oxidase (MAO) inhibitor influence serotonin, dopamine, GABA, and norepinephrine levels and availability in the brain. Increase theta waves in the brain. Theta waves normally occur during sleep and have been associated with deep meditation, serene pleasure and heightened creative activity. St. John’s Wort effectually may improve perception and clarify thinking processes. Regenerative and trophorestorative nerve tonic, to strengthen and heal the brain. The evidence in severe major depression remains unclear. Serious or severe depression can included psychotic symptoms such as delusion, depression with increased suicidal risk, or intense depression that does not allow for the normal continuation of profession or family life. In these cases, more intensive treatment under the care of psychiatric professionals is required. St John’s Wort is never to be used not for severe depression!

St John’s Wort a most prominent anti-depressant effect for the Seasonal Affective Disorder (SAD). Maybe also be effective for obsessive-compulsive disorder (OCD). Effective for Benzodiazepine drug withdrawal. Nicotine withdrawal. Substance abuse of all kinds. Depression and irritability following injury, stress, shock. Compare with Arnica. Embryonic Arnica and St John’s Wort when mixed together yield unbelievable results for acute trauma and not only for the long term use as for depression where its action take longer to show effectiveness approximately three weeks.
This plant is very effective in Somatoform Disorder which is a condition in which the physical symptoms a person feels are due to mental factors. These symptoms cannot be traced to a specific physical cause. Almost like that of “Mal Imaginere”. The patients do have a strong belief that they are sick and in turn might not be faking the illness. Somatoform disorder is also known as Briquet’s syndrome, Pain disorder, or Body dysmorphic disorder. According to the Diagnostic and Statistical Manual for Mental Disorder, 4th edition (DSM-IV-TR), they set up categories for somatic symptoms and it can be called as the somatoform disorder: (1) Somatization Disorder, (2) Conversion Disorder, (3) Pain Disorder, (4) Hypochondriasis and lastly 5 Body Dysmorphic Disorder (BDD). And this is further discussed below (American Psychiatric Association, 2000).

  • Somatization Disorder One common general etiological explanation is that internal psychological conflicts are unconsciously expressed as physical signs.
  • Undifferentiated Somatoform Disorder
  • Pain disorder – appears largely to come from the patients psychological factors, it is more commonly in the older age and the ration is nearly equal 2:1.
  • Conversion disorder – is where the patient’s senses of mobility are impaired with no cause only stressed being the main factor.
  • Hypochondriasis – is mostly related to the stresses that one faces in life, it is marked by fear and lack of assurance. It is now in all age groups it is no long a disorder for the grown adults nut also the adolescents and children,
  • Body dysmorphic disorder – is a disorder that affects the features of the face or head that are exaggerated.
  • Somatoform Disorder not Otherwise Specified ( NOS )

Depression comes in several forms and its symptoms and severity can vary from person to person. For example:

  • In major depression (also called major depressive disorder), people experience symptoms that interfere with their ability to work, study, sleep, eat, and take pleasure in activities they once enjoyed. Symptoms last for at least 2 weeks but frequently last for several months or longer.
  • In dysthymia (also called dysthymic disorder), a less severe, but more chronic form of depression, people experience symptoms that are not as disabling but keep them from functioning well or feeling good. Symptoms last at least 2 years. Many people with dysthymia also have episodes of major depression.
  • In bipolar disorder (also called manic–depressive illness), people have periods of depressive symptoms that alternate or may co-exist with periods of mania. Symptoms of mania include abnormally high levels of excitement and energy, racing thoughts, and behavior that is impulsive and inappropriate.

In addition, milder forms of depression exist that fall into the category of minor depression. In minor depression, people experience the same symptoms as major depression, but they are fewer in number and are less disabling. Symptoms last at least 6 months but less than 2 years continuously.

Anxiety disorders

Overall, there is currently not enough evidence to recommend St. John’s Wort for the primary treatment of anxiety disorders. But we do have wonderful agents for this being: Fig – Ficus Carica (buds), Linden Tree – Tilia Tomentosa (buds) with low serotonin level and anxieties, California Poppy – Eschscholtzia Californica (buds) when serotonin level are high with anxieties. When a patient suffers from anxiety and depression you can synergistically add to your prescription of St John’s Wort providing you precisely know what the levels of serotonin are in a patient you can add one or even two of the above mentioned buds if need for the management of anxieties. Novel Silver Birch – Betula Verrucosa (embryonic germinating seed-rootlets) in the long care management you can permanently correct long standing chronic anxieties these embryonic germinating seeds contain a natural steroid-brassinosteroids which will regrow a shriveled up stunt growth amygdala back to a normal size. Once this happens 6 to 24 months later, when fully regrown anxieties will be experience in a normal fashion toward stress, versus the continuous high stress exacerbated anxieties and or panic attacks. It has been proven that peoples with a normal size, well functioning amygdala rarely ever experience stress like those with shriveled shrunk amygdala. If stress or anxiety are not well managed during this time with other plants in synergy of the antidepressant that Hypericum is or if other drugs are taken during the course of such treatment or if the patient keeps drinking caffeine or caffeine based soda drinks (I cannot call them soft drinks because they are far from soft) this will interfered with these brassinosteroids and will keep stunted the growth of the amygdala. Many other factors can also interfere with the success of this therapy too innumerous to list here.

Note: when prescribing Linden Tree to a patient and that instead of having the desirable effect of sedation they are jazz up from taking it. That is a clear indication that they have high serotonin level in the brain and that for this you will need to change your prescription to the California poppy for anxieties, without ever posing the risk of unwanted abnormal drop in serotonin level which would results in further depression. You will be managing the anxieties in an effective way. Fig serves has an adjuvant for anxieties and does not work in the same way has Linden tree buds or the California poppy buds. Fig buds are for milder cases of anxiety but when combined with St John’s Wort which potentiate its sedation biological activities Fig converts into a most potent anti-anxiolytic. The synergy of well calculated phytochemistry is everything in the design of custom Rx. Individual Protocols, Biotherapeutic Programs. In this way you can heal conditions and diseases that no one else can.

The conflicting Research of St John’s Wort: The official German Commission E monograph for St. John’s Wort lists psycho vegetative disturbances, depressive states, fear, and nervous disturbances as clinical indications for the use of this plant. Clinical studies have shown significant improvement in symptoms of anxiety (which I have not myself observed), apathy, hypersomnia, and insomnia, anorexia (better use Fig buds for anorexia), psychomotor retardation seen only in people with severe depression which St John’s Worth cannot affect (elusive claim), depression feelings of worthlessness. And is much better tolerated with fewer side effects than conventional antidepressants. In addition to Hypericum mood-elevating properties, Germany’s Commission E has approved this herb for the treatment of anxiety and sleep disorders (not so). Yet Hypericum is not addictive and does not impair cognitive functions.


Pediatric:


St. John’s Wort is generally well-tolerated when used by children between the ages of seven and thirteen. St. John’s Wort can also be effective in the treatment of incontinence and bed-wetting in children.


Neurological/Nervous System:


Severed Nerves Regenerative! Neuropathic (nerve pain) for Neuralgias, Neuropathy, Sciatica, Nerve injuries. For pain that radiates or shoots from the injury. Antiinflammatory, Analgesic. Prevent stress induced memory disorders. The herb not only prevented stress and corticosterone-induced memory impairments, but it significantly improved recognition memory.

(Pharmacology, Medical University of Bialystok, Waszyngtona 15A, 15-274 Bialystok, Poland Emil Trofimiuk, Anna Walesiuk and Jan J. Braszko 25 August 2004).

Amentoflavone is able to pass the blood-brain barrier. Parkinson’s disease depresses dopamine levels. Reduce Neuronal Degeneration Caused By Parkinson’s Disease. Free radicals cause dopaminergic neurons in the substantia nigra, avoiding the action of apoptosis. St John’s Wort extracts can prevent the increase of the three enzymes superoxide dismutase, catalase, and glutathione peroxidase, reducing them significantly. This implies that the powerful antioxidant effects of the plant is caused by a synergic action of several of its active compounds.

Burning mouth syndrome: Other names for this syndrome include scalded mouth syndrome, burning tongue syndrome, burning lips syndrome, glossodynia and stomatodynia. Conditions that have been reported in association with burning mouth syndrome include chronic anxiety or depression, various nutritional deficiencies, type 2 diabetes (formerly known as non­insulin-dependent diabetes) and changes in salivary function. Recent studies have pointed to dysfunction of several cranial nerves associated with taste sensation as a possible cause of burning mouth syndrome. This reduction in bitter taste at the chorda tympani branch of the facial nerve (cranial nerve VII) results in intensification of taste sensations from the area innervated by the glossopharyngeal nerve (cranial nerve IX) and the production of taste phantoms. It has been suggested that damage to taste might also be associated with loss of central inhibition of trigeminal-nerve afferent pain fibers, which can lead to oral burning symptoms. Burning mouth pain is often absent during the night but progressively increases throughout the day and into the evening. Based on the makeup of most studies published to date, oral burning appears to be most prevalent in postmenopausal women. It has been reported in 10 to 40 percent of women presenting for treatment of menopausal symptoms. Approximately one third of patients relate time of onset to a dental procedure which In my opinion is the biggest cause of the syndrome, recent illness or medication course (including antibiotic therapy). Most studies have found that oral burning is frequently accompanied by other symptoms, including dry mouth and altered taste (bitter, metallic, or both). Chemical irritation and allergic reactions to dental materials and galvanic currents between dissimilar metals maybe the cause of this burning mouth syndrome. Case reports have linked burning mouth symptoms to the use of angiotensin-converting enzyme (ACE) inhibitors.

References: Grinspan D, Fernandez Blanco G, Allevato MA, Stengel FM. Burning mouth syndrome. Int J Dermatol 1995;34:483-7.
Ship JA, Grushka M, Lipton JA, Mott AE, Sessle BJ, Dionne RA. Burning mouth syndrome: an update. J Am Dent Assoc 1995;126:842-53.
Ben Aryeh H, Gottlieb I, Ish-Shalom S, David A, Szargel H, Laufer D. Oral complaints related to menopause. Maturitas 1996;24:185-9.
Klausner JJ. Epidemiology of chronic facial pain: diagnostic usefulness in patient care. J Am Dent Assoc 1994;125:1604-11.
Grushka M. Clinical features of burning mouth syndrome. Oral Surg Oral Med Oral Pathol 1987;63:30-6.
Basker RM, Sturdee DW, Davenport JC. Patients with burning mouths. A clinical investigation of causative factors, including the climacteric and diabetes. Br Dent J 1978;145:9-16.
American Dental Association status report on the occurrence of galvanic corrosion in the mouth and its potential effects. Council on Dental Materials, Instruments, and Equipment. J Am Dent Assoc 1987;115:783-7.
Bartoshuk LM, Grushka M, Duffy VB, Fast L, Lucchina L, Prutkin J, et al. Burning mouth syndrome: damage to CN VII and pain phantoms in CN V [Abstract]. Chem Senses 1999;24:609.
Brown R, Krakow AM, Douglas T, Chokki SK. ‘Scalded mouth syndrome’ caused by angiotensin converting enzyme inhibitors. Oral Surg Oral Med Oral Pathol Oral Radiol Endod 1997;83:665-7.


Musculoskeletal System:


Joint pains, sprains, first aid kit for crushed fingers from slammed doors, puncture wounds (including bites and from medical procedures), tailbone injuries. Indicated in spinal irritation, sticking pains, tearing pain, hypersensitivity to pain. Jerking and Twitching of Muscles, Darting pain. hypericum preparations have anti-inflammatory activities that may be useful in treating arthritis, a rheumatic disease that causes pain, stiffness, and swelling of joints. Germany’s Commission E (a panel of experts roughly equivalent to the U.S. Food and Drug Administration) heaps praise on St. John’s Wort, for external use, for myalgias (pain in one or more muscles). Restless legs syndrome when not link to any deficiencies like that of Low calcium, magnesium potassium, zinc, and iron.


Gi-Digestive Hepatology:


induces Cytochrome; CYP3A4, but also inhibits CYP1A1, CYP1B1, CYP2D6, and CYP3A4. Most CYPs can metabolize multiple substrates, and many can catalyze multiple reactions, which accounts for their central importance in metabolizing the extremely large number of endogenous and exogenous molecules. In the liver, these substrates include drugs and toxic compounds as well as metabolic products such as bilirubin. Cytochrome P450 enzymes are present in most other tissues of the body, and play important roles in hormone synthesis and breakdown (including estrogen and testosterone synthesis and metabolism), cholesterol synthesis, and vitamin D metabolism. Hepatic cytochromes P450 are the most widely studied. Although there are some contradictory descriptions, some saying that it inhibits this enzyme, St. John’s Wort appears to increase metabolic activity of CYP3A enzymes. See Whitten DL, Myers SP, et al 2006. A number of papers describing in vitro and in vivo research have been published and there are several review papers looking at these. One paper concludes “This suggests that long-term administration of St John’s Wort may result in diminished clinical effectiveness or increased dosage requirements for all CYP 3A4 substrates, which represent at least 50% of all marketed medications.” (Markowitz, Donovan, et al. 2003). Also good for stomach ulcers, due to its chymotrypsin inhibitor and for the treatment of hypertension and gastrointestinal disorders.


Endrocrine System:


Enhance salivary cortisol via a U-shaped dose-response relationship and that this may be mediated through a 5-HT2 mechanism. Chymotrypsin inhibitor can also advantageously be used to treat and/or prevent type 2 diabetes, Chymotrypsin does not digest blood proteins because of protective factors in the blood that block the enzyme. Research also shows hypericum can help with mood swings and depression that may result from hormonal changes like peri-menopause or accomplished menopause.


Immunological System:


Chymotrypsin inhibitor immuno-enhancing and antiinflammatory effects. Chymotrypsin inhibitor can stimulate the proliferation of different cells of the immune system, splenocytes, splenic lymphocytes and bone marrow cells, also suppress the formation of hydrogen peroxide in neutrophils and macrophages. Antioxidative effect. Like that of a Proteinase inhibitor.


Infectious Diseases:


Excellent for Herpes Zoster’s (Shingles), Post Herpetic Neuropathy. Epstein-Barr virus infection. Hypericin is active against several viruses, including Cytomegalovirus, Human Papillomavirus, Hepatitis B, and Herpes I & II. The herb seems to work against viruses by oxidation. The herb’s antiviral effect is stronger when exposed to light. Hypericum antiviral powers pass through the skin and into the nerve endings, preventing and checking a variety of problems. Multiple reports of significant adverse effects and interactions with drugs used for HIV/AIDS, including protease inhibitors (PIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs), suggest that patients being treated for HIV/AIDS with these drugs should avoid this herb.

St. John’s Wort contains proven antiviral that can help speed healing when applied topically. It also can help heal cold sores and fever blisters caused by herpes simplex I, as well as the blisters of its cousins, chickenpox and shingles (varicella-zoster). And when this plant is used topically regardless of prescription drug it does not poses the same problems has when taken internally.

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Two aromatic polycyclic diones hypericin and pseudohypericin have potent antiretroviral activity; these substances occur in plants of the Hypericum family. Both compounds are highly effective in preventing viral-induced manifestations that follow infections with a variety of retroviruses in vivo and in vitro. Pseudohypericin and hypericin probably interfere with viral infection and/or spread by direct inactivation of the virus or by preventing virus shedding, budding, or assembly at the cell membrane. These compounds have no apparent activity against the transcription, translation, or transport of viral proteins to the cell membrane and also no direct effect on the polymerase.
References: Nat’l Academy Sciences U S A (1988 Jul) 85(14):5230-4 Meruelo D Lavie G Lavie D


Hematology:


Has blood-thinning effects. Decrease Platelets Count. Good for thrombocytosis associated with depression. Contraindicated in ITP.


Endocrine:


Studies now show hypericum acts on serotonin and likely a whole host of other brain chemicals. Some think it may prove helpful in the obesity battle. If Prozac can help curb obesity by increasing brain levels of serotonin, St. John’s Wort may have the same positive effect.


Oncology:


Damage from radiation treatments. Women who applied the extract before and after treatments report their skin stayed healthy and flexible, even after dozens of exposures. A potent protein kinase C inhibitor, inhibited the glioma growth hypericin for 48 hours exhibited a classical “ladder” pattern of oligonucleosome-sized fragments characteristic of apoptosis.


Pulmonary System:


Convincing evidence that St. John’s Wort extract plus individual motivational/behavioral support is likely to be effective as an aid in smoking cessation. Research suggests cigarette smoking raises the brain’s availability of the feel-good chemical dopamine–probably a major reason people find it so tough to quit. Some phytochemicals in hypericum also enhance dopamine in the brain.


Surgery:


Very effective treatment for pain after surgery. Integrative German physicians use it extensively they have proven that it is more effective than that of Morphine without the euphoria and toxicity, Not only does it help the pain effectively but accelerate the time of recovery for this purpose must be used in an intramuscular injection of 2ml with a 1ml of B-12 to buffer the stinging of the acid present use Bid or Qid, depending on response or extent of surgical procedure.


Environmental Medicine:


Free radical scavenging activity, metal-chelation activity, and reactive oxygen quenching activity. Contrary to the roots and leaf petals which are toxic with cadmium. Some medicinal plants produce specific secondary metabolites that can detoxify some of toxic metals. Hypericum perforatum is a cadmium hyperaccumulator because they accumulate in their shoots over 100 µg g-1 d.m.


Dermatology:


Antiphlogistic qualities, hypericum-cream or plain straight from the extract itself in the topical treatment of mild to moderate atopic dermatitis is effective. 1st and 2nd degree burns. Skin damage caused by heat, caustics, electricity, or radiation. St John’s Wort with embryonic Arnica buds makes this probably the best healing synergy of all type of wounds, hemorrhoids, sprains, myalgias, cuts, scrape and bruises use topically 2 to 4 x a day at a dose of 3-5 drops of each plant.

Posology: As far as frequency of dosage, many products recommend taking it three times a day. Because of its ‘half life’ of 26.5 hours this is not necessary contrary to other herbs whose half life is less and needs to be taken 3 x a day in order to keep blood saturation. Simply combine the total amount for the day and take it as one dose. It works just fine this way and is much more convenient. Suggested use either 10-30 drops 3 x a day or 30 to 90 drops at once.


Side Effects and Risks:


Side effects of hypericum extracts are mild and uncommon. The most common side effects of St. John’s Wort include dry mouth, dizziness, diarrhea, nausea, increased sensitivity to sunlight, and fatigue but only 2% in 3,000 users. And reported toxicity of cadmium which are present in the roots and in the adult petal leaf of the fully develop flower.

Research has shown that taking St. John’s Wort can limit the effectiveness of some prescription medicines, including:

  • Antidepressant medicines Serotonin syndrome may occur when St. John’s Wort is combined with sympathomimetics, antidepressants, or triptans.
  • Birth control pills (this has never been proven to be a contraindication)
  • Cyclosporine an anti-rejecting drug for transplanted organs
  • Simvastatin, Theophylline
  • Digoxin, Antiepileptics, Tacrolimus
  • Indinavir used to control HIV infection
  • Irinotecan and other chemotherapeutic drugs
  • Warfarin and related medicines used to thin the blood (known as anticoagulants)
  • Laser or sunlight since it is photosensitive
  • Induction of cytochrome P-450 3A4 and other mechanisms. Significant interactions include decreased efficacy of many allopathic drugs
  • Avoid if low platelet Idiopathic Thrombocytopenia Vera ITP
  • Avoid if you are developing cataracts
  • Avoid if pregnant
  • Avoid, wine, cheeses, tryptophan, tyrosine, narcotics, amphetamines

Frequently reported adverse events include nausea, headache, constipation, dizziness, confusion, fatigue, and dry mouth. St. John’s Wort should be used under medical supervision. Serotonin syndrome is a condition defined by muscle rigidity, fever, confusion, increased blood pressure and heart rate, and coma. Mania is defined by symptoms of elevated or irritable mood, rapid speech or thoughts, increased activity, and decreased need for sleep. A possible interaction with loperamide (Imodium®) has been reported; confusion and agitation occurred in one patient taking St. John’s Wort, loperamide, and the herb valerian ( Valeriana officinalis ). St. John’s Wort may interact with triptan-type headache medications. Examples include naratriptan (Amerge®), rizatriptan (Maxalt®), sumatriptan (Imitrex®), and zolmitriptan (Zomig®). Allopathic antidepressant have a somewhat long half-life, meaning that it is slow to be eliminated from your system. It takes around five weeks for it to be fully eliminated from your body. St. John’s Wort conversely is slow to build up in your system, slower than Prozac (you will see progressive improvement in the moods up to three months into being on it). Pregnancy in my own opinion is that one should avoid antidepressants of any type during the first trimester. In the second and third trimester, if a woman becomes sufficiently depressed that she requires an antidepressant she should by all means take one.

Phytopharmacokinetics: St. John’s Wort is a long acting agent, with a ‘half life’ of 26.5 hours (half-life is the amount of time it takes your body to eliminate half of the dose of this plant). It is likely that levels of St. John’s Wort would be low after one week, but there are no studies regarding this. A safe approach would be to discontinue the medication one month before attempting to get pregnant. The Los Angeles Timescommissioned a private laboratory to analyze several of the most popular brands of St. John’s Wort in the US. The results were shocking. Three out of ten had less than 50% potency. Four had less than 90%. Sundown Herbals, a leading supplier of herbals in the US, had an abysmal 20% of the labeled potency. St. John’s Wort may interfere with the way the body processes certain herbs and supplements using the liver’s “cytochrome P450” enzyme system. As a result, the levels of these drugs may be increased in the blood in the short-term, causing increased effects or potentially serious adverse reactions, or decreased in the blood in the long-term, which can reduce the intended effects. Taking St. John’s Wort with herbs or supplements with antidepressant activity may lead to increased side effects, including serotonin syndrome, mania, or severe increase in blood pressure. There is a particular risk of these interactions occurring with agents that possess possible monoamine oxidase inhibitory properties. One well documented effect of St. John’s Wort extracts is to decrease the duration of alprazolam (and probably other benzodiazepines). In one study, the elimination half life was cut in half, from an average of 12 hours to an average of 6 hours, after giving St. John’s Wort for 14 days prior to the test. See Markowitz, Donovan, et al. 2003.

Research

Effect of sub-chronic treatment with Jarsin (extract of St John’s Wort, Hypericum perforatum) at two dose levels on evening salivary melatonin and cortisol concentrations in healthy male volunteers.

Franklin M, Hafizi S, Reed A, Hockney R, Murck H.
Molecular Neurosciences, BMS, Oxford Brookes University, Oxford, UK.
OBJECTIVE: The aim of the present study was to measure the effect of two doses of extracts from Hypericum perforatum (HP), Jarsin, on evening salivary cortisol and NA-mediated melatonin in healthy male volunteers. METHODS: Twenty healthy male volunteers were randomly given a low or high dose of Jarsin for 7 days. Saliva samples for cortisol and melatonin, and overnight urine samples were collected for cortisol and 6-sulfatoxymelatonin and measured by specific radioimmunoassays. RESULTS: Treatment significantly increased salivary cortisol throughout the whole collection period in the low dose group but had no discernable effect in the high dose group. Salivary melatonin was not increased in either dose group following treatment. CONCLUSION: Salivary cortisol was enhanced in the low dose group only and melatonin was not affected by either treatment. We suggest that HP may enhance salivary cortisol via a U-shaped dose-response relationship and that this may be mediated through a 5-HT2 mechanism.

Does St. John’s Wort interfere with the antiandrogenic effect of oral contraceptive pills? Fogle RH, Murphy PA, Westhoff CL, Stanczyk FZ.
Department of Obstetrics and Gynecology, Division of Reproductive Endocrinology and Infertility, Women’s and Children’s Hospital, University of Southern California, Keck School of Medicine, Los Angeles, CA 90033, USA. robinfogel@yahoo.com
BACKGROUND: St. John’s Wort (SJW), a commonly used herbal remedy, has been shown to compromise the efficacy of drugs, including oral contraceptive pills (OCPs), by inducing cytochrome P-450. We investigated whether the simultaneous use of SJW with OCPs resulted in elevated serum androgen levels with implications of impaired OCP treatment of hirsutism and acne. MATERIALS AND METHODS: Fifteen healthy women were treated with the low-dose OC Loestrin 1/20trade mark for 2 months and then additionally with SJW for 2 months. Androgen and sex hormone-binding globulin (SHBG) levels were measured in serum by immunoassay methods; free testosterone (fT) was calculated. Results were analyzed using the Wilcoxon signed-rank test. RESULTS: There were no statistically significant differences in androgen levels after the addition of SJW in women using Loestrin 1/20trade mark. However, there were decreases in total testosterone and fT levels (10.7% and 15.8%, respectively) along with a small increase in SHBG levels (7.0%). CONCLUSIONS: In women using OCPs and SJW simultaneously, it appears that SJW does not interfere with the antiandrogenic properties of OCPs.

A dramatic increase in cell growth and hypericin production was observed after exposure to jasmonic acid (JA). However, other elicitors such as salicylic acid (SA) and fungal cell wall elicitors failed to show any stimulatory effect on either cell growth or hypericin production. Cell cultures treated with JA and incubated in the dark showed increased growth and hypericin production as compared to the cultures grown under light conditions. Jasmonate induction in dark conditions played an important role in growth and hypericin production in cell suspension cultures, to our knowledge an undocumented observation

Best Peak Time to Collect Most Active Phytochemicals Concentration from embryonic buds of flowers were determined
This research was conducted to investigate effects of morphogenetic and diurnal variability on the hypericin content of St. John’s Wort (Hypericum perforatum L.) populations originating from Turkey for maximum utilization of the active substance in plants. During 2002 and 2003, field trials were conducted at Uludag University, Faculty of Agriculture, Department of Field Crops, Bursa (buds). Samples of bud, flower and capsule of H. perforatum L. populations were collected in the second year of cultivation (2003). Factorial arrangements of three H. perforatum L. populations (Bursa, Edirne, and Izmir), three part of plant (bud, flower, capsule) and six collection hour (8.00, 10.00, 12.00, 14.00, 16.00, 18.00) were evaluated in a completely randomized design with three replications. Hypericin content (%) in parts of H. perforatum L. populations was determined according to DAC (1986). Consequently, the content of hypericin in the examined populations varied from 0.260% in Bursa to 0.283% in Izmir. Evaluating parts of plant, we also found hypericin content both in floral parts (0.309%) and buds (0.308%) were higher in comparison to capsule tissues (0.208%) for all populations. When collection hours were examined for the hypericin content of plants, the highest content was recorded at 10.00 (0.279%) and the lowest value at 16.00 (0.272%) and 18.00 (0.272%). As a result of this study, it is possible to say that the highest hypericin ratio was determined in flowers and buds generally collected at 8.00 between 10.00 pm within a day for examined populations.

Hyperfor.jpg

The structure of hyperforin was elucidated by a research group from the Shemyakin Institute of Bio-organic Chemistry (USSR Academy of Sciences in Moscow) and published in 1975. Hyperforin is a prenylated phloroglucinol derivative. Total synthesis of hyperforin has not yet been accomplished, despite attempts by several research groups.
Hyperforin is believed to be the primary active constituent responsible for the antidepressant and anxiolytic properties of the extracts of St. John’s Wort. It acts as a reuptake inhibitor of monoamines, including serotonin, norepinephrine, dopamine, and of GABA and glutamate, with IC50 values of 0.05-0.10 mcg/ml for all compounds, with the exception of glutamate, which is in the 0.5 mcg/ml range. It appears to exert these effects by activating the transient receptor potential ion channel TRPC6. Activation of TRPC6 induces the entry of sodium and calcium into the cell which causes inhibition of monoamine reuptake.
Hyperforin is also thought to be responsible for the induction of the cytochrome P450 enzymes CYP3A4 and CYP2C9 by binding to and activating the pregnane X receptor (PXR).

Hyperforin has antibiotic properties and is active against methicillin-resistant strains of Staphylococcus aureus (MRSA) with a minimal inhibitory concentration (MIC) value of 1.0 μg/ml, as well as against other gram-positive bacteria.
St John’s Wort has been shown to cause multiple drug interactions through induction of the cytochrome P450 enzyme CYP3A4, but also CYP2C9. This results in the increased metabolism of those drugs, resulting in decreased concentration and clinical effect. The principal constituent thought to be responsible is hyperforin. St. John’s Wort also has been shown to cause drug interactions through the induction of the P-glycoprotein (P-gp) efflux transporter. Increased P-gp expression results in decreased absorption and increased clearance of those drugs which leads to lower clinical concentrations and efficacy.

The exact mechanism by which St John’s Wort and even conventional antidepressants functions is unclear and subject to conjecture. The St John’s Wort mechanism is believed to involve inhibition of serotonin (5-HT) reuptake, much like the conventional selective serotonin reuptake inhibitor (SSRI) antidepressants. The major active antidepressive constituents in St John’s Wort are thought to be hyperforin and hypericin, although other biologically active constituents present, for example, flavonoids and tannins, may also be involved.
Some believe that hyperforin is the major constituent responsible for antidepressant activity, and it has been shown to inhibit the uptake of 5-HT, dopamine, noradrenaline, GABA and glutamate. On the other hand, a hyperforin free extract of St John’s Wort (Ze 117 – Remotiv) has been shown to still have significant antidepressive effects.

Hypericin.jpg

Hypericin is a red-colored anthraquinone-derivative, which, together with hyperforin, is one of the principal active constituents of Hypericum. Hypericin is believed to act as an antibiotic and non-specific kinase inhibitor. Hypericin may inhibit the action of the enzyme dopamine β-hydroxylase, leading to increased dopamine levels, although thus possibly decreasing norepinephrine and epinephrine.

The crude extract of Hypericum has weak receptor affinity for MAO-A and MAO B receptors. Isolated hypericin does not display this activity, but does have affinity for NMDA receptors.
The large chromophore system in the molecule means that it can cause photosensitivity when ingested beyond threshold amounts. Because hypericin accumulates preferentially on cancerous tissues, it is also used as an indicator of cancerous cells. In addition, hypericin is under research as an agent in photodynamic therapy, whereby a biochemical is absorbed by an organism to be later activated with spectrum-specific light from specialized lamps or laser sources, for therapeutic purposes.
Acute effects of LI 160 (extract of Hypericum perforatum, St John’s Wort) and two of its constituents on neuroendocrine responses in the rat
M. Franklin. University of Oxford Department of Psychiatry, Psychopharmacology Research Unit, Warneford Hospital, Headington, Oxford OX3 7JX, UK.
J. D. Chi. University Department of Psychiatry, Warneford Hospital, Oxford OX3 7JX, UK.

M. Mannel. Lichtwer Pharma AG D-1235 Berlin, Germany.
P. J. Cowen. University Department of Psychiatry, Warneford Hospital, Oxford OX3 7JX, UK.

Extracts of Hypericum perforatum (St John’s Wort), such as LI 160, which are effective antidepressants have several active constituents. Their mode of action in depression, however, is unclear. In the present investigation, we assessed the effect of equivalent doses of LI 160 and two of its components, hypericin and hyperforin on serotonin (5-HT) and dopamine (DA)-mediated neuroendocrine responses in the rat. LI 160, hypericin and hyperforin significantly and equivalently increased plasma corticosterone. This effect was blocked by ketanserin but not WAY-100635, suggesting mediation via 5-HT2 receptors. LI 160 also lowered plasma prolactin and prevented the increase in plasma prolactin following haloperidol administration. Hyperforin had a similar but somewhat less pronounced effect. We conclude that LI 160, hypericin and hyperforin all increase 5-HT-mediated corticosterone release while LI 160 enhances DA-mediated inhibition of prolactin release. Hyperforin may contribute to the facilitatory effect of LI 160 on DA function, but hypericin does not.

Accumulation of Hypericin in Dark Glands
Accumulation.jpg
Stage 1 of flower development: an intact flower bud.

Glands.jpg
Hypericin, those little black dots.

Variation.jpg

Variation in Hypericins from Wild Populations of Hypericum perforatum L. in the Pacific Northwest of the U.S.A
Tara M. Sirvent, Loren Walker, Nan Vance, and Donna M. Gibson

  • aDepartment of Plant Pathology, Cornell University, Ithaca, NY
  • bPortland State University, Portland, OR
  • cUSDA Forest Service, Pacific Northwest Research Station, Corvallis, OR
  • dUSDA, Agricultural Research Service, Plant Protection Research Unit, U.S. Plant, Soil, and Nutrition Laboratory, Tower Road; Ithaca, NY 14583.

Abstract

Representatives from eight wild populations of Hypericum perforatum L. were collected from Montana and Northern California at flowering, and subsequently analyzed for hypericin and pseudohypericin using HPLC analysis. Total individual plant concentrations in these wild populations were from 0.0003–0.1250% dry weight (DW) hypericin and 0.0019–0.8458% DW pseudohypericin. In general, hypericin concentrations were highest in the plant’s reproductive (flower and bud) tissues, followed by leaf and stem tissues, respectively. Hypericin and pseudohypericin concentrations were positively correlated in all samples, although the relative ratio of hypericin to pseudohypericin varied with site location.
Traditional use of the St. John’s Wort herb indicated 2 to 4 g/day doses. However, most clinical studies have been conducted with extracts, with the hypericin content of 0.3% as the earliest form of standardization. With the discovery of hyperforin’s bioactivity, a content of 3% to 5% hyperforin has been used as a new standard.