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St. John's Wort In A Nutshell

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Hyperforin: The Key to
effective St. John's Wort

In a randomized, double-blind placebo controlled study, published in Pharmacopsychiatry a group of 147 people took either a St. John's Wort extract with 3 percent hyperforin, one with 0.5 percent hyperforin or a placebo. At the end of the six-week trial, those taking the highest hyperforin dose showed the most positive results. After eight days, those who took the higher hyperforin showed the greatest changes in delta, theta and alpha-1 brain wave activity. Scientists hypothesize that this is physical evidence that hyperforin is inhibiting the re-uptake of seratonin, noradrenaline and dopamine.

This finding is so significant that Pharmacopsychiatry, a highly regarded German journal of clinical pharmacology and psychiatry, recently devoted an entire supplemental issue to hyperforin. It includes several recent clinical studies that show hyperforin to be the compound responsible for inhibiting neurotransmitter reuptake --- rather than the compound hypericin as previously believed. With every passing day, clinical research is amassing more data demonstrating hyperforin to be the key to St. John's Wort's power. "This discovery is extremely exciting for people seeking a dependable route to a positive outlook on life," said Derrick DeSilva Jr., MD, a practicing internist who teaches at JFK Medical Center in Edison, NJ, and is author of Ask The Doctor: Herbs & Supplements for Better Health. "While previous clinical studies have shown St. John's Wort is effective, questions remained about the identity of the active component and how it relates to efficacy.

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Hyperforin Studies

Hyperforin, a Major Antidepressant Constituent of St. John's Wort, Inhibits Serotonin Uptake by Elevating Free Intracellular Na+1 1

Role of hyperforin in the pharmacological activities of St. John's Wort.

Safety of Hypericum extract in mildly to moderately depressed outpatients

Investigation of the bioavailability of hypericin, pseudohypericin, hyperforin

Aristoforin, a novel stable derivative of hyperforin, is a potent anticancer agent.

Biosynthesis of the hyperforin skeleton in Hypericum calycinum cell cultures.

Hyperforin represents the neurotransmitter reuptake inhibiting constituent of hypericum extract.

Hyperforin activates nonselective cation channels (NSCCs).

Liquid chromatography-mass spectrometry studies of St. John's wort methanol extraction

Potential antidepressant properties of IDN 5491 (hyperforin-trimethoxybenzoate), a semisynthetic ester of hyperforin.

Hyperforin, the active component of St. John's wort, induces IL-8 expression in human intestinal epithelial cells via a MAPK-dependent, NF-kappaB-independent pathway.

Simultaneous determination of hypericin and hyperforin in human plasma with liquid chromatography-tandem mass spectrometry.

Air/light-free hyphenated extraction/analysis system: supercritical fluid extraction on-line coupled with liquid chromatography-UV absorbance/electrospray mass spectrometry for the determination of hyperforin and its degradation products in Hypericum pertoratum.

Liquid chromatographic determination of St. John's wort components in functional foods.

Flavonoids of St. John's Wort reduce HPA axis function in the rat.

Historical St. John's Wort Applications
The historical use of medical St. John's wort is well documented. Commencing 2400 years ago St. John's wort was used as a nerve tonic, a painkiller for arthritis, menstrual cramping, gastrointestinal problems (such as diarrhea, nausea . . . ) as well as ulcers.

The ancient Greeks and Romans used to treat many ailments, including sciatica and poisonous reptile bites as well as to ward against evil spirits, placing sprigs of the plant on statues of their Gods. In fact, the genus name Hypericum is from Greek and means "over an apparition" as the herb was once considered odiferous enough to cause evil spirits to depart.

In the first century St. John’s wort was referred to in Pliny the Elders famous book on natural history for its bracing quality in treating diarrhea and promoting urine flow and bladder troubles.

Dioscorides, a Roman army surgeon, recommended drinking St Johns wort in his medical text, “For it expels choleric excrements…†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 “phatasmataâ€.

During medieval times, the Europeans used the plant to treat all forms of madness (They thought St. Johns wort had magical properties) as it blooms near the Summer Solstice. The Saltenitan drug list of the thirteenth century also referred to St. John’s wort as herba demonis fuga--an herb to chase away the devil.

Sixteenth century medical books refers to the plant as Fuga demonum, or devil’s scourge, a term that was repeated frequently in the literature of the next several hundred years.

The oil made from the flowers was listed in the first Pharmacopoeia Londinensis (1618). 1630 Angelo Sala stated that St. John’s wort treated illnesses of the imagination, melancholia, anxiety and disturbances of understanding. He wrote, “St. John’s wort cures these disorders as quick as lightening.†Gerard wrote that its use as a balm for wounds, burns, ulcers and bites was without equal (Gerard 1633).

There is even evidence that the American Indians used St. John's wort used it in the treatment of Tuberculosis and other breathing ailments.

Civil War soldiers collected St. John's wort to use on battle wounds. A prolific and hardy plant that threatened grazing land, a beetle was introduced into the Pacific Northwest in the early 1900's to keep St. John's wort under control.

19th century literature incorporated the use of hypericum to treat melancholia. 19th century British and American literature stressed the superficial use of the herb for the treatment of burns and wounds. A powerful antibacterial, St. John’s wort has been used through the centuries as an analgesic (pain reliever) to treat saddle sores and in poultices for certain lameness's in horses.

More contemporary St. Johns Wort applications

  • Over time, and the advent of modern pharmaceutical science, St. John's Wort was nearly forgotten as a medicinal herb. Only recently has St. John's Wort gained a renewed reputation as an effective treatment for all manner of infirmities most notably depression. Its complex and diverse chemical makeup has also shown to support depression related infirmities such as chronic fatigue syndrome, and pms.
  • St. John's Wort's antibacterial / antiviral properties render it very useful adjunctive treatment for bacterial and viral infections.
  • St. Johns Wort has also been shown to be useful in treating pulmonary complaints, bladder trouble, suppression of urine, dysentery, worms and nervous depression.
  • St. Johns Wort can act to dissolve and remove bacterially based tumors and boils. It calms the nerves and increase the flow of urine.
  • St. John's Wort is an excellent blood cleanser and blood purifier.
  • For Tourette's syndrome - used with Wormseed
  • Bells' Palsy (apply directly on face)
  • St. Johns Wort antibacterial/viral properties have been shown useful in relieve phlegm obstructions in the chest and lungs. It can be beneficial in addressing bronchitis as well.
  • Like Horsechestnut, St. Johns Wort may be valuable for treating internal bleeding.
  • St. Johns Wort is used to treat chronic uterine problems and will correct irregular and painful menstruation.
  • St. Johns Wort contains an alkaloid that is a heart and artery stimulant
  • Is useful for low back pain
  • Mattioli wrote of its use as an emmenagogue and antimalarial (Bombardelli and Morazzoni 1995).
  • Most recent research at two of the world's leading medical institutions, New York University and the Weizman Institute of Science in Israel ,found that 2 of the main constituents of St. John's Wort namely hypercin and pseudohypericin were found to inhibit the growth of retroviruses( including HIV, the AIDS virus) in animals. Although the results of these studies are promising, more work needs to be done. The mechanism is thought to involve the production of oxygen free radicals which can damage the viral envelope.

A Closer Look at the
St. John's Wort Plant