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St. John's Wort (Hypericum Perforatum L.): A Review

© Christopher Hobbs LAc, AHG
 (Excerpted from HerbalGram)

Although there have been a considerable number of studies published demonstrating the phototoxicity of hypericin in various animal species (119, 120), a thorough search by this writer brings to light no evidence that there has ever been a case involving human toxicity.

Some authors recommend caution when using large quantities of St. John's wort extract for medicinal uses, particularly for people with fair skins, who should not expose themselves to strong sunlight during Hypericum therapy (121). Judging by the available literature, a very moderate dose, up to 4 g of the dried herb, 30 ml of the 1:5 tincture (40% EtOH), or 240 grams of the 1:5 powdered extract per day (standardized to 0.125% hypericin), should not pose a problem, if sunlight restriction is followed (122, 123), especially given the widespread use of H. perforatum extracts in Europe. One major product is recommended by the manufacturer to be taken as 40 mg tablets (1-2 tablets, 3 times a day).

Preparations
Hypericin was more effectively extracted with glycol and sunflower seed oil when the moisture content of the herb was between 50 and 70%, and 2-7 times higher at 70 degree C. than at 20 degree C. The menstruum was saturated after 12 hours and 24 hours respectively, but it took 3-4 extractions to exhaust the herb (124). The total extraction in one hour of hypericin with ethanol was not dependent on water content of the herb. The authors conclude that ethanol is the most suited menstruum for the extraction of dried material (125).

Freshly air-dried herb was moistened to 70-72% moisture and extracted at 70 degree at 1:7 with sunflower seed oil. The total content of hypericin was 2.5 mg%, and extracting the marc with ethanol could increase the content to 3.32 mg% (a 25% increase)(126).

Hypericin content of a juice of H. perforatum and a powdered extract dropped by 14% during 1 year, and the dry extract remained stable, when stored at 20 degree C. When stored at 60 degree C., the hypericin content dropped 33%, 33%, and 47% from a powdered extract, tablets, and liquid juice, respectively (127).

In one extensive study, up to 80% of the hypericin was destroyed by drying of the fresh plant in sunlight (128). For this reason, modern herbalists generally grind the fresh tops of Hypericum and immediately macerate them in olive oil or sunflower seed oil. The oil is then pressed and filtered after two weeks, and should be stored in amber bottles away from heat and light. An alcoholic tincture is made in the same way, macerating the fresh, ground tops in 70% ethyl alcohol and 30% distilled water.

St. John's wort is currently official in the pharmacopeias of Czeckoslovakia, Poland, Roumania, and Soviet Union (129).

Identification and Adulteration
For identification of cut and sifted material from the commercial drug market, note the two opposite ridges on the stems. These are prominent, and an important character in differentiating different Hypericum species (see Fig. 1).

Ideally, the commercial drug should consist mostly of flowering tops, but in common practice the whole above-ground plant with a considerable quantity of stem may be present. Flowers that are present should consist of 70-90% (or more) with immature capsules, otherwise the plants may have been harvested too late in the season. The hypericin content declines immediately after anthesis (flower maturity and pollination).

The leaves, when observed with a 10X hand lens, should be characterized by many punctate glands, clearly distinguishable by holding them up to a light source. The flowers will all contain fragments of the persistent dried petals, which may have red glands (appearing black) around the perimeter.

The taste (and smell) of St. John's wort is characteristicly slightly sweet, bitter, and astringent.

A commercial oil or tincture of Hypericum should be vivid, almost fluorescent red. If the preparation is pale red to pink, the hypericin content, and thus the quality of the product, is suspect.

Several methods are given in the literature for the TLC and HPLC identification of hypericin (130, 131, 132, 133, 134, 135, 136, 137, 138), and Katalin et al (1982) report on the histological examination of St. John's wort leaves (139).

Since tannins play a role in the therapeutic action of St. John's wort extracts, standardization with this fraction has been recommended (liquid extract containing 1% tannins) (140).


Literature

Review: An earlier review (1969) covers the history, development and photodynamic effect, chemical constituents, synthesis of hypericin, pharmacology and uses with 127 references (in German) 141.


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About The Author
Christopher Hobbs is a fourth generation herbalist and botanist with over 30 years experience with herbs. Founder of Native Herb Custom Extracts (now Rainbow Light Custom Extracts) and the Institute for Natural Products Research. Christopher writes and lectures internationally on herbal medicine. He is a consultant to the herb industry and is currently practicing and working on a......more
 
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