SOPHORA
Of all the different sophora species and plant parts used in Chinese medicine, Sophora flavescens roots are by far the most frequently used, which is why the common name “sophora” is appropriately selected to represent it. Sophora (see Figure 2) was first described in the Shennong Bencao Jing (ca. 100 A.D.). It is traditionally used to dispel heat, dry dampness, expel wind, and eliminate intestinal parasites. It is thus administered in formulas for dysentery and jaundice (damp-heat syndromes), edema and dysuria (dampness syndromes), and eczema and pruritis (damp-heat-wind syndromes).
Sophora root is called kushen (bitter shen; see: The meaning of shen in renshen), and is obtained mainly from Sophora flavescens, though Sophora angustifolia is a minor source of kushen. Another related species, Sophora subprostrata also called Sophora tonkinensis (shandougen: mountain bean root), has similar constituents, properties, and applications, and is sometimes designated as subprostrata to distinguish it (see Figure 3). Kushen and shandougen are usually presented as separate entries in the Chinese Materia Medica books, appearing in two subcategories of the heat-clearing section: dry dampness (kushen) and clean toxin (shandougen).
Sophora subprostrata was first recorded in the Kaibao Bencao (973 A.D.). It is traditionally used to alleviate heat and toxin, and is said to disperse swellings. Subprostrata is administered in formulas for painful swelling in the throat, mouth, and gums, to clear lung heat, to alleviate constipation, and to resolve masses (including carcinoma). According to the modern Materia Medica, “Shandougen removes toxic materials in many herbs, stops pain, reduces inflammation and stops cough; it cures pharyngitis when sucked, eliminates abdominal distension when ground and taken orally, relieves female abdominal distention due to blood stasis when taken with wine, and treats baldness and bites (snake, dog, or spider) when squeezed to get a juice for application to the affected site. For esophageal cancer and pharyngeal cancer, it is ground with ginger for sucking.”(1) A passage that illustrates the ultimate similarities in usage between kushen and shandougen is recorded in the Canon of Materia Medica: “kushen is mainly indicated for knotted syndromes and mass in the chest and abdomen” (1) thus suggesting its anticancer activity in common with shandougen.
The flower buds (huaimi), flowers (huaihua), fruits (huaijiao),
and branches (huaizhi) of the related
species Sophora japonica are also
used in the practice of Chinese medicine, though for different applications
than the roots: they cool blood and control bleeding. Despite the differences, there is at least one case of overlap:
both the roots and flowering tops of sophora are used in the treatment of
intestinal hemorrhage such as occurs with ulcerative colitis (administered by
retention enema in severe cases of the disease). This antihemorrhagic action is probably due to the flavonoids in
both of these parts. There is a far
higher concentration of flavonoids in the flowers and fruits—those parts of the
plant more often used for treating hemorrhage—which are listed in the Materia
Medica in the hemostatic category.
Also, all the plant parts of the various sophora species have some
inhibitory effects against intestinal pathogenic organisms (bacterial or
amebic) so that they may inhibit intestinal bleeding that is secondary to the
activity of these infections.
TRADITIONAL PRESCRIPTIONS
One of the earliest traditional formulas containing sophora is Sanwu Huangqin Tang (Scute Three Herb Combination), made with sophora, scute, and raw rehmannia (in a ratio of 1:1:2, with 6–9 grams sophora). This bitter, cold formula for purging fire was recorded in the Jingui Yao Lüe (220 A.D.). It was originally recommended for treatment of post-partum fevers, which, we know today, arise from infections of the reproductive organs that occur during childbirth. In modern practice, especially in Japan, this formula is also applied in the treatment of hemorrhage, skin rashes (allergic disorders), and various heat syndromes. An interesting aspect of this formulation is that it relies on three important types of active constituents: alkaloids from sophora, flavonoids from scute, and sterols from rehmannia.
The Sophora Pill (Kushen Wan) was described in the Yi Bu
Quan Lu, and consists of 67% sophora, 22% zaocys, and 11% acorus. The ingredients are powdered, formed into
pills, and taken in a total daily dosage of 30 grams per day. It is mainly prescribed for skin disorders
with itching or accompanied by rashes.
Another well-known prescription is Xiaofeng San (Tang-kuei and Arctium Formula), made with sophora, anemarrhena, raw rehmannia, akebia, gypsum, arctium, siler, cicada, schizonepeta, sesame, tang-kuei, atractylodes, and licorice. This formula, described in Waike Zheng Zong (1617 A.D.), relies on both the heat-clearing and wind-alleviating action of sophora. The prescription is designed to treat skin diseases with itching and discharge of pus. It is widely used in Japan to treat chronic eczema and chronic itching skin, and has been adopted for that use in the West (veterinarians have deemed it valuable for the common skin ailments of animals). Several variations of the formula have been published in the Chinese medical literature for treating chronic skin diseases.
It can be seen that skin ailments are a primary target of therapy with sophora. Sophora is used topically as often as internally. A traditional formula for topical application is Sophora Combination (Kushen Tang), comprised of sophora, phellodendron, kochia, cnidium fruit, wild chrysanthemum, lonicera, angelica, and acorus. This formula first appeared in Yi Zong Jin Jian (1742 A.D.) along with other similar formulations for external application in the treatment of skin diseases. Numerous variations of this prescription have been recorded in the modern medical literature.
SOPHORA ROOT ACTIVE CONSTITUENTS AND THEIR SAFETY
Matrine and the similar compound oxymatrine are the principal active constituents of sophora root (2,3,4). These components are alkaloids, and they comprise about 2% of the dried root stock for kushen and about 1% for shandougen. Dozens of other alkaloids are also present, but in relatively tiny amounts (in order to analyze their pharmacological activities, they must be separated from the other alkaloids).
When properly prepared, the
traditional decoction made with sophora root (kushen) will provide 60–300 mg of the main alkaloids, derived from
3–15 grams of dried herb, the dosage range listed in the traditional medical
literature. In modern practice, up to
30 grams of herb in decoction form are given daily, in two or more divided
doses.
In China, oxymatrine has been prepared as an herbal drug product, given either orally or by injection. When taken orally, oxymatrine is converted to matrine, which is the more absorbable form. Matrine is stable in the blood (not converted by the liver) and is excreted by the kidneys within 24 hours. When oxymatrine is administered by injection, it is stable and is excreted as oxymatrine. It is not known if the actions of matrine and oxymatrine (see Figure 1) are slightly different. The alkaloid fraction from sophora, called kushensu, is frequently used in clinical practice, especially for oral administration.
Unlike many of the well-known alkaloids from other plants that are used in medical practice, the toxicity of matrine and oxymatrine is very low and the central nervous system effects are mild. As an example of the low level of toxicity, the LD50 (dose that is lethal to 50% of animals) for injection of the herbal extract (from S. subprostrata) in mice corresponded to a dose of 15 grams of herb per kg (in human terms, this corresponds, roughly, to a single dose of 1 kg of the herb). The LD50 of injected total alkaloids of Sophora subprostrata in dogs was 650 mg/kg (human equivalent of over 40 grams of alkaloids per day, compared to the less than 1 gram per day medicinal dose). Daily injection of 100 mg/kg of oxymatrine to mice (human equivalent would be about 7 grams per day) for two weeks yielded no pathological changes.
The main effect of sophora on the central nervous system is sedative in nature, and this corresponds with traditional comments about the effect of the herb. A clinical trial of sophora for treating insomnia involved providing a dose of syrup derived from 10 grams of root extract (containing about 200 mg of alkaloids) before going to bed; this treatment was considered effective and could sometimes replace the previous use of tranquilizer drugs by the patients.
According to Niu Kuizhi (5), “Sophora has little side effect. When used in excessive dosage, it might give rise to some symptoms of the digestive tract, such as malaise of stomach, nausea, vomiting, and constipation; occasionally, dizziness, alopecia, and rash. The adverse effects are related to dosage. When the dose used is under 30 grams per day, generally, no adverse reaction appears.”
Typical dosing of the extracted sophora alkaloids for humans is 300–600 mg per day (at 2% alkaloids, this corresponds to 15–30 grams/day of the root), though higher doses are sometimes used (in one study of arrhythmia treatments (2), the dose was gradually raised to 1,000–1,500 mg each time, three times daily). Adverse reactions to the alkaloids are rarely noted. When given by injection, the injection-site reactions (mainly pain) are common, as occurs with many other herbal compounds; when given orally, some individuals may report gastric reactions (e.g., nausea). In another study of arrhythmia, continuous treatment for 8 weeks was found to produce no adverse reactions, and no abnormalities were detected in the blood or urine of the patients. Some patients being treated for asthma with a sophora-alkaloids dose of just 100 mg each time, three times daily, reported dizziness or gastric discomfort. These symptoms spontaneously resolved, however, without discontinuing treatment. At very high dosages, beyond those usually applied clinically, oxymatrine can exert an immune suppressive effect by enhancing the level of calcium within lymphocytes.
Sophora alopeculoides (kudouzi), contains the alkaloids not only in the root, but in the whole plant, and is sometimes used as a source of the alkaloids for manufacture of drug products (4). Sophora viciifolia (baicihua) seeds are also being developed as a source of the alkaloids (12).
APPLICATIONS
The following is a summary of the benefits of sophora and its extracts according to Chinese medical literature. Due to insufficient controls in most Chinese clinical studies (see: Controlled clinical trials of Chinese medicine), the outcomes reported here should not be viewed as reliable, but, instead, as a guide to seeing how the Chinese physicians apply this herbal material. According to Pharmacology and Applications of Chinese Materia Medica (2) and Modern Study and Application of Materia Medica (3), the following are applications that were developed mainly during the period 1974–1979:
·
Adjunct to cancer therapy: Injection of sophora extract, containing mainly
the alkaloids, was used as an adjuvant to standard medical therapy in 200 cases
of lung cancer, with reported good effects.
The injection at 200–400 mg each time, once daily, was reported to
counter leukopenia induced by radiation therapy (said to improve the WBC for 21
out of 25 patients); the total dosage of alkaloids used (sum of daily
treatments) ranged from 2.8 to 18 grams.
The same basic result was found in patients who suffered from leukopenia
due to either radiation therapy or chemotherapy, at a dose of 200–400 mg each
time, once or twice daily for 4–37 days (total alkaloid dose ranging from
1.6–29.6 grams). It was reported that
the effects were rapid: the improved WBC could be detected within one week of
therapy in nearly all responding patients.
In yet another study, a dose of 400 mg once daily for less than three
weeks total time was sufficient to improve WBC in women with gynecological tumors
(26 of 30 cases). According to Anticancer Medicinal Herbs (1), in the
treatment of cancer, subprostrata has the function of stimulating the immune
mechanism rather than inhibiting cancer cells directly.
· Arrhythmia: Short-term benefits were noted in the treatment of arrhythmia, especially in cases of coronary disease and particularly in premature beats. The dosage and administration varied somewhat. Injections were given with 30 mg each time, twice daily, while capsules were given 50 mg each time, three times daily, with that dose doubled if it was not effective within one week.
· Asthma: Capsules of the sophora alkaloids and inhalant sprays were found helpful. Tablets of the total alkaloids, given at a dose of 100 mg, three times daily for 10 days, was reported to be highly effective for asthma. A decoction of 15 grams sophora taken once daily, or tablets of sophora extract taken three times daily was said to have effects nearly equal to aminophylline.
· Female reproductive system infections: Sophora root powder or a foam containing sophora alkaloids applied to the cervix was found effective in the treatment of cervix erosion. In another report, the alkaloids at 50–100 mg, given two to three times daily by injection for 10 days, which would be continued for another 10 or 20 days if necessary, effectively treated women with various infections of the reproductive organs, including salpingitis, chronic pelvic inflammatory disease, endometritis, chronic cervicitis, and vaginitis. According to Modern Study and Application of Materia Medica (3), the alcohol extract of sophora (which would be rich in the alkaloids) inhibits vaginal trichomonas (of 176 patients treated topically, 126 were cured).
· Intestinal infections: Matrine tannate (the sophora alkaloids complexed with tannin), at a dose of 600 mg each time, three times daily), was used to treat bacillary dysentery with a high rate of effectiveness. The ordinary matrine capsule or tablet (600–900 mg each time, three times daily) was also effective. Recent studies have indicated that a decoction of 30 grams of sophora root (taken in 4 divided doses daily) could effectively treat giardia if administered regularly for 1–4 weeks (30 grams of sophora root contains about 600 mg of the main alkaloids). Bacterial dysentery is also treated by using 30 grams sophora in decoction, with two divided doses daily for 1–2 weeks.
· Allergic reactions: According to Modern Study and Application of Materia Medica (3), both sophora and its alkaloids are effective for treating urticaria, acute eczema, pudendal eczema, and other types of dermatitis. One of the alkaloids, aloprene, was shown to be a potent inhibitor of swelling induced by many agents (11).
· Viral hepatitis: recent research has shown that sophora and its alkaloids inhibit hepatitis B and hepatitis C (see: Hepatitis C: Recent treatment strategies). Sophora subprostrata has been incorporated into several formulas for treatment of hepatitis B. Oxymatrine was demonstrated to have good clinical effects in patients with hepatitis C. In laboratory animals, it was also shown that oxymatrine exhibits a protective effect against induced liver damage (injection dosage 3.6 mg/kg, corresponding to a human dosage, by weight, of about 250 mg).
TOPICAL APPLICATIONS
Sophora is frequently applied topically in herbal formulations as a wash and, less frequently, in a cream. It is most often used in treatment of infections and allergy reactions. The following formulations serve as examples, described in Manual of Dermatology in Chinese Medicine (6). The dosages listed are in grams but may be adjusted proportionately to make smaller or larger amounts of the finished product. It will be noted from these formulations that certain herbs appear repeatedly with sophora, such as phellodendron, cnidium fruit, and lonicera—ingredients of the traditional Kushen Tang. These provide a broad spectrum of antiseptic and anti-inflammatory active constituents that can have a marked effect on skin disorders, and, when used as a douche, vaginal disorders. Many of the ingredients in these formulas are present in Shen Bai Wash, a topical preparation that has been made available by ITM for more than 5 years (see: Shen Bai Wash). The usual method of application for these washes is to make a decoction or vinegar extract and apply it to the affected part for 20–30 minutes at a time, 1–3 times daily, for several days, usually not more than 2 weeks, and not to exceed one month at a time.
Formulas
for Infections
Kushen Tang (Sophora Decoction, a traditional prescription; sample indications: leprosy and tinea)
sophora 60
phellodendron 15
lonicera 30
cnidium fruit 30
angelica 15
wild chrysanthemum 60
kochia 15
acorus 9
Xi Chuang Fang (Formula to Wash Sores; sample application: strep and staph sores)
sophora 30
phellodendron 30
stemona 20
lonicera 20
rhubarb 30
dandelion 20
Sanhuang Xi Ji (Three Yellows Wash; sample application: furuncles, usually caused by staph)
sophora 30
phellodendron 30
rhubarb 30
scute 30
Qingre Jiedu Xi Ji (Clear Heat, Reduce Toxin Wash; sample application: venereal warts)
sophora 15
stemona 15
cnidium fruit 15
stellaria (langdu) 10
carpesium 10
protulaca 15
zanthoxylum 5
Ku Jiao Tang (Sophora and Zanthoxylum Decoction; sample application: scabies)
sophora 30
zanthoxylum 9
Formulas
for Dermatitis (allergy-mediated
reactions)
Shi Cu Hu Ji (Vinegar Wash; sample application: seborrheic dermatitis)
sophora 20
zanthoxylum 15
rice vinegar (boiled down to reduce volume to 1/10)
Zhi Yi Xi Fang (Seborrhea Wash)
sophora 15
vacarria 30
xanthium 30
alum 9
Baixiefeng Ding (Psoriasis Wash)
sophora 40
cnidium fruit 40
pseudolarix (tujingpi) 20
menthol 10
Cang Bo Niuxi Fang (Atractylodes, Phellodendron, Achyranthes Formula; sample application: diaper rash)
sophora 30
smilax 20
kochia 20
lonicera 20
atractylodes (cangzhu) 10
phellodendron 10
achyranthes 10
capillaris 10
anemarrhena 10
dictamnus 10
alum 10
TOPICAL APPLICATIONS FOR GYNECOLOGICAL DISORDERS
In addition to Qingre Jiedu Xi Ji, listed above for venereal warts, there are several other sophora formulas that have been recommended in the treatment of gynecological disorders. For cervical dysplasia and cancer, Prevention and Treatment of Tumors reports successful use of Kushen Tang (Sophora Decoction, see above) applied daily to the cervix with a piece of gauze (1). For vulvitis, the English-Chinese Encyclopedia of Practical Traditional Chinese Medicine, Vol. 12 (7) recommends Progenital Detergent No. 1, which is a derivative of Kushen Tang, deleting kochia, acorus, and angelica, replacing them with smilax, zanthoxylum, and moutan, and adding 3 grams of borneol at the end of the decoction period (otherwise, borneol is evaporated during decoction). It is used as a sitz bath, for 15–20 minutes twice daily.
For infection accompanied by uterine prolapse (8), a traditional prescription Zigong Tuochui Xi Fang (Washing Formula for Uterine Prolapse), also related to Kushen Tang, is:
sophora 15
cnidium fruit 30
phellodendron 10
lonicera 30
dandelion 30
viola 30
coptis 6
alum 10
Cnidium fruit powder (Shechaungzi San) is a modern prescription recorded in a Shanghai medical journal (8) that is to be made into a sitz bath for vulvar pruritis:
sophora 15
stemona 15
cnidium fruit 15
zanthoxylum 15
alum 15
Two formulas derived from Kushen Tang (proportions of individual ingredients not specified) were mentioned in the recent medical literature as suitable for gynecological disorders. For vaginitis and cervicitis (9):
Yindoa Chongji
stemona
phellodendron
cnidium fruit
forsythia
schizonepeta
alum (kufan)
pseudolarix
atractylodes (cangzhu)
This formula was reported to be 100% effective when applied as a douche 1–2 times daily, with six days equaling one course of therapy; may be repeated as needed.
For vaginal pruritis due to various infections (10), a modified Kushen Tang called Shen Bai Shi was used:
|
sophora |
kochia |
hu-chang |
|
stemona |
hibiscus bark |
gentiana |
|
cnidium fruit |
smilax |
alum |
|
phellodendron |
carpesium |
gall (wubeizi) |
|
zanthoxylum |
dictamnus |
|
This was administered to 700 women over a 20 year period. The treatment time ranged from 7–24 days, with 568 of 700 cases improved (infection resolved).
In general, when using the herb formulas for vaginal douche or sitz bath, a common method recommended in China is to first have the steam from the decoction fumigate the affected area, and then, when the temperature is lower, the liquid is applied directly.
REFERENCES
1. Chang Minyi, Anticancer Medicinal Herbs, 1992 Hunan Science and Technology Publishing House, Changsha.
2. Hson-Mou Chang and Paul Pui-Hay But (eds.), Pharmacology and Applications of Chinese Materia Medica, (2 vols.), 1986 World Scientific, Singapore.
3. Dong Zhi Lin and Yu Shu Fang, Modern Study and Application of Materia Medica, 1990 China Ocean Press, Beijing.
4. Tang W and Eisenbrand G, Chinese Drugs of Plant Origin, 1992 Springer-Verlag, Berlin.
5. Niu Kuizhi, Pharmacology and clinical application of Sophora flavescens, 1996 unpublished manuscript.
6. Shen De-Hui, Wu Xiu-Fen, and Nissi Wang, Manual of Dermatology in Chinese Medicine, 1995 Eastland Press, Seattle, WA.
7. Xu Xiangcai (chief ed.), The English-Chinese Encyclopedia of Practical Traditional Chinese Medicine (vol. 12: Gynecology), 1989 Higher Education Press, Beijing.
8. Huang Bingshan and Wang Yuxia, Thousand Formulas and Thousand Herbs of Traditional Chinese Medicine (vol. 1), 1993 Heilongjiang Education Press, Harbin.
9. Chen Jinfeng, Treatment of 156 cases of vaginitis and cervicitis with Yindao Chongji, Jiangsu Journal of Traditional Chinese Medicine 1985; 6(8): 354–356.
10. He Guoxing, Vaginal lavage and perineal fumigation with herbal drugs in the treatment of 700 patients with vaginitis, Jiangsu Journal of Traditional Chinese Medicine 1991; 12 (10): 445–446.
11. Zhou Chongchu, et.al., Anti-inflammatory and anti-allergic actions of aloprine, ACTA Pharmacologica Sinica 1989; 10(4): 360–365.
12. Wang Xiukun, et.al., Isolation of six alkaloids from the seed of Sophora viciifolia, Chinese Journal of Chinese Materia Medica 1995; 20(3): 168–169.
Figure 1: Matrine (left) and oxymatrine (right).
Figure 2: Sophora flavescens.
Figure 3: Sophora subprostrata (a.k.a. S. tonkinensis).