MATRINE AND OXYMATRINE

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MATRINE AND OXYMATRINE

Subjects Of Chinese Research

by Subhuti Dharmananda, Ph.D., Director, Institute for Traditional Medicine,

Portland, Oregon

Matrine and oxymatrine are the two major alkaloid components found in sophora

roots. They are obtained primarily from Sophora japonica (kushen), but also from

Sophora subprostrata (shandougen), and from the above ground portion of Sophora

alopecuroides. The matrines were first isolated and identified in 1958; they are

unique tetracyclo-quinolizindine alkaloids (see Figure 1) found only in Sophora

species thus far. An intensive investigation into the pharmacology and clinical

applications of these alkaloids has gone on for the past decade and remains one

of the focal points of Chinese medical research. The main clinical applications

are treatment of people with cancer, viral hepatitis, cardiac diseases (such as

viral myocarditis), and skin diseases (such as psoriasis and eczema).

The crude herb and crude hot-water extracts of sophora have been available in

the West for more than 25 years. An alkaloid fraction of sophora roots

containing a standardized level of oxymatrine and matrine (20%) was first

introduced by the Institute for Traditional Medicine, and made available to

practitioners in tablet form under the name Oxymatrine (White Tiger) in 1998. It

has been used without reported side effects. In China, the alkaloids are often

given by injection, but this method of administration is not acceptable in the

West, so oral dosing is used here instead. When taken orally, much of the

oxymatrine is converted to matrine; to get high blood levels of oxymatrine, it

must be given by injection. However, it is unclear whether oxymatrine is

clinically more effective than matrine. Chinese researchers have also used the

alkaloids in capsule form, with results that appear similar to the injection.

Sophora is also administered in complex formulas made as decoctions and

taken orally.

Sophora japonica contains about a dozen alkaloids, with matrine and oxymatrine

being by far the highest, together comprising about 2% of the dried root stock

(most of it in the form of oxymatrine), followed by closely related alkaloids:

mainly sophocarpine, but also minute amounts of sophoranol, sophoramine,

sophoridine, allomatrine, isomatrine, and others (see Figure 2). These alkaloids

were first reported as constituents of kushen in a series of publications from

1958-1978.

An overview of recent research on the pharmacology and clinical applications

of the sophora alkaloids is presented below. In general, the dosage of the

sophora alkaloids administered clinically is in the range of 400-600 mg per day.

VIRAL HEPATITIS As described by Chen Yanxi and his colleagues at the Shanghai

Second Medical University (1):

In recent years, oxymatrine has been recommended for treating chronic

hepatitis B and chronic hepatitis C and has been shown effective in clinical

practice. It has been utilized for these applications broadly, but the factors

affecting its efficacy have not yet been determined.

Chen and his group gave oxymatrine injection to patients with hepatitis B. He

confirmed that the viral load declined by this treatment, suggesting that

oxymatrine served to inhibit the viral replication, not just reduce liver

damage, which is the primary and more limited effect of many herbs used for

hepatitis. Antiviral activity, for hepatitis C virus, was confirmed by the same

group in cell culture tests (2). Clinical effectiveness for patients with

hepatitis C had been reported earlier, including reduction of viral load (3).

Oxymatrine may reduce death of liver cells damaged by means other than by

inhibiting viral activity, as indicated in a pharmacology study of liver

protective effects in immune-based liver damage (4).

Kang Junjie and Kang Suqiong, at the Treatment Center for Hepatic Diseases of

the Amoy Municipal Hospital, reported that oxymatrine injection did not cause

side effects other than rare local reactions at the injection site (5). They

used this injection along with oral administration of complex Chinese herb

formulas designed to match symptom-sign complexes and claimed that the effects

were comparable to those attained with interferon therapy, except that adverse

reactions were avoided. In particular, they claimed that the use of oxymatrine

and Chinese herb formulas inhibited liver fibrosis (for further information on

Chinese herbs for this purpose, see: Treatment and prevention of liver

fibrosis). The inhibition of fibrosis appears to be a separate for additional

function of sophora alkaloids beyond inhibiting viral activity. In laboratory

animal studies carried out by Chen Weizhong and his colleagues at the Changzheng

Hospital in Shanghai, matrine was shown to reduce the formation

of liver fibrosis that was caused by chemical damage to the liver (6).

Thus, in relation to viral hepatitis, the sophora alkaloids appear to inhibit

the viral replication, reduce destruction of liver cells, and protect against

fibrosis. It has also been suggested that the alkaloids promote the flow of

bile.

CANCER Sophora subprostrata has long been regarded an anticancer herb in

China. According to cancer specialist Chang Minyi (7), " Sophora subprostrata

works through stimulating the anticancer immune mechanism of the patient and

reinforcing his resistance against the growth of the tumor. " In 1998, Xu Xiangru

and Jiang Jikai, working at the Congqing University of Medical Sciences,

published a review of anticancer activity of sophora alkaloids (8). They relayed

pharmacology studies indicating the alkaloids could inhibit growth of tumor

cells directly, and could also affect immune functions. In clinical work, they

described the use of sophora alkaloids for treating the side effect of

leukopenia caused by cancer chemotherapy or radiation therapy and for treating

certain cancers, notably uterine cervical cancer and leukemia. The herb is also

considered an important ingredient in treatment of esophageal and laryngeal

cancer. In a recent pharmacology study, it was reported that matrine

could help leukemia cells differentiate into mature and normal white blood

cells (9). Nonetheless, sophora alkaloids should not be relied upon as a sole

treatment for cancer, but as an adjunct therapy, as there is no proof that the

herb or these compounds are curative.

CARDIAC DISEASES Sophora and its alkaloids are commonly used in China for

treatment of heart arrhythmias (10). A possible mechanism of action is to help

block sodium and calcium channels, a mechanism relied on by several

antiarrhythmic pharmaceuticals. In a review of sophora alkaloid effects on the

heart, Li Yan and He Liren, at the Affiliated Yueyang Hospital of Shanghai

University of TCM, reported that:

 

sophora total alkaloids or matrine could counteract arrhythmia induced by

many causes;

the total alkaloids or oxymatrine could regulate heart contractility;

the total alkaloids could dilate the coronary artery, increase blood flow,

and improve oxygen delivery to cardiac cells; and

sophora root could counteract the coxsackie virus that causes myocarditis.

Li and He also relayed a clinical report from the Third Clinical Medical

College of Beijing Medical University, about treatment of 167 patients with fast

arrhythmia. The patients received each day 3-10 sophora root tablets (extract of

2 grams crude herb/tablet). The results indicated positive effects on various

kinds of arrhythmia, such as premature systole, paroxysmal ventricular

tachycardia, atrial fibrillation, and sinus tachycardia; the efficacy for

premature systole appeared to be the best. This Beijing study and others were

described also by Niu Kuizhi in his review (12) of clinical applications of

sophora (kushen).

SKIN DISEASES Sophora is frequently used in treatment of skin diseases,

applied topically and consumed orally. One of the primary uses for topical

therapy is treatment of vaginitis, particularly that due to candida infection

(13). Recently, a topical liniment was developed combining sophora's matrine

with the anti-inflammatory flavonoid baicalin from scute (huangqin) for

treatment of eczema, neurodermatitis, and psoriasis (14). This treatment was

reported to be highly effective, especially for eczema, though the number of

cases was small, so that further research must be done. The use of sophora for

psoriasis is a promising new area (15). Zhang Junling and his colleagues at the

Department of Dermatology, Tianjin Changzheng Hospital, studied the mechanism by

which sophora alkaloids reduce psoriasis patches (16). They found that the

alkaloids could inhibit keratinocytes, the cells that reproduce continuously to

produce the characteristic scales.

REFERENCES

Chen Yanxi, et al., Relationship between serum load of HBV-DNA and

therapeutic effect of oxymatrine in patients with chronic hepatitis B, Chinese

Journal of Integrated Traditional Chinese and Western Medicine 2002; 22 (5):

335-336.

Chen YX, et al., The inhibitory effect of oxymatrine on hepatitis C virus in

vitro, Chinese Journal of Liver Diseases 2001; 9 (Supplement): 12-14.

Li Jiqiang, et al., A preliminary study on therapeutic effect of oxymatrine

in treating patients with chronic hepatitis C, Chinese Journal of Integrated

Traditional and Western Medicine, 1998; 18(4): 227-229.

Xiang X, et al., Effect of oxymatrine on murine fulminant hepatitis and

hepatocye apoptosis, Chinese Journal of Medicine, 2002; 115(4); 593-596.

Kang Junjie and Kang Suqiong, 30 cases of chronic hepatitis B treated with

oxymatrine injection combined with syndrome differentiation of Traditional

, Journal of Traditional , 2002; 43(1): 53.

Chen Weizhong, et al., Effect of matrine on experiment rat liver fibrosis,

Chin Journal of New Drugs, 2000; 19(5): 410-412.

Chang Minyi, Anticancer Medicinal Herbs, 1992 Hunan Science and Technology

Publishing House, Changsha.

Xu Xiangru and Jiang Jikai, Recent progress in anticancer bioactivity study

of Sophora flavescens and its alkaloids, Chinese Journal of Integrated

Traditional Chinese and Western Medicine 1998; 4 (3): 235-239.

Zhu Ningxi, et al., Study on inducing and differentiating function and

mechanism of matrine on leukemia cells, ACTA Traditional and

Pharmacology (Shanghai), 2001; 15(1): 43-44.

Ding Guangsheng, Anti-arrhythmia agents in traditional Chinese medicines,

Abstracts of 1987; 1(2): 287-308.

Li Yan and He Liren, Pharmacological study of Sophora alkaloid actions on the

cardiovascular system, Chinese Traditional and Herbal Drugs, 2000; 31(3):

227-229.

Niu Kuizhi, Pharmacology and clinical application of sophora flavescentis,

International Journal of Oriental Medicine 1997; 22(1): 75-81.

Li Xiuying, et al., Treatment of 50 patients with candida albicans vaginitis

by cortex sophorae, Chinese Journal of Integrated Traditional Chinese and

Western Medicine 2000; 6 (2): 146-147.

Ding Ting, et al., The preparing and clinical applications of Complex Matrine

Liniment, ACTA and Pharmacology, 2002; 30(2): 47-48.

Zhang Yaolong, Clinical study on matrine for the treatment of psoriasis,

Hebei Journal of Medical Science, 1996; 69 (2): 590-591.

Zhang Junling, et al., Study on Apoptosis induced by oxymatrine in cultured

keratinocytes, Chinese Journal of Dermatology and Venereology, 2000; 14(6):

367-368.

http://www.itmonline.org/arts/oxymatrine.htm

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Flavescent sophora root (Kushen) Pharmaceutical Name : Radix Sophorae

flavescentis

Botanical Name : Sophora flavescens Ait.

Common Name : Flavescent sophora root

Source of Earliest Record : Shennong Bencao Jing

Part Used & Method for Pharmaceutical Preparations : The roots are dug in

spring or autumn. After the fibrous roots have been removed, the roots are

cleaned, cut into slices and dried in the sun.

Properties & Taste : Bitter and cold

Meridians : Heart, liver, stomach, large intestine and urinary bladder

Functions:

1. To clear heat and dry dampness;

2. To promote urination;

3. To disperse wind and stop itching

Indications & Combinations :

1. Damp-heat syndrome: a) damp-heat jaundiceFlavescent sophora root (Kushen) is

used with Phellodendron bark (Huangbai), Capejasmine (Zhizi), Chinese gentian

(Longdancao) and Oriental wormwood (Yinchenhao); b) damp-heat diarrhea and

dysenteryFlavescent sophora root (Kushen) is used with Costus root (Muxiang) and

Licorice root (Gancao); c) damp-heat leukorrhea and eczema of the

genitalsFlavescent sophora root (Kushen) is used with Phellodendron bark

(Huangbai), Cnidium fruit (Shechuangzi) and Chinese gentian (Longdancao).

2. Skin diseases, including itching of the skin, scabies and impetigo.

Flavescent sophora root (Kushen) can be used internally and externally. The herb

is combined with Chinese angelica root (Danggui), Dittany bark (Baixianpi),

Broom cypress fruit (Difuzi) and Red peony (Chishao).

3. Painful urination caused by damp-heat. Flavescent sophora root (Kushen) is

used with Dandelion herb (Pugongying) and Pyrrosia leaf (Shiwei).

Dosage: 3-10 g

Cautions & Contraindications: This herb should never be used with the herb

Black false bellebore (Lilu). It is contraindicated in cases with weakness and

cold in the spleen and stomach.

http://www.herbalshop.com/tcm/ChineseHerb_F134.html

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Oxymatrine

 

Oxymatrine is a substance found in sophora roots. In a comparison of oxymatrine

versus vitamins in one study, nearly half of 43 patients had reduced their viral

load to non-detectable levels, compared to only one patient taking vitamins,

researchers at the University of Shanghai in China reported.17

However, while liver enzyme levels were higher in the treatment group after

two months of treatment, they were generally the same between both groups after

3 months, the researchers reported.

In the end, Coon and Frist " identified several promising complementary

therapies " , but definitive conclusions couldn't be drawn because of questionable

designs of the studies they had researched.

" More research is warranted to establish the role of these and other therapies

in the treatment of hepatitis C, " they wrote.

http://janis7hepc.com/nutrition1.htm

 

 

 

 

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