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SOURCESTrichosanthes (gualou) refers to the plant Trichosanthes kirilowii. The part of the plant that was original-ly considered important as a med-icine was the fruit (gualou; named the same as the entire plant), which is either used whole (quan-gualou; quan = whole) or subdivid-ed into two components: the peri-carp (gualoupi; pi = peel) and the seed (gualouren; ren = seed). Addi-tionally, trichosanthes root has al-so been adopted into medicinal use, it is called gualougen (gen = root) or tianhuafen (heavenly flower pow-der; the root has a powdery quality). Today, the root is used more often than the fruit for many of the origi-nal applications.

This plant belongs to the gourd family, Curcubitaceae: the fruit of Trichosanthes kirilowii forms a rela-tively spherical gourd (gua= gourd). The common names for trichosanthes in Englishare Chinese cucumber and snakegourd (derived from the long snake-like gourds produced by some other species of Trichosanthes). Trichosanthes fruit is des-cribed in the Shennong Ben-cao Jing (1):

Gualou is bitter and cold. It mainly treats wasting, thirst, generalized fever, vexatious fullness, and great heat. It supplements vacuity, qui-ets the center, and mends expiry and damage. Its oth-er name is dilou. It grows in rivers and valleys as well as shady places in the moun-tains.

MEDICINAL USEAccording to Oriental Materia Medi-ca (2), the pericarp of the fruit is es-pecially used for relieving stagnan-cy of qi circulation in the chest, the seed is especially useful as a mois-tening agent for treating dry con-stipation, the whole fruit possess-es both properties and may be used as a substitute for either of the two. The root was first official-ly described more than 800 years after the fruit in the Tujing Ben-cao (1062 A.D.), though it was brief-ly mentioned earlier (ca. 470 A.D.) in Leigong Paozhi Lun (Discussion of Herb Preparation by Leigong). Trichosanthes root is described as sweet, slightly bitter, and slightly cold, is said to be particularly use-ful for treating diabetes and skin swellings (it is reputed to decrease pus formation and thus treat fu-

TRICHOSANTHESThe phlegm resolving herb

runcles, carbuncles, boils, and ab-scesses). The stalk and leaves of the plant are also used as a folk remedy for feverish diseases. As relayed by Shen Ruoxiang (14):

Trichosanthes fruit is sweet, its na-ture cold, it enters the lungs, stom-ach, and large intestine channels. This product is able to ease the chest and free the diaphragm. It clears heat and transforms phlegm, so it chiefly treats complaints such as lung heat cough with thick, sticky, rattling phlegm, oppressive chest pains, pustulating lung ulcers, and intestinal dryness constipation. Trichosanthes root is sweet, its na-ture cold, and it enters the lung and stomach channels. It is used to clear heat and stop thirst, boost the stomach and generate fluids. It mainly treats patterns involving yin deficiency and fluid injury, diseases

consequent to yin deficien-cy heat, fire poison pustu-lar sores, and middle wasting diabetes.

IN FORMULASTrichosanthes is a promi-nent herb in the ShanghanLun and its companion volume Jingui Yaolue (220 A.D.). Among the formulas mentioned in those texts (3, 4) are the 7 formulas that are still referenced in Chine-se and Japanese medical books today, listed in Table1. In some cases, trichosan-thes root was substituted for the fruit by later herb schol-ars, and this substitution is indicated as such in the in-gredients list presented in

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the Table. In general, these for-mulas are used for chest disorders marked by pain, difficult breathing, and phlegm accumulation, and for disorders in which thirst is a signifi-cant symptom. The prescriptions are small ones, with just 2-7 ingredi-ents, usually including one or more ingredients, aside from trichosan-thes, for treating phlegm-damp ac-cumulations, such as pinellia, oys-ter shell, ginger, or hoelen.

In subsequent Chinese medical works (5), trichosanthes has main-ly been used in large formulas (9 or more ingredients) for treatment of lung disorders that are character-ized by thick phlegm and thirst. Ex-amples of these larger traditional Chinese formulas with trichosan-thes still in use are: Ophiopogon and Trichosanthes Combination (Maimendong Yinzi); Bupleurum and Scute Combination (Chai Xian

Table 1: Formulas of the Shanghan Lun and Jingui Yaolue that contain trichosanthes

Common name Ingredients Indications

Pin Yin

Minor Trichosanthes Combination coptis, pinellia, trichosanthes chest distress, including painXiao Xianxiong Tang seed fullness and pressure, coughing, viscid phlegm

Bupleurum, Cinnamon & Ginger Combination bupleurum, cinnamon chest discomfort’Chaihu Guizhi Ganjiang Tang dry ginger, trichosanthes root accompanied by chills and scute, oyster shell, licorice fever, thirst, sweating

Trichosanthes & Dianthus Formula trichosanthes root, hoelen severe thirst and waterGualou Xiebai Baijiu Tang vinegar or white wine shortness of breath, coughing and phlegm accumulation

Trichosanthes & Cinnamon Combination trichosanthes root, cinnamon, stiffness of the neck and Gualou Guizhi Tang peony, baked licorice, fresh back, accompanied by ginger, jujube aversion to cold and fever with lack of perspiration

Trichosanthes, Bakeri, & Pinellia Comb. trichosanthes fruit, bakeri, chest pain with difficultyGualou Xiebai Banxia Tang pinellia expectorating phlegm

Trichosanthes & Oyster Shell Formula trichosanthes root, oyster thirst accompanying severeGualou Muli San shell fatigue

Tang); and Trichosanthes and Chih-shih Combination (Gualou Zhishi Tang). One of the formulas of few ingredients, Fritillaria and Tricho-santhes Formula (Beimu Gualou San), is comprised of trichosanthes fruit, trichosanthes root, fritillaria, hoelen, red citrus, and platycodon; like the other formulas, it is indicat-ed for phlegm that is difficult to ex-pectorate (thick phlegm) and dry throat (thirst). Modern patent reme-dies (11, 12) for cough and phlegm accumulation sometimes include trichosanthes as an ingredient. Ex-amples are Qingfei Yihuo Pian (with trichosanthes root), Qingchi Huatan Wan (with trichosanthes seed), and Superior Brand Loquat Flavored Syr-up (with trichosanthes seed).The combination of trichosanthes fruit (especially the peel) and bak-eri (xiebai) is considered to provide a harmonizing balance for the cir-culation in the chest. The cold tri-

DRAWING OF TRICHOSANTHESFROM MENGCHUAN BENCAO

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chosanthes moistens and loosens, while the warm bakeri dissipates fluids and frees the flow of qi; to-gether, they “free the flow of yang and move the qi, loosen the chest, and clear the lungs (15).” The in-dication of trichosanthes fruit for chest pain in ancient times in-spired development of this herb in-to a treatment for angina pectoris in modern times. The fruit extract (in tablet form and injection) has been reported effective in treating this coronary disorder (6). Bakeri is a rel-ative of onion and garlic; the lat-ter has been developed as a health product for improving cardiovascu-lar conditions.

TRICHOSANTHES FOR DIABETESThe use of trichosanthes for treat-ing diabetes (see: Treatment of di-abetes with Chinese herbs) may be traced back to the discussions on disease causation by Liu Wansu (ca. 1120-1200 A.D.). He propounded the theory that diseases are usually caused by heat in the body, which should be countered by herbs that had a cold nature. His theory, in re-lation to diabetes, has largely been retained to the present: the initial stage of the disease is treated pri-marily by herbs that clear heat and nourish yin. One of his formulas that is still used for treatment of di-abetes is Ophiopogon and Tricho-santhes Combination (Maimendong Yinzi). Most of the herbs in this for-mula (which is also used for treat-ing of cough with sticky phlegm) have been shown by modern re-search to lower blood sugar.Modern Chinese treatments for dia-betes frequently include trichosan-thes root as an ingredient. For ex-ample, Jiangtang Pian (Reducing Sugar Tablet) is comprised of astra-

galus, polygonatum, trichosanthes root, pseudostellaria, and rehman-nia, and is recommended for those with low levels of insulin, but who are still capable of producing insu-lin. In a clinical trial of this formula, the herbs were administered as ex-tracts in tablet form at a total dose of over 40 grams per day (raw ma-terials equivalent). The herb tharapy was reported to improve sugar tol-erance and elevate the level of se-rum insulin. In the treatment of 405 cases of diabetes with this prepara-tion, 76.5% of the patients were re-ported to have improved sugar tol-erance.

Yuquan Wan (Jade Spring Pill), is a patent formula recommended for diabetes. The extract pills are swal-lowed in large quantities, amount-ing to 36-48 grams per day, and are taken for at least one month. In lab-oratory animal studies, this formula was shown to increase glycogen in liver cells (that is, uptake of sugar by the cells was improved). A sec-ond generation of Jade Spring Pills, comprised of pueraria, trichosanthes root, rehmannia, licorice, and schi-zandra (plus other herbs not men-tioned on the label) were then pro-duced. These pills are indicated in the package labe-ling for the “ill function of the islets of Lan-gerhans.” The instructions are to take a 6 gram dose of the pills four times daily (24 grams of pills per day). Compared to the first gen-eration prod-uct, it is said

on the package insert, the new ver-sion has been clinically proved to have an improved rate of cure, while the dose has been reduced. In a recent clinical evaluation of a Chinese herb formula for diabetes, Jade Spring Pills, used for the con-trol group, was reported to be effec-tive in reducing blood sugar for 79% of cases treated.

INJECTION ADMINISTRATIONOF PROTEIN FRACTIONA protein fraction from trichosan-thes root, called trichosanthin (Fig-ure 5), has been developed into an injection drug in China (7). This compound is destroyed during boil-ing of the herb to make a tea and is degraded by stomach acid and pro-teases when taken orally, so there is little to be absorbed when used as a tea or extract given by the oral route.

The protein (MW 24,000) was de-veloped for clinical use in induc-ing abortion as part of China’s in-tensive birth control policy (“one family: one child”). Dr. Jin Yucai, who worked with this drug in clin-

THE PROTEIN FRACTION TRICHOSANTHIS

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ical practice in China, wrote an ex-tensive review of the compound’s use for abortion in an introduc-tion to the book Compound Q: Tri-chosanthin and Its Clinical Applica-tions (9). There was a comment in Qianjin Yifang (682 A.D.) by the fa-mous scholar Sun Simiao that tri-chosanthes root promotes menstru-al flow; this comment was echoed by Li Shizhen in the Bencao Gang-mu (1578 A.D.) that trichosanthes root can re-establish menstruation and facilitate the expulsion of a re-tained placenta. Since then, tricho-santhes was included in most of the herbal prescriptions for induc-ing abortions. In the 1960s, Chinese researchers examined prescriptions used for that purpose and found that they usually contained both tri-chosanthes root and gleditsia fruit (zaojia). However, it was found that trichosanthes contained the primary abortifacient activity and gleditsia fruit tended to produce some tox-ic symptoms without making a sig-nificant contribution to the intend-ed effect. In 1970, a research group in Shanghai (the main center in Chi-na where development of gyneco-logical treatments with traditional herbal medicine is carried out) iso-lated trichosanthin and produced the injection form. Purity of prepa-ration is important for safe use.Trichosanthin was initially admin-istered by intramuscular injection, but intra-amniotic injection im-proved the efficacy (success rate for

inducing abortion in different stud-ies ranged from 87% to 99%). Tri-chosanthin has also been used to treat ectopic pregnancies, placental tumors, and retained dead fetus.

Because trichosanthin is a protein, a strong antigenicity can devel-op when it is injected, with severe consequences if the agent is used repeatedly (see Toxicity below). Therefore, in China, before using tri-chosanthin injection, a skin test is performed.

Trichosanthes is reputed to have been used in treating breast ab-scess and breast cancer since the Ming Dynasty. Today, trichosan-thin is used as a treatment for some cancers (8), for example, by using 10 mg per day by IV infusion, once or twice per week for malignant hy-datidiform mole (a type of placen-tal tumor). It was also developed as an antiviral therapy for HIV infec-tion (9). In 1990, trichosanthin was viewed by some as the most prom-ising therapy for AIDS, functioning as a ribosome inhibitor that could block viral reproduction. How-ever, its use was limited by the im-munological consequences of any prolonged administration, as ap-peared necessary for HIV treatment. New drugs (introduced in 1995) have proven highly effective for this disease while being administered orally and without the risk of anti-genic reactions.

ACTIVE CONSTITUENTS

In relation to oral consumption, the active constituents of interest in the fruit and root are triterpene sa-ponin alcohols (sterols), present in the amount of about 1%. The dom-inant sterols are camposterol, sito-sterol, and stigmasterol (Figure 6) which are also ingredients in gin-seng (the saponin glycosides of ginseng are related to these com-pounds as well). The sterols may have phlegm-thinning (mucolytic) activity and some antiinflammatory actions. Other members of the Cur-cubitaceae, such as gynostemma (jiaogulan), also contain ginseng-type saponin components. There are some alkaloids (not clearly iden-tified) in the peel, while the seeds are rich in oils (with sterols present in the oil fraction). Another member of this family of gourds, beninca-sa (dongguazi; winter melon seed) is similarly used in China to treat cough due to heat-phlegm, thirst, and dry constipation (its main ingre-dients are fatty oils, and it has ster-ols as well). The starch in the tri-chosanthes root, comprising about 25% of the dry weight, may con-tribute to the action of treating dry throat, since it provides a mucilag-inous substance. The bitter melon, Momoridca charantia, mainly used in Ayurvedic medicine, is consid-ered one of the more valuable treat-ments for diabetes and contains a compound, called “plant insulin,” which may be found in other Curcu-bitaceae gourds. Bitter melon also

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contains a protein (momordicharin, similar to trichosanthin) that has been tried as a treatment for HIV in-fection.

DOSAGETrichosanthes root, fruit, seed, and pericarp are normally administered in doses of 9-15 grams in decoc-tion (or equivalent of dried decoc-tion); trichosanthes seed is some-times used in higher doses, up to 20 grams, in the treatment of con-stipation (its oil lubricates the intes-tines). When powdered and made into pills (as traditionally done with Gualou Qumai Wan), trichosanthes is consumed at a dose of 2-3 grams daily. Trichosanthin is given by in-jection or IV once or twice to in-duce abortion, and repeatedly for treatment of cancer or HIV infec-tion; for IV infusion, 10 mg is sus-pended in 500 ml of normal saline for a one day dose. TOXICITY AND ADVERSE EFFECTSThere are no cautions in most of the traditional Chinese literature about using trichosanthes. In The Illus-trated Chinese Materia Medica (10), it is said that trichosanthes root is contraindicated in “spleen-stom-ach vacuity cold with diarrhea and in patterns without repletion heat.” This contraindication appears to be a direct reflection of the cold nature of trichosanthes. In Chinese Mate-ria Medica: Chemistry, Pharmacol-ogy, and Applications (6), it is men-tioned that use of 9 grams per day of trichosanthes root for one month caused mild nausea and diarrhea in a few patients. However, no gas-tric-irritant substances have been identified in the root (saponins are known to cause gastric irritation at high doses, but the 90 mg that may

be present in the tea is probably not adequate to account for such claimed responses). It is also report-ed that overdosage of the seed may cause gastric discomfort, nausea, vomiting, abdominal pain, and di-arrhea; this is likely due to the high content of oil, as the defatted seed powder produces much milder reac-tions (13).

Trichosanthes fruit is contraindicat-ed in “spleen-stomach vacuity cold with diarrhea and in cold phlegm or damp phlegm” (the fruit is indicat-ed for treatment of hot phlegm that is dry) (10). Trichosanthes fruit ex-tract is used in China in both tablet and injection form for angina pec-toris. Side effects are noted with on-ly the injection form, though infre-quently: 1.7% of cases treated with intravenous administration, but no cases with intramuscular injection (13). An LD50 for trichosanthes peel was reported to be over 300 g/kg by intraperitoneal injection or intra-venous administration in mice. A re-lated fruit from Trichosanthes cu-cumerina is used as food (in soups) in Asia.

As indicated above, the injection of trichosanthin is potentially danger-ous and should not be used in the modern setting where alternatives are available. IV trichosanthin can produce fever, headache, arthralgia, skin rashes, or anaphylactic shock; repeated use can produce neurolog-ic disorders. Literature reports about trichosanthes toxicity in humans are based on the widespread use of the injection form in China rather than oral use of the herb or even in-jection of the whole extract. There-fore, one should be cautious when interpreting the toxicity reports.Although the various Chinese Mate-ria Medica guides indicate no con-traindications for use of trichosan-

thes during pregnancy, it would appear that trichosanthes root should be used cautiously, as high doses may have an abortifacient ef-fect; the fruit, pericarp, and seed have never been suggested to pro-duce a pregnancy-related effect. The small amounts of trichosanthes root typically used in pills and other prepared forms, especially for treat-ment of dry mouth, sticky phlegm, and chest tightness, are not of im-mediate concern, but high doses that are used in some treatments of diabetes, for example, should be avoided during pregnancy. While trichosanthin is largely destroyed after oral consumption, the other components may have some aborti-facient potential (7).wMODERN TRICHOSANTES

PREPARED SPECIES OF TRICHOSANTHESA. SLICES OF WHOLE FRUIT

B. SEEDS - C. WHOLE PEEL - D SLICED PEEL

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BASED FORMULASTrichosanthes fruit, root and seed are commonly used in recent devel-oped formulas. Trichosanthes Fruit Tablets in the Sevens Forest prod-uct range is a typical example. This modern formula is based on Beimu Gualou San (Fritillaria & Trichosan-thes Combination) which is used for the treatment of yellow phlegm, viscous sputum, or dry cough. This symptom pattern usually arises with infections, but may persist for a few days even after an infection has been effectively treated. The traditional formula utilizes fritillaria (chuan beimu), trichosanthes fruit, citrus, and platycodon, four herbs for resolving phlegm accumulation, along with hoelen and trichosan-thes root (which have not been in-cluded here). These latter two herbs are substituted by scute, polygala, and licorice: scute is included to al-leviate lung heat, polygala to help resolve phlegm, and licorice to act as a soothing anti-inflammato-ry. These herbs also provide a mild sedative quality to calm the agita-tion caused by chronic coughing. This formula differs from Belamcan-da 15 and Stemona Tablets, which contain a larger proportion of herbs to treat the infection (clean tox-in), but with a relatively low propor-tion of herbs to resolve phlegm. As such, these other formulas may be more suitable for the initial treat-ment of the disease, to eliminate the infectious agent, while Tricho-santhes Fruit Tablets may be used along with them or later, to resolve phlegm and treat persisting mucus disorder. This formula is also suit-able for treating rhinitis and sinus-itis which is of the phlegm-heat type.

REFERENCES

TRICHOSANTHES FRUIT TABLETS

INGREDIENTS

Trichosanthes fruit gualouFritillaria chuanbeimuPlatycodon jiegengScute huangqinPolygala yuanzhiCitrus chenpiLicorice gancao

GENERAL ACTIVITIES

resolve hot phlegm

SAMPLE INDICATIONS

colored mucus, thick sputum, chest congestion

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