• Toxicological Research
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• v.11 no.2
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• pp.175-180
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• 1995

We found that bufalln, one of the prominent components of the bufadlenolides in the Chinese medicine chan'su, has the potent inhibitory effects on growth and proliferation of the cultured bovine aortlc endothelial (BAE) and human umbilical vein endothelial (HUVE) cells. All naturally-occuring bufadienolides used in this study inhibited the cell growth in a dose-dependent manner. Particularly, bufalin among the bufadienolides showed the strongest inhibitory activity for the cell growth. The order of growth inhibition by bufadienolides on BAE cells was as follows: bufalin > gamabufotalln > bufotalln > cinobufagin > cinobufotalin > resibufogenin. The $IC_50$ values (50% inhibition of cell growth) of bufalin as determined by XTT assay were the range of 1-10 nM in BAE and HUVE cells. Bufalin exhibited a higher sensitivity towards cultured bovine aortic endothelial cells than human umbilical vein endothelial cells.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1993.04a
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• pp.72-72
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• 1993

Chan'su the dried toad venom preparation, has been used for centuries as a cardiotonic a local anesthetic and in the treatment of ecphyma. Bufadienol ides are major effective components of Chan'so. Their pharmacological activities have been studies to date. However, their pharmacokinetic and metabolism have not been studied. Considering variously divergent pharmacological actions of bufadienolides we decided to examine their metabolism and their other biological activites. We isolated and purified various components of bufadienolides. Cinobufagin and bufalin are prominent components. Firstly we examined metabolism of cinobufagin and found that this compound was extensively metabolized into various metabolites by mixed-function oxidase and deacetylase.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.11
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• pp.5339-5343
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• 2012

The induction of apoptosis in target cells is a key mechanism for most anti-tumor therapies. Bufalin is a cardiotonic steroid that has the potential to induce differentiation and apoptosis of tumor cells. Research on bufalin has so far mainly involved leukemia, prostate cancer, gastric cancer and liver cancer, and has been confined to in vitro studies. The bufadienolides bufalin and cinobufagin have been shown to induce apoptosis in a wide spectrum of cancer cell. The present article reviews the anticancer effects of bufalin. It induces apoptosis of lung cancer cells via the PI3K/Akt pathway and also suppressed the proliferation of human non-small cell lung cancer A549 cell line in a time and dose dependent manner. Bufalin, bufotalin and gamabufotalin, key bufadienolides, significantly sensitize human breast cancer cells with differing ER-alpha status to apoptosis induction by the TNF-related apoptosis-inducing ligand (TRAIL). In addition, bufadienolides induce prostate cancer cell apoptosis more significantly than that in breast epithelial cell lines. Similar effects have been observed with hepatocellular carcinoma (HCC) but the detailed molecular mechanisms of inducing apoptosis in this case are still unclear. Bufalin exerts profound effects on leukemia therapy in vitro. Results of multiple studies indicate that bufalin has marked anti-tumor activities through its ability to induce apoptosis. Large-scale randomized, double-blind, placebo or positive drug parallel controlled studies are now required to confirm the efficacy and apoptosis-inducing potential of bufalin in various cancers in the cliniucal setting.

• Biomolecules & Therapeutics
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• v.9 no.1
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• pp.51-54
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• 2001

Bufonis Venenum is a toad venom and its main components are bufadienolides, namely resibufogenin, bufalin and cinobufagin. The desensitizing effect of Bufonis Venenum is useful for the treatment of the premature ejaculation in Chinese medicine. But, minor components of Bufonis Venenum cause problems such as topical burring, pain, and erectile dysfunction. To clarify and eliminate the components responsible for these side effects, we prepared two extracts of Bufonis Venenum with either 70% ethanol or ethylacetate and tested their pharmacological effects. The extract of Bufonis Venenum with 70% ethanol produced pain response in rat hind paw, and exhibited contraction of rabbit corpus cavernosal muscle in vitro. On the other hand, the ethylacetate extract did not cause pain and smooth muscle contraction. The desensitizing effect of the ethylacetate extract was similar to that of the 70% ethanol extract. In conclusion, these results show that the extract of Bufonis Venenum with ethylacetate does not have the components causing side effects and deserve further study for therapeutic potential in premature ejaculation in men.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.281.2-281.2
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• 2002

Chan Su the dried toad venom. has been used in Asian countries as the traditional medicine for the purpose of the alleviation of pain, cardiotonic diuresis. hemostasis and et al.. However, Chan Su is the special attention-needed medication because it is known to contain the highly toxic compounds such as bufotenine, an hallucinogen and aphrodisiac, and a series of bufadienolides, cardiotonic steroids that produce physiological symptoms similar to digoxin. (omitted)

• Journal of Acupuncture Research
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• v.26 no.1
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• pp.121-133
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• 2009

Objectives : The purpose of this study is to find out the clinical possibility of Bufonis Venenum used without toxicity and side effect. Methods : We investigated the pharmacological effects, toxicity and processing of Bufonis Venenum through the literatures and studies. Results : Bufonis Venenum is made by parotid gland of dermato gland of Bufo bufo gargarizns or B. melanostictus Schneider, and it is dried for using. The medical ation of Bufonis Venenum are cardiotonic, respiration stimulation, anticancer, topical anesthesia. The toxic symptoms of Bufonis Venenum are relative with digestive, circulatory, nervous system similared with digitalis toxicity. It is important to take 0.015-0.03g by mouth, external use about 1-4% 0.5-3ml and 2-8ml injections by 20ml mix to 5% dextrose fluid. Bufonis Venenum is processed to prevent toxicity and evaluate efficacy by alcohol and milk. There are 68 prescription consisted by Bufonis Venenum in KTKP(Korean Traditional Knowledge Portal). They usually use for antiabcess, anticancer with Moschus moschiferus(麝香), Cinnabar(朱砂). Conclusions : The results from above literary studies show that internal, external medicine and Aqua-acupuncture of Bufonis Venenum could be clinically used to sedative, antiinflammatory, anticancer and topical ataralgesia without toxity through optimum dose and processing.

• Journal of Pharmacopuncture
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• v.15 no.4
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• pp.52-65
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• 2012

Objectives: Toad venom, called Chan-Su, is a traditional Oriental medicine secreted from the auricular and the skin glands of the Bufo bufo gargarizanz Cantor or B. melanosticus Schneider and has been widely used in China, Korea and other parts of Asia for the treatment of pain, heart conditions, and cancer. We examined the concentrations of the main chemical constituents within a commercially available toad venom product and compared the levels for different extraction methods. Methods: Toad venom was extracted using either cold or hot water, ethanol (EtOH), methanol (MeOH), or ethyl acetate (EtOAc), was fractionated using precipitation or reflux, and was then analyzed using thin layer chromatography (TLC), high-performance liquid chromatography (HTLC), and liquid chroma-tography - mass spectrometry (LC-MS). Individual components were identified by comparisons of the retention times, the ultraviolet spectra, and mass spectras and differences in chemical constituents for different solvents and extraction methods are presented. Results: Components with authentic standards, including serotonin and bufodienolides (cinobufagen, bufalin, cinobufalin, and resibufogenin), were detected. The water extract of toad venom contained the greatest amount of serotonin ($75.7{\pm}0.1$ mg/g), but very small amounts of bufodienolides ($3.8{\pm}0.0$ mg/g). In contrast, the use of MeOH or EtOH extraction solutions resulted in 5-26 times higher concentrations of bufodienolides, with only trace amounts of serotonin. The relative and the absolute concentrations of the component also varied based on the extraction method; i.e., EtOH extracts yielded the greatest total amounts of bufodienolides, and EtOAc precipitation had the lowest amounts of bufodienolides. Conclusions: Toad venom consists of serotonin and several bufodienolides, and the choice of solvent to extract chemical the constituents is important as a way to enrich the purported active components for treating different conditions.