• Advances in Traditional Medicine
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• v.3 no.2
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• pp.51-55
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• 2003

Resibufogenin is a single compound isolated from the skin venom gland of the toad (Bufo bufo gargarizans cantor). Formulations containing toad venom have been widely used as complementary and alternative medicines. However, like digitalis, resibufogenin possesses both pharmacological and toxicological activities. Our previous data indicated that resibufogenin induces electro-toxicity, including delayed afterdepolarization and triggered arrhythmias at high concentration, both in cardiac fiber in vitro and in beating heart in vivo.

• 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.

• 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.

• Advances in Traditional Medicine
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• v.2 no.1
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• pp.28-35
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• 2002

Toad venom, 'Chan su' in Chinese and 'somso' in Korean, is a well-known traditional oriental medicine obtained from the skin venom gland of the toad. Formulations of toad venom have been widely applied in China, Japan, Korea and other oriental countries for a long time. It is often found in traditional Chinese formulations, such as Jiuxin (or Kyushin in Japan), Yixin, Huoxin, Shexiang baoxin wan, Lu shen wan and Laryngitis pills. According to a pharmaceutical chemistry study, toad venom contains multiple biological active substances, such as bufalin, resibufogenin and cinobufagin. Modern pharmacological studies indicated that toad venom has multiple pharmacological actions, including acting as a cardiotonic, antitumor local anesthetic effects, stimulates the respiratory center, vasopressor action, anti-inflammatory and diuretic effects. Like other medications, toad venom also has certain toxicity and adverse effects, for example, inducing delayed afterdepolarization and triggered arrhythmia. The major chemical constituents, basic pharmacological actions and adverse reactions of toad venom are discussed in this article.

• 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.