• Journal of Life Science
• /
• v.27 no.1
• /
• pp.95-99
• /
• 2017

A previous study demonstrated that four kinds of natural compounds, Corydaline, (${\pm}$)-Car-3-ene-2,5-dione, cinobufagin, and corilagin, enhanced the gene expression of ERAP1 and FOXO1 (DFA16) more than two-fold in a cell culture system. In this study, the experimental food was made finally 30 ml in which included 1% agar, 5% sucrose, and each natural compound $20{\mu}l$. A fruit fly of Drosophila melanogaster fed a natural product for 4 hr after 4 hr starvation. Both natural compounds of Cinobufagin and Corilagin induced 6-8 days more survival comparing than it controls group. The resulting fruit flies were estimated the gene expression of ERAP1 and FOXO1 by RT-PCR that also demonstrated meaningful results with the same lifespan results. Cinobufagin from BufonisVenennumis has $C_{26}H_{34}O_6$ molecular formula and 442 kDa molecular weight. Corilagin from Euphorbiapekinensisis has $C_{27}H_{22}O_{18}$ molecular formula and 634 kDa molecular weight. The two types of natural products screened in this study will be used in the early diagnosis and treatment of insect industry in the near future. In addition, the natural products will be used in longevity experiments in a mouse model. The results may give one of the clues for studying new drug development candidates of the longevity.

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

• Journal of Life Science
• /
• v.26 no.3
• /
• pp.359-363
• /
• 2016

We have screened four natural products against 640 single compounds, which shows more two folds gene expression for both endoplasmic reticulum aminopeptidase 1 (ERAP1) and FOXO-family transcription factor (FOXO1). The results were as follows. (±)-Car-3-ene-2,5-dione from Asarum sieboldii Miq. is C₁₀H₁₂O₂ molecular formula and the 164 kDa molecular weight. Cinobufagin from Bufonis Venennum is C₂₆H₃₄O₆ molecular formula and 442 kDa molecular weight. So far reported main biological function is Na⁺/K⁺-ATPase inhibition. Corilagin from Euphorbia pekinensis is C₂₇H₂₂O₁₈ molecular formula and 634 kDa molecular weight. Carbonic anhydrase inhibition is well known its biological function. Corydaline from Corydalis turtschaninovii is C₂₂H₂₇NO₄ molecular formula and 369 kDa molecular weight. The main biological function is acetylcholinesterase inhibition. In the short future, four types of natural products will be used in longevity experiments with insects. The results may give one of the clues for studying new drug development candidates of the longevity.

• Biomolecules & Therapeutics
• /
• v.9 no.1
• /
• pp.51-54
• /
• 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
• /
• v.11 no.2
• /
• pp.175-180
• /
• 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
• /
• v.2 no.1
• /
• pp.28-35
• /
• 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 Convergence for Information Technology
• /
• v.7 no.6
• /
• pp.89-95
• /
• 2017

Cancer-inducing PMA stimulates cells to increase the expression of transcription factor c-Jun/c-fos and then increase the activity of AP-1 in the nucleus. The activity of AP-1 has been reported to cause cancer. In this study, We conducted cytotoxicity experiments to assess the safety of natural marker compounds and also observed inhibition of activator protein(AP-1) activity to predict cancer-preventing effects. The results of this experiment indicated that arctigenin, manassantin A, and B can predict the development of cancer prevention agents.

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