Resibufagin
(Synonyms: 脂蟾毒精) 目录号 : GC65288Resibufagin 是一种从 "Chan'Su" 中分离的蟾蜍二烯羟酸内酯,具有抗肿瘤活性。
Cas No.:20987-24-0
Sample solution is provided at 25 µL, 10mM.
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Resibufagin is a kind of bufadienolide isolated from the venom of Bufo bufo gargarizans, has anti-tumor activities[1].
[1]. Li Qiao, et al. One new bufadienolide from Chinese drug "Chan'Su". J Asian Nat Prod Res
Cas No. | 20987-24-0 | SDF | Download SDF |
别名 | 脂蟾毒精 | ||
分子式 | C24H30O5 | 分子量 | 398.49 |
溶解度 | 储存条件 | 4°C, away from moisture and light | |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.5095 mL | 12.5474 mL | 25.0947 mL |
5 mM | 0.5019 mL | 2.5095 mL | 5.0189 mL |
10 mM | 0.2509 mL | 1.2547 mL | 2.5095 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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2.
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One new bufadienolide from Chinese drug "Chan'Su"
J Asian Nat Prod Res 2008 Mar-Apr;10(3-4):233-7.PMID:18335338DOI:10.1080/10286020701604839.
A new bufadienolide named 16beta-acetoxy-bufarenogin (1), together with six known bufadienolides, namely, 11alpha,12beta-dihydroxy-bufalin (2), bufotalin (3), hellebrigenin (4), desacetylbufotalin (5), gamabufotalin (6), and Resibufagin (7) were isolated from Chan'Su. Of these, 2 was a new natural product. Their structures were elucidated by spectral methods. The cytotoxic activities in vitro of these compounds have been assayed against HeLa cell line. They all showed strong cytotoxic activities.
[Inhibitory effect of total bufadienolides from toad venom against H22 tumor in mice and their metabolites]
Zhongguo Zhong Yao Za Zhi 2011 Nov;36(21):2987-93.PMID:22308689doi
Objective: To evaluate the inhibitory effect of total bufadienolides from toad venom against H22 tumor in mice and preliminarily analyze the structures of the metabolites in tissues. Method: HPLC and LC-MS were used for analysis of the chemical composition of TBFs. High, middle and low dosages of TBFs were orally administered or intra-peritoneally injected to H22 tumor-bearing mice for thirteen days. The animals were killed and the tumors were stripped and weighed. The metabolites in the tissues such as heart, liver, spleen, lung and kidney, were analyzed by HPLC and LC-MS. Result: The chemical composition of TBFs were identified by comparison of the retention times with those of reference substances, on-line UV spectra and MS data. Its main components are concerned with gamabufotalin, arenobufagin, bufotalin, Resibufagin, cinobufotalin, bufalin, cinobufagin and resibufogenin. TBFs had no obvious influence on body weight of H-22 tumor-bearing mice orally administered and the inhibition rate against tumor were 14.76%, 16.38% and 10.32% for low (5 mg x kg(-1)), middle (10 mg x kg(-1)) and high dosage (20 mg x kg(-1)), respectively. The mice intra-peritoneally injected with middle and high-dose of TBFs gained body weight slower than the control mice on the 5th day and recovered on the 13th day. The inhibition rate against tumor were 17.30%, 19.80% and 40.95% for low (1.5 mg x kg(-1)), middle (3 mg x kg(-1)) and high dose (6 mg x kg(-1)), respectively. The inhibitory effect took on dose-dependent manner. Based on the HPLC analyses on heart, liver, spleen, lung and kidney, bufadienolides were found in the liver tissue and 11 compounds of them were tentatively identified by LC-DAD-MS. Conclusion: TBFs by oral administration had no inhibitory effect against H22 tumor in mice, however, TBFs by intra-peritoneal injection displayed the significantly inhibitory effect, accompanying some toxicity for early duration of the study. The identification of bufadienolides in the liver provides a good basis for the further investigation of the metabolic pathways of TBFs in vivo.
[Systematic comparison of two kinds of Bufonis Venenum derived from different Bufo gargarizans subspecies based on metabolomics and antitumor activity]
Zhongguo Zhong Yao Za Zhi 2023 Mar;48(5):1280-1288.PMID:37005812DOI:10.19540/j.cnki.cjcmm.20220627.202.
This paper compared the differences between two kinds of Bufonis Venenum produced by Bufo gargarizans gargarizans and B. gararizans andrewsi, and verified the rationality of the market value orientation of Bufonis Venenum based on the zebrafish mo-del. Twenty batches of Bufonis Venenum from Jiangsu province, Hebei province, Liaoning province, Jilin province, and Liangshan, Sichuan province, including B. gargarizans gargarizans and B. gararizans andrewsi, were collected. The UHPLC-LTQ-Orbitrap-MS combined with principal component analysis was used to compare the differences between two kinds of Bufonis Venenum. According to the limiting conditions of VIP>1, FC<0.5 or FC>2.0, and peak total area ratio>1%, 9 differential markers were determined, which were cinobufagin, cinobufotalin, arenobufagin, resibufogenin, scillaredin A, Resibufagin, 3-(N-suberoylargininyl)-arenobufagin, 3-(N-suberoylargininyl)-marinobufagin, and 3-(N-suberoylargininyl)-resibufogenin. The content of 20 batches of Bufonis Venenum was determined according to the Chinese Pharmacopoeia(2020 edition) by high-performance liquid chromatography, and the 2 batches of Bufonis Venenum, CS7(8.99% of total content) and CS9(5.03% of total content), with the largest difference in the total content of the three quality control indexes of the Chinese Pharmacopoeia(bufalin, cinobufagin, and resibufogenin) were selected to evaluate their anti-liver tumor activity based on the zebrafish model. The tumor inhibition rates of the 2 batches were 38.06% and 45.29%, respectively, proving that only using the quality control indexes of the Chinese Pharmacopoeia as the value orientation of Bufonis Venenum market circulation was unreasonable. This research provides data support for the effective utilization of Bufonis Venenum resources and the establishment of a rational quality evaluation system of Bufonis Venenum.