C23 steroids from the venom of Bufo bufo gargarizans.
Five new C23 steroids (1-5) together with five known bufadienolides (6-10) were isolated from the venom of Bufo bufo gargarizans (ChanSu in Chinese). The structures of the new steroids were elucidated by extensive spectroscopic methods in combination with X-ray diffraction analysis. Among these C23 steroids, only compound 3 showed cytotoxicities against HepG2 and A549 cancer cells, with respective IC50 values of 26.8 ± 8.3 and 45.6 ± 2.5 μM. In contrast, the bufadienolides (7-10) displayed potent inhibitory activities against these cancer cells, with respective IC50 values in the ranges 0.5-5.5 and 0.6-6.5 μM, but relatively less cytotoxicity on normal mouse spleen cells. In addition, the Na(+)/K(+)-ATPase inhibitory activities of 2, 5, and 7 revealed that the lactone moiety of a bufadienolide was important for the inhibitory activity.
Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University , Guangzhou 510632, People's Republic of China.
Hai-Yan
HY
Tian
Shi-Lin
SL
Luo
Jun-Shan
JS
Liu
Lei
L
Wang
Ying
Y
Wang
Dong-Mei
DM
Zhang
Xiao-Qi
XQ
Zhang
Ren-Wang
RW
Jiang
Wen-Cai
WC
Ye
D000664:Amphibian Venoms / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D002018:Bufanolides / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D002023:Bufo bufo; D002681:China; D004354:Drug Screening Assays, Antitumor; D056945:Hep G2 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D008815:Mice, Inbred Strains; D015394:Molecular Structure; D000254:Sodium-Potassium-Exchanging ATPase / Q000037:antagonists & inhibitors; D013154:Spleen / Q000166:cytology / Q000187:drug effects; D013329:Structure-Activity Relationship
D000664:Amphibian Venoms; D000970:Antineoplastic Agents; D002018:Bufanolides; C095591:chan su; D000254:Sodium-Potassium-Exchanging ATPase