2. Academic Validation
  3. Bufadienolides from the Eggs of the Toad Bufo bufo gargarizans and Their Antimelanoma Activities

Bufadienolides from the Eggs of the Toad Bufo bufo gargarizans and Their Antimelanoma Activities

  • J Nat Prod. 2021 May 28;84(5):1425-1433. doi: 10.1021/acs.jnatprod.0c00840.
Shi-Wen Zhou 1 2,  Jing-Yu Quan 3,  Zi-Wei Li 1,  Ge Ye 1,  Zhuo Shang 4,  Ze-Ping Chen 1,  Lei Wang 1,  Xin-Yuan Li 1,  Xiao-Qi Zhang 1,  Jie Li 4,  Jun-Shan Liu 3,  Hai-Yan Tian 1 4
Affiliations

Affiliations

  • 1 Institute of Traditional Chinese Medicine and Natural Products, College of Pharmacy, Jinan University, Guangzhou 510632, People's Republic of China.
  • 2 Department of Biomedical Sciences, City University of Hong Kong, Hong Kong, SAR 999077, People's Republic of China.
  • 3 Guangdong Provincial Key Laboratory of Chinese Medicine Pharmaceutics, School of Traditional Chinese Medicine, Southern Medical University, Guangzhou 510515, People's Republic of China.
  • 4 Department of Chemistry and Biochemistry, University of South Carolina, Columbia, South Carolina 29208, United States.
PMID: 33882233 DOI: 10.1021/acs.jnatprod.0c00840
Abstract

Toads produce potent toxins, named bufadienolides, to defend against their predators. Pharmacological research has revealed that bufadienolides are potential Anticancer drugs. In this research, we reported nine bufadienolides from the eggs of the toad Bufo bufo gargarizans, including two new compounds (1 and 3). The chemical structures of 1 and 3, as well as of one previously reported semisynthesized compound (2), were elucidated on the basis of extensive spectroscopic data interpretation, chemical methods, and X-ray diffraction analysis. Compound 1 is an unusual 19-norbufadienolide with rearranged A/B rings. A biological test revealed that compounds 2 and 4-8 showed potent cytotoxic activities toward human melanoma cell line SK-MEL-1 with IC50 values less than 1.0 μM. A preliminary mechanism investigation revealed that the most potent compound, 8, could induce Apoptosis via PARP cleavage, while 5 and 6 significantly suppressed angiogenesis in zebrafish. Furthermore, an in vivo biological study showed that 5, 6, and 8 inhibit SK-MEL-1 cell growth significantly.

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