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

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.

SUBMITTER: Zhou SW

PROVIDER: S-EPMC9042390 | biostudies-literature | 2021 May

REPOSITORIES: biostudies-literature

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

Zhou Shi-Wen SW Quan Jing-Yu JY Li Zi-Wei ZW Ye Ge G Shang Zhuo Z Chen Ze-Ping ZP Wang Lei L Li Xin-Yuan XY Zhang Xiao-Qi XQ Li Jie J Liu Jun-Shan JS Liu Jun-Shan JS Tian Hai-Yan HY

Journal of natural products 20210421 5

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 extensiv ...[more]

PMID: 33882233

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Project description:Simple Summary In this study, the sexual dimorphism of the limb bones of the Asiatic toad was investigated. Despite male toads having smaller body lengths than females, they possess longer upper arms, forearms, thighs, calves, and feet. Additionally, the humerus and radioulna bones of males are heavier compared to females, and the protrusions on the humerus and femur of males are longer and higher than females. However, female toads have significantly longer hands than males. These sexual differences in limb morphology are believed to be adaptations to specific reproductive behaviors. We propose that the sexual dimorphism in the limb morphology of the Asiatic toad may be attributed to amplexus and male–male competition during the long process of adaptive evolution. Abstract Sexual dimorphism is often considered to be the result of differences in the intensity of sexual selection between sexes. From this point of view, the sexual dimorphism of the limb bones of the Bufo gargarizans in southwest China was studied. Results showed that the fore- and hindlimb skeletons of this species were sexually dimorphic in anatomy. The humerus, radioulna, and total lengths of the forelimb skeleton of males were substantially longer than those of females, but the hand length of males was smaller than that of females. Several other features of males, such as deltoid and medial crest areas and humerus and radioulnar weights, were also significantly larger than those of females. The femoris, tibiofibula, talus–calcaneus, and foot lengths; total hindlimb skeleton length; and femoral upper crest areas of males were significantly greater than those of females. However, no significant intersexual difference in femoris and tibiofibular weights was observed. These findings suggested that robust forelimb bones and long hindlimb bones could contribute to the mating success of males; if so, sexual selection promotes the evolution of sexual size and shape dimorphism in the limb bones of the B. gargarizans.

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

Publications

Bufadienolides from the Eggs of the Toad <i>Bufo bufo gargarizans</i> and Their Antimelanoma Activities.

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