Synthesis，anti-melanoma activity and acute toxicity of aporphine alkaloids in zebrafish

WAN Yili; ZHONG Hui; CHEN Li; SUN Jianbo

doi:10.11665/j.issn.1000-5048.20210503

Journal of China Pharmaceutical University > 2021 > 52(5): 529-535. > DOI: 10.11665/j.issn.1000-5048.20210503

WAN Yili, ZHONG Hui, CHEN Li, SUN Jianbo. Synthesis，anti-melanoma activity and acute toxicity of aporphine alkaloids in zebrafish[J]. Journal of China Pharmaceutical University, 2021, 52(5): 529-535. DOI: 10.11665/j.issn.1000-5048.20210503

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Synthesis，anti-melanoma activity and acute toxicity of aporphine alkaloids in zebrafish

School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009, China

Funds: This study was supported by the National Natural Science Foundation of China (No.31870325, No.31500277)

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Received Date: March 28, 2021
Revised Date: September 13, 2021

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Abstract

Abstract

In this study, 10 aporphine alkaloids were synthesized with 1, 2-methylenedioxy substituent in ring A and 9, 10, 11-position with different substituents in ring D. Their structures were determined by ESI-MS,¹³C NMR and ¹H NMR.The potencial antitumor activity of these compounds against B16F10 melanoma cells were evaluated by MTT assay, and their structure-activity relationship was further analyzed.Meanwhile, zebrafish acute toxicity test was conducted to evaluate the safety of the active compounds.The results showed that some compounds had strong inhibitory activity on tumor cells, and could significantly inhibit the proliferation of B16F10 melanoma cells.Compound IVa has the best anti-melanoma activity with wide safety range, and can be used as a lead compound for further study on anti-proliferation of B16F10 melanoma cells.
- aporphine alkaloids,
- synthesis,
- melanoma,
- safety evaluation,
- structure activity relationship

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