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Cytotoxic polyhydroxylated pregnane glycosides from Cissampelos pareira var. hirsuta.

ABSTRACT: Fourteen new polyhydroxylated pregnane glycosides, cissasteroid A-N (1-14), and five known analogues (15-19), were isolated from the dried whole plant of Cissampelos pareira var. hirsuta. Their structures and stereochemistry were elucidated by extensive spectroscopic data, chemical hydrolysis, and ECD measurements. All the compounds were tested for their cytotoxicity against five human cancer cell lines, and inhibitory activity against NO release in LPS-induced RAW 264.7 cells. Compared with cisplatin, compound 7 showed more potent cytotoxicities against the HL-60, A549, SMMC-7721, MCF-7, and SW480 cell lines, with IC₅₀ values of 2.19, 14.38, 2.00, 7.58, and 7.44 μM, respectively. The preliminary study of structure-activity relationship indicated that benzoic acid esterification at C-20 may have a negative effect on the cytotoxic activity of polyhydroxylated pregnane derivatives in these five human cancer cell lines. These results revealed the potential of compound 7 as an ideal antitumor lead compound.

SUBMITTER: Sun YJ

PROVIDER: S-EPMC8693877 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature

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Cytotoxic polyhydroxylated pregnane glycosides from Cissampelos pareira var. hirsuta.

Sun Yan-Jun YJ Chen Hao-Jie HJ Han Rui-Jie RJ Zhao Chen C Si Ying-Ying YY Li Meng M Du Kun K Chen Hui H Feng Wei-Sheng WS

RSC advances 20211222 1

Fourteen new polyhydroxylated pregnane glycosides, cissasteroid A-N (1-14), and five known analogues (15-19), were isolated from the dried whole plant of Cissampelos pareira var. hirsuta. Their structures and stereochemistry were elucidated by extensive spectroscopic data, chemical hydrolysis, and ECD measurements. All the compounds were tested for their cytotoxicity against five human cancer cell lines, and inhibitory activity against NO release in LPS-induced RAW 264.7 cells. Com ...[more]

PMID: 35424474

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Project description:BackgroundViral infections have a history of abrupt and severe eruptions through the years in the form of pandemics. And yet, definitive therapies or preventive measures are not present. Herbal medicines have been a source of various antiviral compounds such as Oseltamivir, extracted using shikimic acid from star anise (Illicium verum) and Acyclovir from Carissa edulis are FDA (Food and Drug Administration) approved antiviral drugs. In this study, we dissect the anti-coronavirus infection activity of Cissampelos pareira L (Cipa) extract using an integrative approach.MethodsWe analysed the signature similarities between predicted antiviral agents and Cipa using the connectivity map ( https://clue.io/ ). Next, we tested the anti-SARS-COV-2 activity of Cipa in vitro. Molecular docking analyses of constituents of with key targets of SARS-CoV2 protein viz. spike protein, RNA‑dependent RNA‑polymerase (RdRp) and 3C‑like proteinase. was also performed. A three-way comparative analysis of Cipa transcriptome, COVID-19 BALF transcriptome and CMAP signatures of small compounds was also performed.ResultsSeveral predicted antivirals showed a high positive connectivity score with Cipa such as apcidin, emetine, homoharringtonine etc. We also observed 98% inhibition of SARS-COV-2 replication in infected Vero cell cultures with the whole extract. Some of its prominent pure constituents e.g. pareirarine, cissamine, magnoflorine exhibited 40-80% inhibition. Comparison of genes between BALF and Cipa showed an enrichment of biological processes like transcription regulation and response to lipids, to be downregulated in Cipa while being upregulated in COVID-19. CMAP also showed that Triciribine, torin-1 and VU-0365114-2 had positive connectivity with BALF 1 and 2, and negative connectivity with Cipa. Amongst all the tested compounds, Magnoflorine and Salutaridine exhibited the most potent and consistent strong in silico binding profiles with SARS-CoV2 therapeutic targets.

Dataset Information

Cytotoxic polyhydroxylated pregnane glycosides from Cissampelos pareira var. hirsuta.

Publications

Cytotoxic polyhydroxylated pregnane glycosides from <i>Cissampelos pareira</i> var. <i>hirsuta</i>.

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