Background Litsea ghatica C.J. Saldanha belongs to the evergreen family Lauraceae, endemic to the Western Ghats of India. Our laboratory has studied the phytochemistry and biological activity of solvent extracts of this plant since 2018 (Tiwari and Khan in Indian Drugs 60(1):44-49, <CitationRef CitationID="CR1">2023</CitationRef>). Objective The present work reports the potential of an endemic plant L. ghatica in therapeutics. The objective of this research was to evaluate the cytotoxic activity of L. ghatica bark and identify some secondary metabolites in the same. Methods The total phenolic and flavonoid content of the toluene, dichloromethane, methanol extracts and flavonoid rich fraction of the bark of L. ghatica was estimated using Folin-Ciocalteu and aluminium chloride spectrophotometric assays respectively. The antioxidant activity of these extracts and the flavonoid rich fraction was evaluated using DPPH and nitric oxide assays. HPTLC fingerprints were developed as a standardization tool for the same. Bioactivity guided fractionation yielded active fractions that were analysed by LCMS. In silico studies like target prediction, molecular docking and ADME prediction were conducted on the identified constituents to identify potential molecular targets. The cytotoxic activity of the extracts and fractions thereof were evaluated in breast cancer (MCF-7, MDA-MB-231), cervical cancer (HeLa), and lymphoma (U-937) cell lines using the Sulforhodamine assay. Results The methanol extract exhibited promising antioxidant activity versus the standard quercetin. The aqueous methanol fraction of DCM extract exhibited potent cytotoxicity in HeLa and MCF-7 cell lines. The LCMS studies identified the presence of several secondary metabolites some of which are could be responsible for the cytotoxic activity. Of these, Apigenin7-(6’’-E-pcoumaroylgalactoside), Epicatechin-(4beta-6)-epicatechin-(2beta-7,4beta-8)-epicatechin, Cynaroside and Castillene A emerged to be top four VEGF inhibitors with good binding scores with this target. Conclusion Phytochemical analysis of L. ghatica provides new evidence of the presence of cytotoxic secondary metabolites having potential antioxidant activity. The in silico studies further confirmed that some of these compounds exhibit strong binding affinity to the VEGF receptor, indicating their potential as hits/leads for development as anticancer agents. The ADME studies of the identified compounds supported their utility as lead like molecules for further developmental studies.

Phytochemical Investigations and Cytotoxic Activity of Litsea ghatica, an Endemic Plant from Western Ghats of India

期刊论文
发表日期：

2025年10月29日

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Sayali Churi,
Tabassum Khan,
Sahaya Nadar

摘要

Background

Litsea ghatica C.J. Saldanha belongs to the evergreen family Lauraceae, endemic to the Western Ghats of India. Our laboratory has studied the phytochemistry and biological activity of solvent extracts of this plant since 2018 (Tiwari and Khan in Indian Drugs 60(1):44-49, 2023).

Objective

The present work reports the potential of an endemic plant L. ghatica in therapeutics. The objective of this research was to evaluate the cytotoxic activity of L. ghatica bark and identify some secondary metabolites in the same.

Methods

The total phenolic and flavonoid content of the toluene, dichloromethane, methanol extracts and flavonoid rich fraction of the bark of L. ghatica was estimated using Folin-Ciocalteu and aluminium chloride spectrophotometric assays respectively. The antioxidant activity of these extracts and the flavonoid rich fraction was evaluated using DPPH and nitric oxide assays. HPTLC fingerprints were developed as a standardization tool for the same. Bioactivity guided fractionation yielded active fractions that were analysed by LCMS. In silico studies like target prediction, molecular docking and ADME prediction were conducted on the identified constituents to identify potential molecular targets. The cytotoxic activity of the extracts and fractions thereof were evaluated in breast cancer (MCF-7, MDA-MB-231), cervical cancer (HeLa), and lymphoma (U-937) cell lines using the Sulforhodamine assay.

Results

The methanol extract exhibited promising antioxidant activity versus the standard quercetin. The aqueous methanol fraction of DCM extract exhibited potent cytotoxicity in HeLa and MCF-7 cell lines. The LCMS studies identified the presence of several secondary metabolites some of which are could be responsible for the cytotoxic activity. Of these, Apigenin7-(6’’-E-pcoumaroylgalactoside), Epicatechin-(4beta-6)-epicatechin-(2beta-7,4beta-8)-epicatechin, Cynaroside and Castillene A emerged to be top four VEGF inhibitors with good binding scores with this target.

Conclusion

Phytochemical analysis of L. ghatica provides new evidence of the presence of cytotoxic secondary metabolites having potential antioxidant activity. The in silico studies further confirmed that some of these compounds exhibit strong binding affinity to the VEGF receptor, indicating their potential as hits/leads for development as anticancer agents. The ADME studies of the identified compounds supported their utility as lead like molecules for further developmental studies.