Purpose <p><i>Hemidesmus indicus</i> (L.) R. Br., an Indian ethnomedicinal plant, representative of family Apocynaceae is extensively utilised for its pharmacological activities including antidiabetic, anti-inflammatory, anti-microbial, hepatoprotective and cardioprotective effects. The present study examined the phytochemical composition, antioxidant, genoprotective and antiproliferative activities of <i>H. indicus</i> root fractions.</p> Methods <p>Phytochemical analysis, total phenolic, total flavonoid content analysis and various radical scavenging assays were employed. The genoprotective ability was investigated using single-cell gel electrophoresis technique. Antiproliferative assessment was performed on human neuroblastoma (SH-SY5Y), human colorectal carcinoma (HCT116) and dermal epidermoid carcinoma (A431) cell lines. Spectroscopic analysis was conducted using Gas chromatography and mass spectroscopy (GC-MS), High resolution liquid chromatography and mass spectroscopy (HR-LCMS) and Fourier transform infrared (FT-IR) spectroscopic techniques.</p> Results <p>The results showed that methanolic fraction (Hi-Me) possessed maximum phenolic (427.44&#xa0;mg GAE/g dw), flavonoid content (251.11&#xa0;mg RE/g dw) and scavenged α-diphenyl-β-picrylhydrazyl, hydroxyl, superoxide, lipid peroxyl radicals with IC<sub>50</sub> values of 62.06, 72.25, 170.45 and 84.63&#xa0;µg/mL respectively. Additionally, it exhibited maximal genoprotective effects with DNA content reduction to 4.99% against H<sub>2</sub>O<sub>2</sub> induced oxidative DNA damage in human blood lymphocytes. Furthermore, Hi-Me fraction yielded highest cytotoxic effects at 83.67 and 100.44&#xa0;µg/mL in A431 and HCT116 cancer cells respectively. Furthermore, spectroscopic analysis indicated the enrichment of the Hi-Me fraction with numerous polyphenols. The molecular docking studies validated the observed protective effects of Hi-Me fraction exhibiting strong binding affinities and DNA stabilisation effects.</p> Conclusion <p>The above findings suggest that the methanolic fraction (Hi-Me) contains diverse phytocomponents associated with antioxidant, DNA protective and cytotoxic activities warranting further mechanistic and in vivo investigations for evaluating its therapeutic potential in oxidative stress-related disorders.</p>

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Phytochemical profiling, antioxidant, DNA protective and antiproliferative potential of methanolic fraction of Hemidesmus indicus (L.) R. Br. roots: in vitro and in silico studies

  • Simrandeep Kaur,
  • Rasdeep Kour,
  • Majed Alrobaian,
  • Ashish Kumar,
  • Aman Agrawal,
  • Sandeep Kaur,
  • Vijai Malik,
  • Satwinderjeet Kaur,
  • Sheikh Showkat Ahmad

摘要

Purpose

Hemidesmus indicus (L.) R. Br., an Indian ethnomedicinal plant, representative of family Apocynaceae is extensively utilised for its pharmacological activities including antidiabetic, anti-inflammatory, anti-microbial, hepatoprotective and cardioprotective effects. The present study examined the phytochemical composition, antioxidant, genoprotective and antiproliferative activities of H. indicus root fractions.

Methods

Phytochemical analysis, total phenolic, total flavonoid content analysis and various radical scavenging assays were employed. The genoprotective ability was investigated using single-cell gel electrophoresis technique. Antiproliferative assessment was performed on human neuroblastoma (SH-SY5Y), human colorectal carcinoma (HCT116) and dermal epidermoid carcinoma (A431) cell lines. Spectroscopic analysis was conducted using Gas chromatography and mass spectroscopy (GC-MS), High resolution liquid chromatography and mass spectroscopy (HR-LCMS) and Fourier transform infrared (FT-IR) spectroscopic techniques.

Results

The results showed that methanolic fraction (Hi-Me) possessed maximum phenolic (427.44 mg GAE/g dw), flavonoid content (251.11 mg RE/g dw) and scavenged α-diphenyl-β-picrylhydrazyl, hydroxyl, superoxide, lipid peroxyl radicals with IC50 values of 62.06, 72.25, 170.45 and 84.63 µg/mL respectively. Additionally, it exhibited maximal genoprotective effects with DNA content reduction to 4.99% against H2O2 induced oxidative DNA damage in human blood lymphocytes. Furthermore, Hi-Me fraction yielded highest cytotoxic effects at 83.67 and 100.44 µg/mL in A431 and HCT116 cancer cells respectively. Furthermore, spectroscopic analysis indicated the enrichment of the Hi-Me fraction with numerous polyphenols. The molecular docking studies validated the observed protective effects of Hi-Me fraction exhibiting strong binding affinities and DNA stabilisation effects.

Conclusion

The above findings suggest that the methanolic fraction (Hi-Me) contains diverse phytocomponents associated with antioxidant, DNA protective and cytotoxic activities warranting further mechanistic and in vivo investigations for evaluating its therapeutic potential in oxidative stress-related disorders.