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Indian Journal of Pharmaceutical Education and ResearchNOW IN
Article

In silico Study, Protein Kinase Inhibition and Antiproliferative Potential of Flavonoids Isolated from Bassia eriophora (Schrad.) Growing in KSA

Arafa Musa1,2, Mohammad Mahmoud Al-Sanea3, Nasser Hadal Alotaibi4, Taghreed Stum Alnusaire5, Shaimaa Rashad Ahmed1,6, Ehab Mohamed Mostafa1,2★★ Corresponding author

  1. 1Department of Pharmacognosy, College of Pharmacy, Jouf University, Sakaka, Aljouf 72341, SAUDI ARABIA.
  2. 2Department of Pharmacognosy, Faculty of Pharmacy, Al-Azhar University, Cairo 11371, EGYPT.
  3. 3Pharmaceutical Chemistry Department, College of Pharmacy, Jouf University, Sakaka, Aljouf 72341, SAUDI ARABIA.
  4. 4Department of Clinical Pharmacy, College of Pharmacy, Jouf University, Sakaka, Aljouf 72341, SAUDI ARABIA.
  5. 5Biology Department, College of Science, Jouf University, Sakaka, Aljouf 72341, SAUDI ARABIA.
  6. 6Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo 11562, EGYPT.

CORRESPONDENCE

Ehab Mohamed Mostafa

Department of Pharmacognosy, College of Pharmacy, Jouf University, Sakaka, Aljouf 72341, SAUDI ARABIA.

emmoustafa@ju.edu.sa

Received: 20-07-2020; Revised: 22-12-2020; Accepted: 01-03-2021.

Volume 55, Issue 2 · pp. 483–490 · PUBLISHED 2021 · DOI: 10.5530/ijper.55.2.86

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ABSTRACT

Introduction: Kinase enzymes play an important role in cellular proliferation, the main target in cancer treatment is to inhibit their functions. Protein kinase inhibitors as flavonoids can be applied for prevention or treatment of cancers through inhibition of cell proliferation. Objectives: To isolate cytotoxic metabolites from B. eriophora, evaluate their antiproliferative and protein kinase inhibitory effects, as well as the in silico study for active compounds. Materials and Methods: Preparative HPLC was used for purification of the isolates. NMR, MS and UV spectroscopy were applied for characterization of the pure compounds. Sulphorhodamine-B and radiometric assay methods were employed for determination of the antiproliferative and protein kinase inhibition activities, respectively. The antiproliferative mechanism was predicted by in silico study using Molecular Operating Environment (MOE). Results: Five flavonoids; luteolin, acacetin-7-O-β-D-glucoside, diosmin, kaempferol-3-O-rutinoside and rutin were isolated and investigated for their antiproliferative and kinase inhibitory effects. Luteolin exhibited strong antiproliferative effect against certain cell lines including MCF-7, HepG2 and HCT-116 with IC50 (33.24 ± 0.83, 26.54 ±1.02 and 31.62 ±1.32 μM, respectively), while diosmin and kaempferol- 3-O-rutinoside showed strong antiproliferative effect against MCF-7 with IC50 (26.56 ± 1.12 and 28.72 ±0.98). Luteolin showed highest inhibitory effect against Aurora B and CDK4/CyclinD1 with IC50 3.16 and 4.95 m3.16 and 4.95 inhibitin slico study for the isolated metabolites against Aurora B and CDK4/CycD1 confirmed their cytotoxic profile. Conclusion: Five flavonoids were firstly isolated from B. eriophora. The putative antiproliferative mechanism of luteolin and kaempferol-3-O-rutinoside on Aurora B and CDK4/CycD1 kinases was predictable by in slico study.

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    Musa, A., Al-Sanea, M. M., Alotaibi, N. H., Alnusaire, T. S., Ahmed, S. R., & Mostafa, E. M. (2021). In silico Study, Protein Kinase Inhibition and Antiproliferative Potential of Flavonoids Isolated from Bassia eriophora (Schrad.) Growing in KSA. Indian Journal of Pharmaceutical Education and Research, 55(2), 483–490. https://doi.org/10.5530/ijper.55.2.86