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Journey Describing the Cytotoxic Potential of Withanolides: A Patent Review

[ Vol. 13 , Issue. 4 ]


Hidayat Hussain*, Rene Csuk, Ivan R. Green, Najeeb Ur Rehman, Ghulam Abbas and Wahid Hussain   Pages 411 - 421 ( 11 )


Withanolides are C-28 ergostane steroids known to demonstrate some very interesting therapeutic properties. Numerous withanolides have been isolated from a variety of different plant species and can be employed to treat various types of cancers. Withanolides are indeed capable of demonstrating excellent anticancer, anti-inflammatory, and neuroprotective activities. Additionally, libraries of prepared withaferin A analogs incorporating an acyl, sulphate, amide and aldehyde functionality have demonstrated the most potential response. It is of particular interest to note that an acetyl group at either C-4, C-19 or C-27 enhances the anticancer effects. Since the majority of natural withanolides reported in patents are classified as “Type-A”, it is our opinion that there should now be a focus on developing “Type-B” withanolides and an investigation into their various therapeutic applications. Moreover, very little real innovation in synthetic methodologies has been reported which opens up huge possibilities for novel synthetic methodologies to be developed for the production of larger libraries new withanolides and their analogs to incorporate chemical diversity. In addition, since withanolides have the capability to conjugate with other anticancer compounds, this should encourage scientists to prepare lead compounds in cancer drug discovery.


Anticancer, drug discovery, ergostane steroids, in vitro, natural products, withanolide.


Leibniz Institute of Plant Biochemistry, Department of Bioorganic Chemistry, Weinberg 3, D-06120 Halle (Salle), Martin-Luther-University Halle-Wittenberg, Organic Chemistry, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Department of Chemistry and Polymer Science, University of Stellenbosch, Private Bag X1, Matieland, Stellenbosch 7600, UoN Chair of Oman’s Medicinal Plants and Marine Natural Products, University of Nizwa, P. O. Box 33, Birkat Al Mauz, Nizwa 616, Department of Biological Sciences and Chemistry, College of Arts and Sciences, University of Nizwa, Nizwa-616, Department of Botany, GPGC Parachinar Kurram Agency

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