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Abstract Title:

Biopharmacological considerations for accelerating drug development of deguelin, a rotenoid with potent chemotherapeutic and chemopreventive potential.

Abstract Source:

Cancer. 2019 Jun 1 ;125(11):1789-1798. Epub 2019 Apr 1. PMID: 30933320

Abstract Author(s):

Rahel Sarah Varughese, Walter Sze-Tung Lam, Ahmad Abdurrahman Bin Hanifah Marican, S Hema Viganeshwari, Anuja Satish Bhave, Nicholas L Syn, Jigang Wang, Andrea Li-Ann Wong, Alan Prem Kumar, Peter E Lobie, Soo Chin Lee, Gautam Sethi, Boon Cher Goh, Lingzhi Wang

Article Affiliation:

Rahel Sarah Varughese

Abstract:

Deguelin is a rotenoid compound that exists in abundant quantities in the bark, roots, and leaves of the Leguminosae family of plants. An analysis of evidence from both in vitro and in vivo studies suggests that deguelin displays potent anticancer activity against multiple cancer types and exhibits chemopreventive potential in Akt-inducible transgenic mouse models. Deguelin appears to impede carcinogenesis by enhancing cell apoptosis and hindering malignant transformation and tumor cell propagation. Crucial oncogenic pathways likely targeted by deguelin include the epithelial-to-mesenchymal transition; angiogenesis-related pathways; and the phosphoinositide 3-kinase/Akt, Wnt, epidermal growth factor receptor, c-Met, and hedgehog signal transduction cascades. This review article provides a comprehensive summary of current preclinical research featuring deguelin as a leading chemotherapeutic and chemopreventive compound, and it highlights the importance of identifying companion molecular biomarkers and performing systemic pharmacokinetic studies for accelerating the process of developing deguelin as a clinical anticancer agent.

Study Type : Review

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