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Open AccessReview

Mechanistic Pathways and Molecular Targets of Plant-Derived Anticancer ent-Kaurane Diterpenes

School of Chinese Medicine, Hong Kong Baptist University, Kowloon Tong, Hong Kong, China
Department of Pharmacy, Noakhali Science and Technology University, Sonapur, Noakhali 3814, Bangladesh
Author to whom correspondence should be addressed.
Biomolecules 2020, 10(1), 144;
Received: 18 December 2019 / Revised: 12 January 2020 / Accepted: 14 January 2020 / Published: 16 January 2020
(This article belongs to the Special Issue Phytochemical Omics in Medicinal Plants)
Since the first discovery in 1961, more than 1300 ent-kaurane diterpenoids have been isolated and identified from different plant sources, mainly the genus Isodon. Chemically, they consist of a perhydrophenanthrene subunit and a cyclopentane ring. A large number of reports describe the anticancer potential and mechanism of action of ent-kaurane compounds in a series of cancer cell lines. Oridonin is one of the prime anticancer ent-kaurane diterpenoids that is currently in a phase-I clinical trial in China. In this review, we have extensively summarized the anticancer activities of ent-kaurane diterpenoids according to their plant sources, mechanistic pathways, and biological targets. Literature analysis found that anticancer effect of ent-kauranes are mainly mediated through regulation of apoptosis, cell cycle arrest, autophagy, and metastasis. Induction of apoptosis is associated with modulation of BCL-2, BAX, PARP, cytochrome c, and cleaved caspase-3, -8, and -9, while cell cycle arrest is controlled by cyclin D1, c-Myc, p21, p53, and CDK-2 and -4. The most common metastatic target proteins of ent-kauranes are MMP-2, MMP-9, VEGF, and VEGFR whereas LC-II and mTOR are key regulators to induce autophagy. View Full-Text
Keywords: isodon genus; ent-kaurane diterpenoids; cancer; natural compounds; pathways isodon genus; ent-kaurane diterpenoids; cancer; natural compounds; pathways
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MDPI and ACS Style

Sarwar, M.S.; Xia, Y.-X.; Liang, Z.-M.; Tsang, S.W.; Zhang, H.-J. Mechanistic Pathways and Molecular Targets of Plant-Derived Anticancer ent-Kaurane Diterpenes. Biomolecules 2020, 10, 144.

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