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Biomedicines 2018, 6(2), 39; https://doi.org/10.3390/biomedicines6020039

Plant-Derived Anticancer Agents: Lessons from the Pharmacology of Geniposide and Its Aglycone, Genipin

1
Pharmacognosy Research Laboratories, University of Greenwich, Central Avenue, Chatham-Maritime, Kent ME4 4TB, UK
2
Herbal Analysis Services, Chatham-Maritime, Kent ME4 4TB, UK
3
Department of Pharmacy-Drug Sciences, University of Studies of Bari Aldo Moro, Via E. Orabona n. 4, 70126 Bari, Italy
*
Author to whom correspondence should be addressed.
Received: 6 March 2018 / Revised: 21 March 2018 / Accepted: 22 March 2018 / Published: 26 March 2018
(This article belongs to the Special Issue Plant Derived Biomedicines)
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Abstract

For centuries, plants have been exploited by mankind as sources of numerous cancer chemotherapeutic agents. Good examples of anticancer compounds of clinical significance today include the taxanes (e.g., taxol), vincristine, vinblastine, and the podophyllotoxin analogues that all trace their origin to higher plants. While all these drugs, along with the various other available therapeutic options, brought some relief in cancer management, a real breakthrough or cure has not yet been achieved. This critical review is a reflection on the lessons learnt from decades of research on the iridoid glycoside geniposide and its aglycone, genipin, which are currently used as gold standard reference compounds in cancer studies. Their effects on tumour development (carcinogenesis), cancer cell survival, and death, with particular emphasis on their mechanisms of actions, are discussed. Particular attention is also given to mechanisms related to the dual pro-oxidant and antioxidant effects of these compounds, the mitochondrial mechanism of cancer cell killing through reactive oxygen species (ROS), including that generated through the uncoupling protein-2 (UCP-2), the inflammatory mechanism, and cell cycle regulation. The implications of various studies for the evaluation of glycosidic and aglycone forms of natural products in vitro and in vivo through pharmacokinetic scrutiny are also addressed. View Full-Text
Keywords: cancer; carcinogenesis; metastasis; genipin; geniposide; reactive oxygen species; apoptosis; uncoupling protein 2 cancer; carcinogenesis; metastasis; genipin; geniposide; reactive oxygen species; apoptosis; uncoupling protein 2
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Habtemariam, S.; Lentini, G. Plant-Derived Anticancer Agents: Lessons from the Pharmacology of Geniposide and Its Aglycone, Genipin. Biomedicines 2018, 6, 39.

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