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Review

Euphorbia Diterpenes: An Update of Isolation, Structure, Pharmacological Activities and Structure–Activity Relationship

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Department of Chemistry, Faculty of Science, Tshwane University of Technology, Pretoria 0001, South Africa
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Department of Chemistry, Rhodes University, Makhanda 6140, South Africa
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Jodrell Laboratory, Department of Unlocking Properties, Royal Botanic Gardens Kew, Richmond TW9 3DS, UK
*
Authors to whom correspondence should be addressed.
Academic Editor: Jorge A. R. Salvador
Molecules 2021, 26(16), 5055; https://doi.org/10.3390/molecules26165055
Received: 19 July 2021 / Revised: 12 August 2021 / Accepted: 16 August 2021 / Published: 20 August 2021
(This article belongs to the Section Natural Products Chemistry)
Euphorbia species have a rich history of ethnomedicinal use and ethnopharmacological applications in drug discovery. This is due to the presence of a wide range of diterpenes exhibiting great structural diversity and pharmacological activities. As a result, Euphorbia diterpenes have remained the focus of drug discovery investigations from natural products. The current review documents over 350 diterpenes, isolated from Euphorbia species, their structures, classification, biosynthetic pathways, and their structure–activity relationships for the period covering 2013–2020. Among the isolated diterpenes, over 20 skeletal structures were identified. Lathyrane, jatrophane, ingenane, ingenol, and ingol were identified as the major diterpenes in most Euphorbia species. Most of the isolated diterpenes were evaluated for their cytotoxicity activities, multidrug resistance abilities, and inhibitory activities in vitro, and reported good activities with significant half-inhibitory concentration (IC50) values ranging from 10–50 µM. The lathyranes, isopimaranes, and jatrophanes diterpenes were further found to show potent inhibition of P-glycoprotein, which is known to confer drug resistance abilities in cells leading to decreased cytotoxic effects. Structure–activity relationship (SAR) studies revealed the significance of a free hydroxyl group at position C-3 in enhancing the anticancer and anti-inflammatory activities and the negative effect it has in position C-2. Esterification of this functionality, in selected diterpenes, was found to enhance these activities. Thus, Euphorbia diterpenes offer a valuable source of lead compounds that could be investigated further as potential candidates for drug discovery. View Full-Text
Keywords: Euphorbia; diterpenes; pharmacological activity; structure–activity relationship Euphorbia; diterpenes; pharmacological activity; structure–activity relationship
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MDPI and ACS Style

Kemboi, D.; Siwe-Noundou, X.; Krause, R.W.M.; Langat, M.K.; Tembu, V.J. Euphorbia Diterpenes: An Update of Isolation, Structure, Pharmacological Activities and Structure–Activity Relationship. Molecules 2021, 26, 5055. https://doi.org/10.3390/molecules26165055

AMA Style

Kemboi D, Siwe-Noundou X, Krause RWM, Langat MK, Tembu VJ. Euphorbia Diterpenes: An Update of Isolation, Structure, Pharmacological Activities and Structure–Activity Relationship. Molecules. 2021; 26(16):5055. https://doi.org/10.3390/molecules26165055

Chicago/Turabian Style

Kemboi, Douglas, Xavier Siwe-Noundou, Rui W. M. Krause, Moses K. Langat, and Vuyelwa Jacqueline Tembu. 2021. "Euphorbia Diterpenes: An Update of Isolation, Structure, Pharmacological Activities and Structure–Activity Relationship" Molecules 26, no. 16: 5055. https://doi.org/10.3390/molecules26165055

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