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Molecules 2017, 22(9), 1412;

Structure Identification and In Vitro Anticancer Activity of Lathyrol-3-phenylacetate-5,15-diacetate

Key Laboratory of Molecular and Clinical Pharmacology, School of Pharmaceutical Sciences and the Fifth Affiliated Hospital, Guangzhou Medical University, Guangzhou 511436, China
Infinitus (China) Company Ltd., Jiangmen 529156, China
Pediatric Department, Guangdong Women and Children Hospital and Health Institute, Guangzhou 511400, China
School of Chinese Medicine, Hong Kong Baptist University, Hong Kong, China
Authors to whom correspondence should be addressed.
Received: 7 August 2017 / Accepted: 22 August 2017 / Published: 25 August 2017
(This article belongs to the Collection Natural Products: Anticancer Potential and Beyond)
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Natural products from the genus Euphorbia show attention-attracting activities, such as anticancer activity. In this article, classical isolation and structure identification were used in a study on Caper Euphorbia Seed. Subsequently, MTT and wound healing assays, flow cytometry, western blotting, Hoechst 33258 staining and fluorescence microscopy examination were applied to investigate the anticancer activity of the obtained compounds. In a result, lathyrol-3-phenyl- acetate-5,15-diacetate (deoxy Euphorbia factor L1, DEFL1) was isolated from Caper Euphorbia Seed. Moreover, the NMR signals were totally assigned. DEFL1 showed potent inhibition against lung cancer A549 cells, with an IC50 value of 17.51 ± 0.85 μM. Furthermore, DEFL1 suppressed wound healing of A549 cells in a concentration-dependent manner. Mechanically, DEFL1 induced apoptosis, with involvement of an increase of reactive oxygen species (ROS), decrease of mitochondrial membrane potential (ΔΨm), release of cytochrome c, activity raise of caspase-9 and 3. Characteristic features of apoptosis were observed by fluorescence microscopy. In summary, DEFL1 inhibited growth and induced apoptosis in lung cancer A549 cells via a mitochondrial pathway. View Full-Text
Keywords: natural products; Caper Euphorbia Seed; lathyrol-3-phenylacetate-5,15-diacetate; diterpenoids; lung cancer; apoptosis natural products; Caper Euphorbia Seed; lathyrol-3-phenylacetate-5,15-diacetate; diterpenoids; lung cancer; apoptosis

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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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Zhang, J.-Y.; Huang, W.-J.; Sun, H.-M.; Liu, Y.; Zhao, X.-Q.; Tang, S.-L.; Sun, M.-N.; Wang, S.; Li, J.-J.; Zhang, L.-L.; Zhou, J.-H.; Pan, Q.-R.; Chen, H.-B. Structure Identification and In Vitro Anticancer Activity of Lathyrol-3-phenylacetate-5,15-diacetate. Molecules 2017, 22, 1412.

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