Investigation of whole plants of Euphorbia fischeriana afforded three new tigliane-diterpenoid glycosides, fischerosides A-C (1-3), together with 11 known diterpenoids. Fischerosides A-C (1-3) are the first tigliane-type diterpenoid glucosides. Their structures were determined by a combination of 1D and 2D NMR, MS, and acid hydrolysis. Inhibitory activity against HIV-1 was assessed for compounds 1-5. The new compound 3 showed an EC₅₀ value of 0.02 μM and a therapeutic index (TI) of 17.50, while prostratin (4) and 12-deoxyphorbol-13,20-diacetate (5) showed significantly greater anti-HIV-1 activity.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1021/np200058c | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
In vitro toxicity of latex, its terpenoidal fractions and isolated phorbol esters from Euphorbia umbellata (Pax) Bruyns on monocytic and melanoma cells.
Fitoterapia
July 2024
Laboratory of Technology for Biodiversity in Health, Institute of Drug Technology, Oswaldo Cruz Foundation, Rua Sizenando Nabuco 100, Manguinhos, Rio de Janeiro 21041-250, RJ, Brazil. Electronic address:
In Brazil, latex from Euphorbia umbellata (African milk tree) has been increasingly used in folk medicine to treat several types of cancer, including melanoma. The effect of lyophilized latex (LL), its hydroethanolic extract (E80), triterpene (F-TRI)- and diterpene (F-DIT)-enriched fractions, along with six isolated phorbol esters from LL and phorbol 12-myristate 13-acetate (PMA) on J774A.1, THP-1, SK-MEL-28, and B16-F10 cell line viability were evaluated by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) method.
View Article and Find Full Text PDFDiterpenoids from Euphorbia peplus possessing cytotoxic and anti-inflammatory activities.
Bioorg Chem
April 2024
Shandong Laboratory of Yantai Drug Discovery, Bohai Rim Advanced Research Institute for Drug Discovery, Yantai, Shandong 264117, People's Republic of China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, People's Republic of China. Electronic address:
Phytochemical investigation into the medium polar fraction of the ethanol extract of Euphorbia peplus led to the identification of 32 diterpenoids with five structural types. Compounds 1-5 and 7-11 are reported for the first time, while the configuration of 6,7-epoxy group of 6 was revised to be β-oriented. Compounds 1-5 feature a rare structural variation of the double bond at Δ migrating to Δ in the tigliane-type diterpenoid family.
View Article and Find Full Text PDFDiterpenoids with Schistosomula-Killing and Anti-Fibrosis Activities In Vitro from the Leaves of .
Molecules
January 2024
College of Pharmacy, Hunan University of Chinese Medicine, Changsha 410208, China.
The leaves of have been comprehensively researched for their structurally novel bioactive natural compounds, especially those with anti-schistosomiasis liver fibrosis activity, because ethyl acetate extract, which can be extracted from the leaves of , has good anti-schistosomiasis liver fibrosis effects. One new tigliane-type diterpene, 20-acetyl-13--(2-metyl)butyryl-phorbol (), and nine known (-) analogues were isolated from the leaves of . Their structures were elucidated on the basis of spectroscopic analysis and ECD analysis.
View Article and Find Full Text PDF[Research progress in tigliane-type macrocyclic diterpenoids].
Zhongguo Zhong Yao Za Zhi
September 2023
State Key Laboratory for Quality Ensurance and Sustainable Use of Dao-di Herbs, National Resource Center for Chinese Materia Medica, China Academy of Chinese Medical Sciences Beijing 100700, China School of Pharmacy, Nanjing University of Chinese Medicine Nanjing 210023, China.
Tigliane type macrocyclic diterpenoids with special structures and diverse bioactivities are mainly extracted from plants of Euphorbiaceae and Thymelaeaceae. According to the different functional groups, they can be classified into types of phorbol esters, C-4 deoxyphorbol esters, C-12 deoxyphorbol esters, C-16 or C-17 substituted phorbol esters and others. Most of them present promising antiviral activities and cytotoxic activities and are expected to be developed as candidates for anti-AIDS, anti-tuberculosis, and anti-tumor clinical trials, demonstrating great potential for the application in healthcare.
View Article and Find Full Text PDFTigliane-and daphnane-type diterpenoids from the buds of with their cytotoxic activities.
Nat Prod Res
November 2022
Qiqihar Medical University, Qiqihar, Heilongjiang, PR China.
Two new tigliane- and daphnane-type diterpenoids, given the trivial names daphnegens A-B - were isolated from the buds of . Their structures were assigned on the basis of extensive spectroscopic. The absolute configurations of both compounds were determined by comparison of their calculated and experimental CD curves.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!