scholarly journals Evaluation of Alangium lamarckii Bark for Antiplasmodial and Cytotoxic Constituents and Isolation of a Novel Tubulosine Analogue

2018 ◽  
Vol 13 (10) ◽  
pp. 1934578X1801301
Author(s):  
Venkata Siva Satyanarayana Kantamreddi ◽  
Gemma Marston ◽  
Steven D. Shnyder ◽  
Colin W. Wright

Alangium lamarkii is traditionally used in India for the treatment of malaria. Partial activity guided-fractionation of the basic chloroform fraction of the methanolic extract of the bark led to the isolation of a novel tubulosine analogue, 10-demethyl-9'- N-methyltubulosine (1), for which the trivial name tubulosatine is suggested. In addition, the known A. lamarkii constituents, tubulosine (2), cephaeline and emetine were isolated as potent antiplasmodial and cytotoxic constituents, but 1 was up to 1000-fold less potent than the former alkaloids against both malaria parasites and human cancer cell lines. The compounds were active against both chloroquine-sensitive and chloroquine-resistant malaria parasites, but no selective toxicity was observed towards malaria parasites compared with cancer cells with any of the alkaloids. Further work to explore the basis for the relatively weak biological activities of 1 would be worthwhile. Betulinic acid, stigmasterol and its 3- O-glucoside were isolated from the neutral chloroform fraction of the methanolic extract.

2021 ◽  
Author(s):  
Elizaveta A. Kvyatkovskaya ◽  
Kseniya K. Borisova ◽  
Polina P. Epifanova ◽  
Aleksey A. Senin ◽  
Victor N. Khrustalev ◽  
...  

A 3,5a-epoxyfuro[2,3,4-de]isoquinoline scaffold, the product of ROCM of 1,4:5,8-diepoxynaphthalenes, is a promising antiproliferative agent toward breast and prostate human cancer cell lines.


2020 ◽  
Vol 19 (6) ◽  
pp. 790-799
Author(s):  
Miryam Chiara Malacarne ◽  
Stefano Banfi ◽  
Enrico Caruso

Two new aza-BODIPY photosensitizers featuring an iodine atom on each pyrrolic unit of their structure, were synthesized in fairly good yields and tested in vitro on two human cancer cell lines to assess their photodynamic efficacy.


2014 ◽  
Vol 69 (1-2) ◽  
pp. 46-52 ◽  
Author(s):  
Leticia F. Porte ◽  
Silvana M. O. Santin ◽  
Lucas U. R. Chiavelli ◽  
Cleuza C. Silva ◽  
Terezinha J. Faria ◽  
...  

The Orchidaceae family is appreciated worldwide for the beauty of its flowers, and hundreds of species of this family occur in Brazil. Yet little is known about the potential of orchids for therapeutic application. We have investigated bioactive compounds produced by the South Brazilian orchid Miltonia flavescens Lindl. Bioguided studies with the fungus Cladosporium herbarum allowed the identification of hydrocinnamic acid as the active antifungal compound. In addition, the chloroform fraction exhibited an interesting activity against human cancer cells, and 5,7-dihydroxy-6,4'- dimethoxyflavone isolated from this fraction was found to be active against seven human cancer cell lines, including NCI/ADR-RES ovary sarcoma, with an IC50 value of 2.6 mg/mL. This is the first report on the cytostatic activity of this flavone against human ovary sarcoma.


2010 ◽  
Vol 30 (8) ◽  
pp. 1083-1087 ◽  
Author(s):  
Hyung-In Moon ◽  
Okpyo Zee

In search for plant-derived cytotoxicity compound against human cancer cells (A549, SK-OV-3, SK-MEL-2, XF498, HCT15), it was found that the chloroform extracts obtained from the whole plant of Carpesium rosulatum MlQ. (Compositae) exhibited significant cytotoxic activity. Four sesquiterpene lactone, CRC1 (2α, 5-epoxy-5,10-dihydroxy-6-angeloyl-oxy-9β-isobutyloxy-germacran-8α,12-olide), CRC2 (2α,5-epoxy-5,10-dihydroxy-6α,9β-diangeloyloxy-germacran-8α,12-olide), CRC3 (2α,5-epoxy-5,10-dihydroxy-6α-angeloyloxy-9β-(3-methyl-butanoyloxy)-gemacran-8α,12-olide), CRC4 (2β,5-epoxy-5,10-dihydroxy-6α,9β-diangeloyloxy-germacran-8α,12-olide) were isolated from the whole parts of C. rosulatum. 2α,5-epoxy-5,10-dihydroxy-6α,9β-diangeloyloxy-germacran-8α,12-olide (CRC2) showed the most potent cytotoxicity with IC50 value of 6.01 μM against SK-MEL-2.


2012 ◽  
Vol 7 (7) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Hyung-In Moon

In the search for antiproliferative compounds against human cancer cells (A549, SK-OV-3, SK-MEL-2, XF498, HCT15), it was found that the chloroform extracts obtained from the whole plant of Carpesium rosulatum Miq. (Compositae) exhibited significant cytotoxic activity. Two sesquiterpene lactones, CT-1 (2α,5-epoxy-5,10-dihydroxy-6-angeloyloxy-9β-isobutyloxy-germacran-8α,12-olide), and CT-2 (2β,5-epoxy-5,10-dihydroxy-6α,9β-diangeloyloxy-germacran-8α,12-olide) were isolated from the whole plant. CT-2 showed the most potent cytotoxicity with an IC50 value of 7.88 μM against SK-MEL-2.


2021 ◽  
Vol 16 (3) ◽  
pp. 1934578X2110030
Author(s):  
Yi Liu ◽  
Wei Wang ◽  
Jian Miao

A new compound, 1,3,7,9-tetrahydroxy-6 H-dibenzo[ b, d]pyran-6-one (1), together with 6 known compounds (2-7), was isolated from the extract of whole plants of Centella asiatica. The chemical structure was elucidated on the basis of spectroscopic and mass spectrometric analyses. All the isolates were evaluated for their cytotoxicities against 4 human cancer cell lines (MCF-7, HepG2, Hela, and A549). Among them, compound 1 was found to exhibit significant cytotoxicity on MCF-7 and HepG2 cancer cells with half-maximal inhibitory concentration values of 4.1 and 7.2 µM, respectively.


2016 ◽  
Vol 14 (1) ◽  
pp. 102-111 ◽  
Author(s):  
Vu Tuan Kien ◽  
Le Huy Binh ◽  
Phan Hai Phong ◽  
Doan Thi Hien ◽  
Nguyen Thi Thuy My ◽  
...  

In continuation of our study on anticancer compounds, a series of novel artemisinin dimers have been synthesized and evaluated for their cytotoxic effects against three human cancer cell lines, including HepG2 (liver cancer), MCF-7(breast cancer) and HL-60 (leukemia cancer). The assay results showed that most of the compounds displayed inhibitory effects against all three human cancer cell lines tested, and seemed to be more cytotoxic toward the blood cancer cells (HL-60) than liver (HepG2), and breast (MCF-7) cancer cells. Among the synthesized artemisinin dimers, the compound 10d with a double bond bridge exhibited the most potent cytotoxicity with IC50 values of 5.08, 4.82 and 1.32 µg/mL against the HepG2, MCF-7, and HL-60 cell lines, respectively.


Metallomics ◽  
2017 ◽  
Vol 9 (8) ◽  
pp. 1132-1141 ◽  
Author(s):  
Ana Podolski-Renić ◽  
Szilvia Bősze ◽  
Jelena Dinić ◽  
László Kocsis ◽  
Ferenc Hudecz ◽  
...  

Epimeric ferrocene–quinidine hybrids with triazolyl-chalcone linkers act as pro-oxidative agents and autophagy modulators in paclitaxel resistant cancer cells.


2012 ◽  
Vol 90 (11) ◽  
pp. 932-943 ◽  
Author(s):  
Sergey Vshyvenko ◽  
Jon Scattolon ◽  
Tomas Hudlicky ◽  
Anntherese E. Romero ◽  
Alexander Kornienko ◽  
...  

Several C-1 homologues of pancratistatin and 7-deoxypancratistatin were synthesized by a phenanthrene–phenathridone oxidative recyclization strategy. The key steps involved the enzymatic dihydroxylation of bromobenzene, addition of an aryl alane to an epoxyaziridine, an intramolecular aziridine opening on silica gel in solid phase, and the above-mentioned recylization strategy. Experimental and spectral data are reported for all new compounds. All synthesized C-1 homologues of pancratistatin and 7-deoxypancratistatin were evaluated for antiproliferative activity in a panel of human cancer cell lines. As expected, the 7-hydroxy compounds were found to be more potent and the activity of the C-1 benzoxymethyl analogue exceeded that of narciclasine, which was used as a positive control.


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