scholarly journals Triterpenoidal and Phenolic Compounds Isolated from the Aerial Parts of Helicteres hirsuta and their Cytotoxicity on Several Cancer Cell Lines

2019 ◽  
Vol 14 (1) ◽  
pp. 1934578X1901400
Author(s):  
Triet Thanh Nguyen ◽  
Nadine Kretschmer ◽  
Eva-Maria Pferschy-Wenzig ◽  
Olaf Kunert ◽  
Rudolf Bauer

Helicteres L. is one of the genera of the Sterculiaceae family with several remarkable activities. Previous studies revealed that terpenoids, flavonoids, and lignans are the dominant constituents of Helicteres species. However, information about this genus is scarce and unsystematic. Most of the phytochemical and pharmacological investigations have been mainly reported on Helicteres angustifolia and Helicteres isora, which are commonly used in China and Indonesia, respectively. In the present study, two terpenoids: 3β- O-acetylbetulinic acid (1) and simiarenol (2) together with three phenolic compounds: 4,4'-sulfinylbis(2-( tert-butyl)-5-methylphenol) (3), 7- O-methylisoscutellarein (4), 7,4'-di- O-methylisoscutellarein (5), and a mixture of stigmasterol and β-sitosterol were isolated and structurally elucidated from the aerial parts of Helicteres hirsuta Lour. Compounds 1-5 were tested for cytotoxicity on four human cancer cell lines: leukemia CCRF-CEM, breast MDA-MB-231, colon HCT116 and glioblastoma U251 cancer cells. Among them, compounds 1 and 3 showed moderate activity on CCRF-CEM and HCT116 cancer cells with IC50 values ranging from 14.6 to 31.5 μM (P < 0.05). This is the first time these compounds have been reported from this plant. To the best of our knowledge, compound 3 is novel in nature although it has been chemically synthesized before, and compounds 1, 2, and 4 are new to this plant family (Sterculiaceae).

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.


2019 ◽  
Vol 9 (4-s) ◽  
pp. 1195-1202
Author(s):  
Nirmala Devi ◽  
Ajay Kumar Gupta ◽  
Sunil Kumar Prajapati

Aims: Apocynaceae family is the 5th largest medicinal plant family rich in potent secondary metabolites such as Alkaloids, Cardiac glycosides,Terpenoids, irridoid/secoirridoids, flavonoids and Phenolic contents. The present study was aimed to evaluate and compare in-vitroantiproliferative activity of three plants of this family.Methods: Aerial parts of Carissa carandas Linn. (C), Nerium indicum Mill. (N) and Wrightia tinctoria RBr. (W), were collected and dried. Thepowdered drugs were extracted in Ethanol (1), 60% Ethanol (2) and Water (3). Estimation of Phytoconstituents performed using standardmethods. In-vitro cytotoxic activity performed using Sulphorhodamine B (SRB) assay in HepG2, HT29 and SKOV3 human cancer cell lines takingAdriamycin (ADR) as standard. For extracts, GI50 value ≤ 20μg/ml was considered to demonstrate activity.Results: For HepG2 cell line graphs and photomicrographs showed GI50 value as ADR=39.79, C1=2.5, N2=66.3, N3<10 and C2=C3= N1=W1-3>80. Also TGI for C1>80. The extracts, C1, C2, N1, N2, and N3 were found to possess activity against HepG2.These extracts were screened onHT 29 and SKOV3cell lines. The GI50 value observed was<10 for C1, N2, N3 and ADR in HT 29 and <10 for N3 and ADR in SK OV3 cell lines.Thus it was found that aqueous extract of Nerium indicum (N3) and Ethanolic extract of Carissa carandas (C1) were most cytotoxic extractsagainst all three cell lines.Conclusions: our study establishes that Apocynaceae family plants could be an important anticancer lead and could serve as Botanical drug forneoplasia.Keywords: Apocynaceae, SRB Assay, Phytoconstituents, Anticancer drug screening models, Hep G2, HT 29, SK-OV3, HCC.


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.


2020 ◽  
Vol 155 ◽  
pp. 112746
Author(s):  
VK Muhammed Ashraf ◽  
V.K. Kalaichelvan ◽  
V.V. Venkatachalam ◽  
R. Ragunathan

2006 ◽  
Vol 95 (2) ◽  
pp. 346-352 ◽  
Author(s):  
Anne De La Torre ◽  
Eric Debiton ◽  
Pierre Juanéda ◽  
Denys Durand ◽  
Jean-Michel Chardigny ◽  
...  

Although many data are available concerning anticarcinogenic effects of industrial conjugated linoleic acid (CLA), few studies have reported the antitumour properties of CLA mixtures originating from ruminant products. The aim of the present study was to investigate thein vitroantiproliferative effects of beef CLA mixtures on breast, lung, colon, melanoma and ovarian human cancer cell lines. For this purpose, four fatty acid (FA) extracts prepared from beef lipid and varying in their CLA composition, their corresponding purified CLA-enriched fractions, and mixtures of pure synthetic CLA, the composition of which reproduced that of the four selected beef samples, were tested on cancer cell lines. Cancer cells were exposed for 48h to medium containing 100μm-FA and their proliferation was determined by quantifying cellular DNA content (Hoechst 33342 dye). Compared with cells incubated without FA, the number of cancer cells was reduced from 25 to 67% (P<0·0001) following FA treatment. Antiproliferative effects of CLA mixtures varied in magnitude according to the source of FA, the CLA composition and the cell lines. CLA mixtures naturally present in beef inhibited the proliferation of human cancer cell lines, a high content incis-transisomers allowing the most important antiproliferative effect. Beef total FA exhibited a greater growth-inhibitory activity than their corresponding CLA-enriched fractions. These results suggested that either beef FA other than beef CLA could possess antiproliferative properties and/or the existence of complementary effects of non-conjugated FA and CLA, which could favour the antiproliferative properties of beef total FA.


2016 ◽  
Vol 14 (21) ◽  
pp. 4829-4841 ◽  
Author(s):  
Sajita Shah ◽  
Chaemin Lee ◽  
Hyukjae Choi ◽  
Jaya Gautam ◽  
Hyeonjin Jang ◽  
...  

Synthesis of a series of hybrid compounds of pyridinol and sunitinib and their cytotoxicity against human cancer cell lines and improved safety windows are described.


1993 ◽  
Vol 104 (2) ◽  
pp. 289-296 ◽  
Author(s):  
N. Hiraiwa ◽  
H. Kida ◽  
T. Sakakura ◽  
M. Kusakabe

Human cancer cell lines A431 and MCF7, which do not produce tenascin (TN) in vitro, were found to produce TN when injected into nude mice or co-cultured with the embryonic mesenchyme. The TN expression in the developing A431 solid tumor was demonstrated by immunohistochemistry and by in situ hybridization. Human TN was detected in culture media by western blot analysis using human specific monoclonal antibody (RCB-1). During tumorigenesis, in the early stage, mouse TN was actively induced and deposited in the peri- and intertumor spaces surrounding the developing tumor. Two days later, TN derived from human epithelial cancer cells was induced and mainly deposited in the intertumor basement membrane. After this stage, tumor cells were actively producing TN. On the other hand, TN induction in non TN-producing cells, such as A431 and MCF7 cell lines, was also observed in vitro. Although cell lines such as NIH-3T3, phi 2, STO, 2H6, 3E5 and CMT315, had no effect on the TN induction, primary cultured embryonic mesenchyme effectively stimulated the TN expression in the cancer cell lines. This mesenchymal effect decreased with age and was entirely lost postnatally. Furthermore, conditioned media from these embryonic mesenchymes could reproduce the same effects on TN induction as observed in the co-culture study. In conclusion, these findings suggest that TN induction in epithelial cancer cells may depend on interactions with the surrounding environment, that these interactions may be mediated by a soluble factor(s) derived from the surrounding mesenchyme and that the TN induction observed in the tumorigenesis may reflect histogenesis during the embryonic period.


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