scholarly journals A New Pyrrolidone Alkaloid and Other Constituents from Rourea oligophlebia Stems

2021 ◽  
Vol 2021 ◽  
pp. 1-5
Author(s):  
Thuc Ngoc Dinh ◽  
Mai Vu Thi Ha ◽  
Luong Ngo Xuan ◽  
Huan Trinh Thi ◽  
Huong Nguyen Thi ◽  
...  

Phytochemical study of Rourea oligophlebia stems led to the isolation of a new 2-pyrrolidone alkaloid (R,S)-N-(5-hydroxyl-pyrrolidin-2-one-1-yl)acetamide (1), together with 14 known compounds including friedelin (2), friedanol (3), taraxerol (4), vanillin (5), coniferyl aldehyde (6), apigenin (7), 7α-hydroxy-3β-sitosterol (8), coniferyl alcohol (9), scopoletin (10), emodin (11), protocatechuic acid (12), catechin (13), procyanidin A1 (14), and (E)-2,3,5,4’-tetrahydroxystilbene-2-β-D-glucoside (15). Several isolated compounds were evaluated for cytotoxicity and antimicrobial activity. Compound 11 exhibited good antimicrobial activity on Gram (+) strains and moderate cytotoxicity against KB, Hep-G2, and LU cancer cell lines. Compounds 6 and 8–10 showed selective activity on HepG-2 and MCF-7 over KB and LU cancer cell lines, while compound 7 exhibited similar effects on KB, HepG-2, and MCF-7 cell lines with IC50 values of 36.46 ± 0.81, 32.00 ± 0.58, and 32.03 ± 0.61 µg/mL, respectively.

2018 ◽  
Vol 40 (2) ◽  
pp. 145-152
Author(s):  
Vu Thi Nguyet ◽  
Nguyen Tien Dat ◽  
Le Mai Huong ◽  
Tran Thi Hong Ha ◽  
Nguyen Hong Chuyen ◽  
...  

This paper reports the cytotoxic effect on several cancer cell lines of the stem extracts and of some isolated compounds from Ehretia asperula. All the extracts exhibited cytotoxic effects on at least one cancer cell line. The n-hexane extract showed potent cytotoxic activity on Hep-G2, MCF-7 and HeLa cell lines with IC50 values of 28.3 g/ml, 14.42 g/ml and 18.59 g/ml, respectively, while the methanolic, ethyl acetate and water extracts exhibited toxicity towards MCF-7 cells with IC50 values of 16.45 g/ml, 13.4 g/ml and 39.78 g/ml, respectively. 06 compounds have been isolated from the ethyl acetate fraction of Ehretia asperula stem. Methyl caffeate has a strong cytotoxicity against Hep-G2, HeLa and MCF-7 cancer cell lines with IC50 values of 2.83 g/ml, 3.38 g/ml and 4.4 g/ml, respectively. Oresbiusin B was active against Hep-G2 with IC50 value of 9.89 g/ml. The other compounds including coniferaldehyde, 9′-methoxydehydrodiconiferyl alcohol and vanillic acid did not have any cytotoxic effect on the tested cancer cell lines. So, the obtained results have suggested possibility of using the potential Ehretia asperula extracts as health food for preventing and curing cancer diseases. Keywords: Ehretia asperula, methyl caffeate, oresbiusin B, Cancer cell lines. Citation: Vu Thi Nguyet, Nguyen Tien Đat, Le Mai Huong, Tran Thi Hong Ha, Nguyen Hong Chuyen, Nguyen Thi Hang4, Đang Đinh Kim, 2018. Evaluating cytotoxic effect of the extracted compounds from ehretia asperula zoll. & mor stem on several cancer cell lines.Tap chi Sinh hoc, 40(2): 145153. https://doi.org/10.15625/0866-7160/v40n2.12955. *Corresponding author: [email protected]


Molecules ◽  
2021 ◽  
Vol 26 (10) ◽  
pp. 3041
Author(s):  
Xiaohan Hu ◽  
Sheng Tang ◽  
Feiyi Yang ◽  
Pengwu Zheng ◽  
Shan Xu ◽  
...  

Two series of olmutinib derivatives containing an acrylamide moiety were designed and synthesized, and their IC50 values against cancer cell lines (A549, H1975, NCI-H460, LO2, and MCF-7) were evaluated. Most of the compounds exhibited moderate cytotoxic activity against the five cancer cell lines. The most promising compound, H10, showed not only excellent activity against EGFR kinase but also positive biological activity against PI3K kinase. The structure–activity relationship (SAR) suggested that the introduction of dimethylamine scaffolds with smaller spatial structures was more favorable for antitumor activity. Additionally, the substitution of different acrylamide side chains had different effects on the activity of compounds. Generally, compounds H7 and H10 were confirmed as promising antitumor agents.


2020 ◽  
Vol 32 (5) ◽  
pp. 1197-1202
Author(s):  
Consolacion Y. Ragasa ◽  
Glenn G. Oyong ◽  
Maria Carmen S. Tan ◽  
Mariquit M. De Los Reyes ◽  
Maria Ellenita G. De Castro

Ergosterol peroxide (1) and ergosterol (2) were commonly isolated as the major compounds of Philippine mushrooms. Sterols 1 and 2 from the dichloromethane extract of Geastrum triplex and Termitomyces clypeatus, respectively, were evaluated for their cytotoxic activities against four human cancer cell lines, viz., breast cancer (MCF-7), colon cancer (HT-29), leukemia (THP-1), and small lung cell carcinoma (H69PR), and a human normal cell line, human dermal fibroblast-neonatal (HDFn), using the PrestoBlue® cell viability assay. Compounds 1 and 2 exhibited the strongest activities against HT-29 with IC50 values of 1.79 and 2.98 μg/mL, respectively, while Zeocin gave an IC50 of 4.89 μg/mL. These compounds also exhibited strong antiproliferative effects against MCF-7 with IC50 values of 4.13 for 1 and 4.20 μg/mL for compound 2, comparable to Zeocin with IC50 = 3.68 μg/mL. Only moderate cytotoxicity resulted when compounds 1 and 2 were tested against H69PR with IC50 values of 7.78 and 6.83 μg/mL, respectively, while Zeocin exhibited an IC50 of 9.81 μg/mL. Furthermore, compounds 1 and 2 showed no effects against THP-1 (IC50 > 100 μg/mL), while Zeocin showed an IC50 of 4.73 μg/mL. Although compounds 1 and 2 have been reported to exhibit different bioactivities in previous studies, the cancer cell lines tested and/or the polarities of the solvents for extraction varied. Therefore, comparisons of the cytotoxic activities of compounds 1 and 2 with earlier studies could not be made extensively.


2014 ◽  
Vol 4 (3) ◽  
pp. 179-189 ◽  
Author(s):  
Roba Talaat ◽  
Waheba El-Sayed ◽  
Hussein Agwa ◽  
Amira Gamal-Eldeen ◽  
Shaden Moawia ◽  
...  

2018 ◽  
Vol 23 ◽  
pp. 2515690X1879072 ◽  
Author(s):  
Sylvester Languon ◽  
Isaac Tuffour ◽  
Emmanuel Ekow Quayson ◽  
Regina Appiah-Opong ◽  
Osbourne Quaye

There are numerous herbal products on the Ghanaian market that are purported to cure various ailments, including cancer. However, scientific investigations on efficacy and toxicity of most of these products are not done. The aim of the study was to assess the anticancer potentials of herbal products on the Ghanaian market. Antiproliferative effects of Kantinka BA (K-BA), Kantinka Herbaltics (K-HER), Centre of Awareness (COA), a stomach (STO) and multicancer (MUT) product were evaluated in vitro using liver (Hep G2), breast (MCF-7), prostate (PC-3 and LNCaP), and blood (Jurkat) cancer cell lines. Cytotoxicity of the medicinal products was assessed using tetrazolium-based colorimetric assay, and total phenolic content and antioxidant activity of the products were determined using Folin-Ciocalteau and 1,1-diphenyl-2-picrylhydrazyl (DPPH) assays, respectively. Phytochemical screening resulted in the detection of terpenoids and flavonoids in most of the products, and alkaloids were detected in only MUT. Tannins were absent from all the products. The highest and lowest concentrations of phenolics were recorded for MUT and K-BA, respectively. The highest and lowest antioxidant activities were measured for MUT and K-HER, respectively. Only 2 products (STO and MUT) were cytotoxic to Hep G2 cells; with MUT being the only product that was cytotoxic to MCF-7 cells. All but K-BA were cytotoxic to PC-3 cells, while all products except K-HER were cytotoxic to LNCaP and Jurkat cells. The study thus confirms that the herbal products have selective cytotoxic activities against the tested cancer cell lines. However, comprehensive toxicity studies must be conducted to establish their safety.


2020 ◽  
Vol 19 (3) ◽  
pp. 577-581
Author(s):  
Najla Ali Alburae ◽  
Afrah Eltayeb Mohammed

Purpose: To investigate the antiproliferative effect of the Red Sea cone snail, Conus geographus, against 4 MCF-7 (breast), MDA-MB-231 (epithelial human breast), HepG2 (hepatocellular) and SKOV-3 (ovarian) cancer cell lines. Methods: Extraction of Red Sea cone snail sample with a mixture of CH2Cl2 and CH3OH (1:1, v/v) yielded 0.55 g of a green viscous material. The cytotoxic effects of the organic extract against the cancer cell lines were determined using cell proliferation (MTT) assay, and the half-maximal concentration (IC50) values measured. The effect of the crude extract on the cell cycle of the HepG-2 was determined by flow cytometry. Results: The extract produced significant inhibitory effects against SKOV-3, MDA-MB-231, MCF-7 and HepG2, with IC50 values of 22.7 ± 2.2, 68.7 ± 6.2, 47 ± 4.2 and 19 ± 2.1 μg/mL, respectively. Cell cycle analysis revealed that the extract enhanced accumulation of HepG2 cells in the Go/G1 phase, at a level of 23.4 and 24.1 % at IC50 (19 μg/mL) and ½ IC50 (9.5 μg/mL), respectively, when compared to the untreated cells. Conclusion: These results indicate that C. geographus extract exhibits potent cytotoxic effect against HepG2 cells via a mechanism involving G0/G1 cell cycle arrest. Thus, C. geographus is a potential source of a new anti-cancer agent. Keywords: Conus geographus, Marine invertebrate, HepG2, Antiproliferation


Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3658
Author(s):  
Solomon Tesfaye ◽  
Hannah Braun ◽  
Kaleab Asres ◽  
Ephrem Engidawork ◽  
Anteneh Belete ◽  
...  

Medicinal plants have been traditionally used to treat cancer in Ethiopia. However, very few studies have reported the in vitro anticancer activities of medicinal plants that are collected from different agro-ecological zones of Ethiopia. Hence, the main aim of this study was to screen the cytotoxic activities of 80% methanol extracts of 22 plants against human peripheral blood mononuclear cells (PBMCs), as well as human breast (MCF-7), lung (A427), bladder (RT-4), and cervical (SiSo) cancer cell lines. Active extracts were further screened against human large cell lung carcinoma (LCLC-103H), pancreatic cancer (DAN-G), ovarian cancer (A2780), and squamous cell carcinoma of the esophagus (KYSE-70) by using the crystal violet cell proliferation assay, while the vitality of the acute myeloid leukemia (HL-60) and histiocytic lymphoma (U-937) cell lines was monitored in the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) microtiter assay. Euphorbia schimperiana, Acokanthera schimperi, Kniphofia foliosa, and Kalanchoe petitiana exhibited potent antiproliferative activity against A427, RT-4, MCF-7, and SiSo cell lines, with IC50 values ranging from 1.85 ± 0.44 to 17.8 ± 2.31µg/mL. Furthermore, these four extracts also showed potent antiproliferative activities against LCLC-103H, DAN-G, A2780, KYSE-70, HL-60, and U-937 cell lines, with IC50 values ranging from 0.086 to 27.06 ± 10.8 µg/mL. Hence, further studies focusing on bio-assay-guided isolation and structural elucidation of active cytotoxic compounds from these plants are warranted.


2020 ◽  
Vol 58 (1) ◽  
pp. 12
Author(s):  
Tran Khac Vu

The paper presents a simple synthesis of new quinazolinone derivatives 13a-i. Synthesized derivatives were tested for their cytotoxic effect against three cancer cell lines including SKLU-1, MCF-7 and HepG-2. The bioassay result showed that only compound 13e exhibited significant cytotoxic effect against cancer cell lines tested with IC50 values of 9.48, 20.39 and 18.04 µg/ mL, 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.


2021 ◽  
Vol 11 (8) ◽  
pp. 3510
Author(s):  
Loubna El Fakir ◽  
Kaoutar Bouothmany ◽  
Amal Alotaibi ◽  
Mohammed Bourhia ◽  
Riaz Ullah ◽  
...  

The current research was conducted to investigate the chemical profile, antiproliferative, and antioxidant activities of methanol extracts obtained by two different methods including maceration and Soxhlet from Berberis hispanica Boiss. & Reut. Antiproliferative activities were evaluated by the MTT (3-(4, 5-dimethylthiazolyl-2)-2, 5-diphenyltetrazolium bromide) assay in four human cancer cell lines including prostate (LnCap and 22 RV1) and breast cancer (MDA-MB-231 and MCF7). The antioxidant power was evaluated by DPPH ((2,2-diphenyl-1-picryl-hydrazyl-hydrate), ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), and FRAPS (Ferric reducing antioxidant power) tests. The chemical composition was conducted by gas chromatography-mass spectrometry (GC-MS) after methylation. Total phenolic and flavonoid contents were assessed using the Folin–Ciocalteu method. The phytochemical analysis showed that the tested extracts possessed inserting potentially active compounds. The MTT test revealed that both extracts (maceration and Soxhlet) reduced cell viability in all cell lines tested. In breast cancer cell lines MDA-MB-231 and MCF-7, the IC50 values obtained by maceration were 16.55 ± 0.58 and 17.95 ± 0.58 µg/mL, respectively. These values were slightly lower than those obtained with the Soxhlet extract toward MDA-MB-231 (19.93 ± 0.74 µg/mL) and MCF-7 (20.22 ± 0.89 µg/mL). Regarding prostate cancer cells 22 RV and LnCap, the IC50 values obtained by maceration extract (22 RV: 11.75 ± 0.35 µg/mL; LnCap: 11.91 ± 0.54 µg/mL) were also slightly lower than those obtained with Soxhlet (22 RV: 13.47 ± 0.52 µg/mL; LnCap: 19.64 ± 1.05 µg/mL). The antioxidant activity showed that the studied extracts had considerable antioxidant activity (DPPH, FRAP, and ABTS) with particular attention to the extract obtained with maceration. The Berberis hispanica Bois. and Reut. can serve society as it provides potentially bioactive compounds that may find application in the medical sector to control such diseases.


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