Biological Activities of Flavonoids from the Wood Extract of Artocarpus heterophyllus L. (Jackfruit)

Background: Artocarpus heterophyllus L. (Jackfruit) has been used traditionally as treatment for inflammation and cancer. The aim of this study was to isolate compounds from A. heterophyllus wood extract and evaluate their biological activities such as anti-tumor promoting effect on Epstein-Barr virus early antigen induction, melanogenesis inhibitory activity on the B16 mouse melanoma 4A5 cell line and cytotoxic activity against three human cancer cell lines (HL60, A549, SK-BR-3). Methods: A. heterophyllus wood was extracted with n-hexane and methanol. The ethyl acetate soluble- fraction separated from the methanol extract was separated and purified with column chromatography to isolate compounds. The structures of isolated compounds were elucidated with spectroscopic methods. These compounds were evaluated for their biological activities. Results: Thirteen known compounds including four prenylflavonoids were isolated from the wood extracts. Nine flavonoids (2, 3, 5-11) exhibited potent anti-tumor promoting activity with IC50 values of 259-296 molar ratio / 32 pmol TPA. Two flavonoids, Norartocarpetin (6) at concentration of 30 μM and cyanomaclurin (11) at the concentration of 100 μM showed melanin content value of 47.6 % and 80.1 %, respectively. Two prenylflavonoids, cudraflavone B (2) and artocarpin (5), showed cytotoxicity against the human cancer cell lines tested. Cudraflavone B (2) showed cytotoxicity against all three human cancer cell lines whereas artocarpin (5) only exhibited cytotoxicity against two out three cell lines testes. The IC50 values were comparable to or better than cisplatin. Conclusion: From the view point of structure activity relationships of the flavonoids isolated, side chains such as prenyl and 3-methyl-1-butenyl moiety were key for their potent biological activities.

Download Full-text

The Evaluation of Potential Cytotoxic Effect of Different Proton Pump Inhibitors on Different Human Cancer Cell Lines

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520619666191029151545 ◽

2020 ◽

Vol 20 (2) ◽

pp. 245-253

Author(s):

Aya Qasem ◽

Violet Kasabri ◽

Eman AbuRish ◽

Yasser Bustanji ◽

Yusuf Al-Hiari ◽

...

Keyword(s):

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Cancer Cell Lines ◽

Raw 264.7 ◽

Human Cancer Cell ◽

Raw 264.7 Macrophages ◽

Human Cancer Cell Lines ◽

Ic50 Values

Objective : To assess the differential cytotoxic activity of PPIs on different human cancer cell lines; namely A549 lung cancer, CACO-2 colorectal cancer, MCF-7 breast cancer, and PANC-1 pancreatic cancer, A375 skin melanoma. Methods: In this study, the five human cancer cell lines and human non-cancerous fibroblasts were treated with increasing concentration of PPIs Omeprazole (OMP), Esomeprazole (ESOM), and Lansoprazole (LANSO) (50-300μM), over 24h, 48h, and 72h. Cell viability was determined using 3-(4,5- Dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) assay and the IC50 values of PPIs were measured. The most sensitive cell line A375 was used for further investigation. The cytotoxic effects of LANSO on these cells were assessed using Annexin-V Propidium Iodide (AV-PI) flow cytometry. As of action mechanism; anti-inflammatory effects of each PPIs and PPIs-DOXO combination therapy on LPS-stimulated RAW 264.7 mouse macrophages were assessed. Results: Dose and time dependence cytotoxic activity of PPIs on human cancer cell lines was founded. Unlike DOXO; All PPIs had a selective cytotoxic effect in the normal fibroblasts. Unlike the equipotent OMP and ESOM; LANSO was the most potent drug with IC50 values at 72h of 99, 217, 272, 208, 181μM against A375, A549, CACO-2, MCF-7, and PANC-1, respectively. AV-PI flow cytometry revealed dose-dependent apoptotic effects of LANSO alone and substantially enhanced in DOXO-co-treatments. Interestingly unlike ESOM and OMP, LANSO proved more effective than indomethacin in LPS-stimulated RAW 264.7 macrophages. None of the tested compounds, as well as indomethacin, exerted any cytotoxicity against RAW 264.7 macrophages. PPIs-DOXO lacked potential synergistic combination antiinflammation therapies. Conclusion: This study provides the evidence that PPIs induce a direct and differential cytotoxic activity against human cancer cell line by the induction of the apoptosis. Moreover, PPIs increase cancer cell lines sensitivity to doxorubicin via apoptosis augmentation. Nevertheless, PPIs-DOXO lacked potential synergistic combination therapies in either antiproliferation or anti-inflammation.

Download Full-text

Novel Artemisinin-Derived Dimers: Synthesis and Evaluation of Anti-cancer Activities

Letters in Drug Design & Discovery ◽

10.2174/1570180813666160810155354 ◽

2016 ◽

Vol 14 (1) ◽

pp. 102-111 ◽

Cited By ~ 4

Author(s):

Vu Tuan Kien ◽

Le Huy Binh ◽

Phan Hai Phong ◽

Doan Thi Hien ◽

Nguyen Thi Thuy My ◽

...

Keyword(s):

Cancer Cells ◽

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Cancer Cell Lines ◽

Human Cancer Cell ◽

Anticancer Compounds ◽

Human Cancer Cell Lines ◽

Ic50 Values ◽

Mcf 7

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.

Download Full-text

Synthesis of New Zerumbone Hydrazones and Their In vitro Anticancer Activity

Current Bioactive Compounds ◽

10.2174/1573407216999200630133625 ◽

2020 ◽

Vol 16 ◽

Author(s):

Vu Van Vu ◽

Tran Khac Vu

Keyword(s):

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Cancer Cell Lines ◽

Human Cancer Cell ◽

Cytotoxic Effects ◽

Human Cancer Cell Lines ◽

Ic50 Values ◽

Bioassay Result ◽

Mcf 7

Background: A series of new zerumbone hydrazones 5a-f and 9a-f have been synthesized via an in situ procedure in high yields. The structure of synthesized compounds has been confirmed using 1H, 13C NMR and HR-MS. The bioassay result showed that several compounds exhibited cytotoxic effects against three human cancer cell lines including HepG-2, SK-LU-1 and MCF-7. Compound 9a showed the best cytotoxic effect against HepG-2, SK-LU-1 and MCF-7 with IC50 values of 8.20, 6.66 and 9.35 µM, respectively. Objective: This study aims at developing new zerumbone hydrazones as anticancer agents based on zerumbone, a natural compound wildly growing in Vietnam. Method: A series of new zerumbone hydrazones was designed, synthesized and evaluated for cytotoxicity against three human cancer cell lines, including HepG-2, MCF-7 and SKLu-1 using MTT method. Results: The bioassay result showed that several compounds exhibited cytotoxic effects against three human cancer cell lines including HepG-2, SK-LU-1 and MCF-7. Especially, compound 9a displayed the best cytotoxic effect against HepG-2, SK-LU-1 and MCF-7 with IC50 values of 8.20, 6.66 and 9.35 µM, respectively. Results: The bioassay result showed that several compounds exhibited cytotoxic effects against three human cancer cell lines including HepG-2, SK-LU-1 and MCF-7. Especially, compound 9a displayed the best cytotoxic effect against HepG-2, SK-LU-1 and MCF-7 with IC50 values of 8.20, 6.66 and 9.35 µM, respectively. Conclusion: The research results suggest that some compounds could be considered as a lead for future design of zerumbone hydrazones in which bio-isosteric replacements in ortho position of the phenyl ring could be performed to improve the cytotoxic activity.

Download Full-text

Design, Synthesis and In vitro Cytotoxic Evaluation of Novel Hybrids of Artemisinin and Quinazolinone

Letters in Organic Chemistry ◽

10.2174/1570178618666211001115131 ◽

2021 ◽

Vol 18 ◽

Author(s):

Tran Khac Vu ◽

Bach Xuan Nguyen ◽

Linh Nguyen Pham Duy ◽

Thuc Bao Nguyen Truong ◽

Anh Tuan Phung ◽

...

Keyword(s):

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Cancer Cell Lines ◽

Human Cancer Cell ◽

Human Cancer Cell Lines ◽

Anti Cancer ◽

Ic50 Values ◽

Mcf 7

Background: In this study, two novel hybrid series of artemisinin and quinazolinones were synthesized and evaluated in vitro cytotoxicity against two human cancer cell lines, including SKLu-1 (lung cancer), MCF- 7 (breast cancer). The bio-assay results indicated that most of the target compounds exhibited cytotoxic activities against both human cancer cell lines tested, and seemed to be more cytotoxic toward the breast (MCF-7) cancer cells than lung (SKLu-1) cancer cells. Among the synthesized artemisinin hybrids, the compound 13d containing a quinazolinone conjugated system exhibited the most potent cytotoxicity against the SKLu-1 and MCF-7 cell lines with IC50 values of 1.62 and 0.77 µM, respectively. Objective: This study aims at developing novel hybrids of artemisinin and quinazolinones as anti-cancer agents. Method: A series of novel hybrids were designed, synthesized and evaluated for cytotoxicity against two human cancer cell lines, including SKLu-1 and MCF-7 using SRB method. Results : All thirteen hybrids of artemisinin with quinazolinone exhibited cytotoxic activity against two tested cancer cell lines, in which the compound 13d exhibited the most potent cytotoxicity against the SKLu-1 and MCF-7 cell lines with IC50 values of 1.62 and 0.77 µM, respectively. Conclusion: The research results suggest that some compounds could be considered as leads for future design of hybrids and have the potential for further studies in the field of anti-cancer agent development.

Download Full-text

Mollicellins O–R, Four New Depsidones Isolated from the Endophytic Fungus Chaetomium sp. Eef-10

Molecules ◽

10.3390/molecules23123218 ◽

2018 ◽

Vol 23 (12) ◽

pp. 3218 ◽

Cited By ~ 4

Author(s):

Jinkui Ouyang ◽

Ziling Mao ◽

Hui Guo ◽

Yunying Xie ◽

Zehua Cui ◽

...

Keyword(s):

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Radical Scavenging ◽

Antibacterial Activities ◽

Cancer Cell Lines ◽

Cytotoxic Activities ◽

Human Cancer Cell ◽

Human Cancer Cell Lines ◽

Ic50 Values

Four new depsidones, mollicellins O–R (compounds 1–4), along with three known compounds 5–7, were isolated from cultures of the fungus Chaetomium sp. Eef-10, an endophyte isolated from Eucalyptus exserta. The structures of the new compounds were elucidated by analysis of the 1D and 2D NMR and HR-ESI-MS spectra. The known compounds were identified by comparison of their spectral data with published values. Compounds 1–7 were evaluated for antibacterial activities against Staphylococcus aureus (sensitive and resistant strains), Escherichia coli, Agrobacterium tumefaciens, Salmonella typhimurium, Pseudomonas lachrymans, Ralstonia solanacearum, Xanthomonas vesicatoria and cytotoxic activities against two human cancer cell lines (HepG2 and Hela). Mollicellin H (6) displayed best antibacterial activity, with IC50 values of 5.14 µg/mL against S. aureus ATCC29213 and 6.21 µg/mL against S. aureus N50, MRSA, respectively. Mollicellin O (1) and mollicellin I (7) also exhibited antibacterial activities against S. aureus ATCC29213 and S. aureus N50. Mollicellin G (5) was active against both two human cancer cell lines, with IC50 values of 19.64 and 13.97 µg/mL while compounds 6 and 7 only showed cytotoxic activity against one cell line. In addition, mollicellin O (1) showed antioxidant activity based on DPPH radical scavenging, with an IC50 value of 71.92 µg/mL.

Download Full-text

Cytotoxicity Activities in Local Justicia gendarussa Crude Extracts against Human Cancer Cell Lines

Jurnal Teknologi ◽

10.11113/jt.v64.2043 ◽

2013 ◽

Vol 64 (2) ◽

Cited By ~ 3

Author(s):

Zahidah Ayob ◽

Azman Abd Samad ◽

Siti Pauliena Mohd Bohari

Keyword(s):

Cytotoxic Activity ◽

Cell Lines ◽

Cancer Cell ◽

Human Cancer ◽

Cancer Cell Lines ◽

Human Cancer Cell ◽

Leaf Extracts ◽

Human Cancer Cell Lines ◽

Ic50 Values ◽

Cytotoxicity Activities

The present study was designed to evaluate the cytotoxic activity of Justicia gendarussa methanolic leaf extracts from five different locations in Johor and also two standards flavonoids (naringenin and kaempferol) as these two compounds were detected in the chromatogram. In this study, leaf extracts and compounds were tested against various human cancer cell lines (HT-29, HeLa and BxPC-3) by using MTT assay. The results showed that methanolic leaf extracts from Mersing and kaempferol were very toxic against BxPC-3 and HeLa cells with IC50 values of 16 µg/ml and 5 µg/ml, respectively. It is suggested that J. gendarussa leaf extracts from Mersing have potential cytotoxic activity on human cancer cell lines particularly BxPC-3 cells.

Download Full-text