scholarly journals Anti-Cancer and Anti-Inflammatory Activities of Three New Chromone Derivatives from the Marine-Derived Penicillium citrinum

Marine Drugs ◽  
2021 ◽  
Vol 19 (8) ◽  
pp. 408
Author(s):  
Yi-Cheng Chu ◽  
Chun-Hao Chang ◽  
Hsiang-Ruei Liao ◽  
Shu-Ling Fu ◽  
Jih-Jung Chen
Keyword(s):  
Human Colon ◽  
Penicillium Citrinum ◽  
Signaling Cascades ◽  
Human Neutrophils ◽  
Cytotoxic Activities ◽  
Western Blot Assay ◽  
Anti Cancer ◽  
Ic50 Values ◽  
Induced Apoptosis ◽  
Ht 29

Three new and uncommon chromone analogs, epiremisporine F (1), epiremisporine G (2), and epiremisporine H (3), were isolated from marine-origin Penicillium citrinum. Among the isolated compounds, compounds 2–3 remarkably suppressed fMLP-induced superoxide anion generation by human neutrophils, with IC50 values of 31.68 ± 2.53, and 33.52 ± 0.42 μM, respectively. Compound 3 exhibited cytotoxic activities against human colon carcinoma (HT-29) and non-small lung cancer cell (A549) with IC50 values of 21.17 ± 4.89 and 31.43 ± 3.01 μM, respectively, and Western blot assay confirmed that compound 3 obviously induced apoptosis of HT-29 cells, via Bcl-2, Bax, and caspase 3 signaling cascades.

scholarly journals Rare Chromone Derivatives from the Marine-Derived Penicillium citrinum with Anti-Cancer and Anti-Inflammatory Activities

Marine Drugs ◽  
2021 ◽  
Vol 19 (1) ◽  
pp. 25
Author(s):  
Yi-Cheng Chu ◽  
Chun-Hao Chang ◽  
Hsiang-Ruei Liao ◽  
Ming-Jen Cheng ◽  
Ming-Der Wu ◽  
...  
Keyword(s):  
A549 Cells ◽  
Penicillium Citrinum ◽  
Signaling Cascades ◽  
Human Neutrophils ◽  
Cytotoxic Activities ◽  
Western Blot Assay ◽  
Chromone Derivatives ◽  
Anti Cancer ◽  
Ic50 Values ◽  
Induced Apoptosis

Three new and rare chromone derivatives, epiremisporine C (1), epiremisporine D (2), and epiremisporine E (3), were isolated from marine-derived Penicillium citrinum, together with four known compounds, epiremisporine B (4), penicitrinone A (5), 8-hydroxy-1-methoxycarbonyl-6-methylxanthone (6), and isoconiochaetone C (7). Among the isolated compounds, compounds 2–5 significantly decreased fMLP-induced superoxide anion generation by human neutrophils, with IC50 values of 6.39 ± 0.40, 8.28 ± 0.29, 3.62 ± 0.61, and 2.67 ± 0.10 μM, respectively. Compounds 3 and 4 exhibited cytotoxic activities with IC50 values of 43.82 ± 6.33 and 32.29 ± 4.83 μM, respectively, against non-small lung cancer cell (A549), and Western blot assay confirmed that compounds 3 and 4 markedly induced apoptosis of A549 cells, through Bcl-2, Bax, and caspase 3 signaling cascades.

scholarly journals Synthesis and biological evaluation of 4-substituted aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione as anti-cancer and anti-angiogenesis agents

2020 ◽  
Author(s):  
Lifang Guo ◽  
Benshan Xu ◽  
Zirui Wan ◽  
Lulu Ren ◽  
Jie Zhang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Cytotoxic Activities ◽  
Chemical Structures ◽  
Piperazine Derivatives ◽  
Anti Cancer ◽  
Ic50 Values ◽  
And Migration ◽  
Anti Tumor Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Abstract Background: A series of aryl-piperazine derivatives of 1,7,8,9-tetrachloro-10,10-dimethoxy-4-azatricyclo [5.2.1.02,6] dec-8-ene-3,5-dione were synthesized. The chemical structures of the desired compounds were identified by 1H NMR, ESI-MS and elementary analytical. The anti-cancer and anti-angiogenesis activities of the newly synthesized compounds were evaluated by proliferation and migration assays, respectively. Results: The screening results demonstrated that compounds 2 and 5 showed potent anti-tumor activity (IC50 values ranging from 7.1 to 15.9μM) with low cytotoxic activities (IC50＞79.3μM). Although compound 5 showed little effects on endothelia proliferation (IC50=65.3μM), it indeed significantly abrogated endothelia cell migration (IC50=6.7μM). Conclusions: This work may impart new direction for the investigations of aryl-piperazine derivatives and lead to the development of potent novel anti-tumor and anti-angiogenesis agents.

scholarly journals Novel O-alkyl Derivatives of Naringenin and Their Oximes with Antimicrobial and Anticancer Activity

Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 679 ◽  
Author(s):  
Joanna Kozłowska ◽  
Ewa Grela ◽  
Dagmara Baczyńska ◽  
Agnieszka Grabowiecka ◽  
Mirosław Anioł
Keyword(s):  
Cancer Cell Line ◽  
Human Colon ◽  
Colon Cancer Cell Line ◽  
Human Colon Cancer ◽  
Anticancer Properties ◽  
Alkyl Derivatives ◽  
Ic50 Values ◽  
Oxime Derivatives ◽  
Derivatives Of ◽  
Ht 29

In our investigation, we concentrated on naringenin (NG)—a widely studied flavanone that occurs in citrus fruits. As a result of a reaction with a range of alkyl iodides, 7 novel O-alkyl derivatives of naringenin (7a–11a, 13a, 17a) were obtained. Another chemical modification led to 9 oximes of O-alkyl naringenin derivatives (7b–13b, 16b–17b) that were never described before. The obtained compounds were evaluated for their potential antibacterial activity against Escherichia coli, Staphylococcus aureus, and Bacillus subtilis. The results were reported as the standard minimal inhibitory concentration (MIC) values and compared with naringenin and its known O-alkyl derivatives. Compounds 4a, 10a, 12a, 14a, 4b, 10b, 11b, and 14b were described with MIC of 25 µg/mL or lower. The strongest bacteriostatic activity was observed for 7-O-butylnaringenin (12a) against S. aureus (MIC = 6.25 µg/mL). Moreover, the antitumor effect of flavonoids was examined on human colon cancer cell line HT-29. Twenty-six compounds were characterized as possessing an antiproliferative activity stronger than that of naringenin. The replacement of the carbonyl group with an oxime moiety significantly increased the anticancer properties. The IC50 values below 5 µg/mL were demonstrated for four oxime derivatives (8b, 11b, 13b and 16b).

scholarly journals Cytotoxic Sterols from Philippine Mushrooms

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
Keyword(s):  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Dermal Fibroblast ◽  
Cancer Cell Lines ◽  
Cytotoxic Activities ◽  
Cell Viability Assay ◽  
Ic50 Values ◽  
Ht 29 ◽  
Mcf 7

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.

Gentio-oligosaccharides from Leuconostoc mesenteroides NRRL B-1426 dextransucrase as prebiotics and as a supplement for functional foods with anti-cancer properties

2015 ◽  
Vol 6 (2) ◽  
pp. 604-611 ◽  
Author(s):  
Damini Kothari ◽  
Arun Goyal
Keyword(s):  
Colon Carcinoma ◽  
Functional Foods ◽  
Leuconostoc Mesenteroides ◽  
Human Colon ◽  
Selective Inhibition ◽  
Prebiotic Activity ◽  
Human Colon Carcinoma ◽  
Anti Cancer ◽  
Ht 29

Gentio-oligosaccharides (GnOS) fromLeuconostoc mesenteroidesNRRL B-1426 dextransucrase showed potential prebiotic activity and selective inhibition of human colon carcinoma (HT-29) cells.

A Novel 4H-Chromen-4-One Derivative from Marine Streptomyces ovatisporus S4702T as Potential Antibacterial and Anti-Cancer Agent

2021 ◽  
Vol 21 ◽  
Author(s):  
Aslıhan Kurt-Kızıldoğan ◽  
Neslihan Akarsu ◽  
Çiğdem Otur ◽  
Arif Kivrak ◽  
Nevroz Aslan-Ertas ◽  
...  
Keyword(s):  
Micrococcus Luteus ◽  
Chemical Characterization ◽  
Bioactive Compound ◽  
Human Colon ◽  
Cytotoxic Activities ◽  
Human Embryonic Kidney Cells ◽  
Anti Cancer ◽  
Cancer Agent ◽  
Bioactive Potential

Background: Marine actinomycetes are among indispensable sources of natural bioactive compounds with unique antimicrobial and anti-cancer activities. Objective: Herein, it was aimed to elucidate bioactive potential of a marine-derived Streptomyces ovatisporus S4702T, isolated previously. Methods: Streptomyces ovatisporus S4702T was cultured in N-Z Amine broth and extraction was carried out using different organic solvents. Bioassay guided purification was followed by chemical characterization using NMR and LC-MS/MS. The compound was then evaluated for its antibacterial, antioxidant and cytotoxic activities. Results: Etyl acetate extracts gave the highest antibacterial activity and chemical characterization of this extract indicated the formula as C15H29O5N3 and the corresponding possible molecular structure as 4H-chromen-4-one derivative. It was found highly potent against Bacillus subtilis ATCC 6633 (MIC: 0.25 µg ml-1) and Micrococcus luteus ATCC 9341 (MBC: 0.5 µg ml-1). It has no remarkable antioxidant activity, but higher EC50 value and less cytotoxicity against normal cells. The EC50 values of this chromen derivative were found as 9.68 µg ml-1 for human colon carcinoma, 9.93 µg ml-1 for human prostate adenocarcinoma and 25.5 µg ml-1 for human embryonic kidney cells. Conclusion: Overall, the presented 4H-chromen-4-one derivative is a remarkable bioactive compound with potent antibacterial and cytotoxic activity. With its high bioactive potential, it is proposed as a good candidate in medicine.

scholarly journals Leptin Counteracts Sodium Butyrate-induced Apoptosis in Human Colon Cancer HT-29 Cells via NF-κB Signaling

2004 ◽  
Vol 279 (16) ◽  
pp. 16495-16502 ◽  
Author(s):  
Patricia Rouet-Benzineb ◽  
Thomas Aparicio ◽  
Sandra Guilmeau ◽  
Cécile Pouzet ◽  
Véronique Descatoire ◽  
...  
Keyword(s):  
Colon Cancer ◽  
Sodium Butyrate ◽  
Human Colon ◽  
Human Colon Cancer ◽  
Induced Apoptosis ◽  
Ht 29
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