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Biological evaluation of sulfone derivatives as anti-inflammatory and tumor cells growth inhibitory agents.
Int Immunopharmacol. 2006 Nov; 6(11):1699-705.II

Abstract

A variety of sulfone derivatives including three dimethyl arylsulfonyl malonates (1-3), two bis-(arylethenesulfonyl)-vinyl benzenes (4 and 5) and a sulfone triazole (6) were evaluated for their anti-inflammatory as well as tumor cells growth inhibitory activities in vitro. The sulfone derivatives 1, 2, 3 and 6 significantly and dose-dependently inhibited the production of inflammatory mediators such as nitric oxide (NO), and cytokines (tumor necrosis factor (TNF)-alpha and interleukin (IL)-12), in lipopolysaccharide (LPS) and interferon (IFN)-gamma activated murine peritoneal macrophages, without displaying cytotoxicity. The inhibitory mechanism is found through reducing iNOS protein expression. In addition, the derivatives 1-3 significantly arrest mitogen-stimulated spleen cells in G0/G1 stage, whereas compounds 4-6 blocked the same in the G2/M phase. Furthermore, the sulfone derivatives 3 and 6 showed dramatically reduction in the ratio of IFN-gamma to IL-4 production from mitogen-stimulated spleen cells. On the other hand, the novel compounds exhibited interesting cytotoxic activities against a panel of cell lines, particularly, 20 muM of compound 3 showed 50% cytotoxic effect on human hepatoma cell line, but has no effect on normal human peripheral blood mononuclear cells. In conclusion, compound 3 showed interesting anti-inflammatory and tumor cells growth inhibitory functions.

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Authors+Show Affiliations

Fang SH
Department of Microbiology, School of Medicine, China Medical University, Taichung 404, Taiwan, ROC.
Padmavathi V
No affiliation info available
Rao YK
No affiliation info available
Venkata Subbaiah DR
No affiliation info available
Thriveni P
No affiliation info available
Geethangili M
No affiliation info available
Padmaja A
No affiliation info available
Tzeng YM
No affiliation info available

MeSH

AnimalsAnti-Inflammatory AgentsAntineoplastic AgentsCell CycleCell Line, TumorCell ProliferationHumansInterferon-gammaInterleukin-12Leukocytes, MononuclearLipopolysaccharidesMacrophages, PeritonealMalonatesMiceMice, Inbred BALB CNitric OxideNitric Oxide Synthase Type IISpleenSulfonesTumor Necrosis Factor-alpha

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

16979124

Citation

Fang, Shih-Hua, et al. "Biological Evaluation of Sulfone Derivatives as Anti-inflammatory and Tumor Cells Growth Inhibitory Agents." International Immunopharmacology, vol. 6, no. 11, 2006, pp. 1699-705.
Fang SH, Padmavathi V, Rao YK, et al. Biological evaluation of sulfone derivatives as anti-inflammatory and tumor cells growth inhibitory agents. Int Immunopharmacol. 2006;6(11):1699-705.
Fang, S. H., Padmavathi, V., Rao, Y. K., Venkata Subbaiah, D. R., Thriveni, P., Geethangili, M., Padmaja, A., & Tzeng, Y. M. (2006). Biological evaluation of sulfone derivatives as anti-inflammatory and tumor cells growth inhibitory agents. International Immunopharmacology, 6(11), 1699-705.
Fang SH, et al. Biological Evaluation of Sulfone Derivatives as Anti-inflammatory and Tumor Cells Growth Inhibitory Agents. Int Immunopharmacol. 2006;6(11):1699-705. PubMed PMID: 16979124.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Biological evaluation of sulfone derivatives as anti-inflammatory and tumor cells growth inhibitory agents. AU - Fang,Shih-Hua, AU - Padmavathi,V, AU - Rao,Yerra Koteswara, AU - Venkata Subbaiah,D R C, AU - Thriveni,P, AU - Geethangili,Madamanchi, AU - Padmaja,A, AU - Tzeng,Yew-Min, Y1 - 2006/07/31/ PY - 2006/05/22/received PY - 2006/06/27/revised PY - 2006/07/06/accepted PY - 2006/9/19/pubmed PY - 2006/12/14/medline PY - 2006/9/19/entrez SP - 1699 EP - 705 JF - International immunopharmacology JO - Int Immunopharmacol VL - 6 IS - 11 N2 - A variety of sulfone derivatives including three dimethyl arylsulfonyl malonates (1-3), two bis-(arylethenesulfonyl)-vinyl benzenes (4 and 5) and a sulfone triazole (6) were evaluated for their anti-inflammatory as well as tumor cells growth inhibitory activities in vitro. The sulfone derivatives 1, 2, 3 and 6 significantly and dose-dependently inhibited the production of inflammatory mediators such as nitric oxide (NO), and cytokines (tumor necrosis factor (TNF)-alpha and interleukin (IL)-12), in lipopolysaccharide (LPS) and interferon (IFN)-gamma activated murine peritoneal macrophages, without displaying cytotoxicity. The inhibitory mechanism is found through reducing iNOS protein expression. In addition, the derivatives 1-3 significantly arrest mitogen-stimulated spleen cells in G0/G1 stage, whereas compounds 4-6 blocked the same in the G2/M phase. Furthermore, the sulfone derivatives 3 and 6 showed dramatically reduction in the ratio of IFN-gamma to IL-4 production from mitogen-stimulated spleen cells. On the other hand, the novel compounds exhibited interesting cytotoxic activities against a panel of cell lines, particularly, 20 muM of compound 3 showed 50% cytotoxic effect on human hepatoma cell line, but has no effect on normal human peripheral blood mononuclear cells. In conclusion, compound 3 showed interesting anti-inflammatory and tumor cells growth inhibitory functions. SN - 1567-5769 UR - https://www.unboundmedicine.com/medline/citation/16979124/Biological_evaluation_of_sulfone_derivatives_as_anti_inflammatory_and_tumor_cells_growth_inhibitory_agents_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S1567-5769(06)00204-9 DB - PRIME DP - Unbound Medicine ER -