دورية أكاديمية
Novel betulin derivatives inhibit IFN-γ and modulates COX-2 expression.
| العنوان: | Novel betulin derivatives inhibit IFN-γ and modulates COX-2 expression. |
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| المؤلفون: | Gonçalves SMC; Laboratory of Immunomodulation and New Therapeutic Approaches (LINAT), Research Center Innovation Therapeutics Suely Galdino (NUPIT-SG), Federal University of Pernambuco, Recife, Brazil., Silva GN; Organic Synthesis Laboratory of Phytochemistry, Federal University of Rio Grande do Sul, Porto Alegre, Brazil., Pitta IDR; Laboratory of Immunomodulation and New Therapeutic Approaches (LINAT), Research Center Innovation Therapeutics Suely Galdino (NUPIT-SG), Federal University of Pernambuco, Recife, Brazil., Rêgo MJBM; Laboratory of Immunomodulation and New Therapeutic Approaches (LINAT), Research Center Innovation Therapeutics Suely Galdino (NUPIT-SG), Federal University of Pernambuco, Recife, Brazil., Gnoato SCB; Organic Synthesis Laboratory of Phytochemistry, Federal University of Rio Grande do Sul, Porto Alegre, Brazil., Pitta MGDR; Laboratory of Immunomodulation and New Therapeutic Approaches (LINAT), Research Center Innovation Therapeutics Suely Galdino (NUPIT-SG), Federal University of Pernambuco, Recife, Brazil. |
| المصدر: | Natural product research [Nat Prod Res] 2020 Jun; Vol. 34 (12), pp. 1702-1711. Date of Electronic Publication: 2018 Dec 22. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Taylor & Francis Health Sciences Country of Publication: England NLM ID: 101167924 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1478-6427 (Electronic) Linking ISSN: 14786419 NLM ISO Abbreviation: Nat Prod Res Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Milton Park, UK : Taylor & Francis Health Sciences, c2003- |
| مواضيع طبية MeSH: | Anti-Inflammatory Agents/*pharmacology , Antineoplastic Agents/*pharmacology , Cyclooxygenase 2/*metabolism , Interferon-gamma/*antagonists & inhibitors , Peptide Fragments/*antagonists & inhibitors , Triterpenes/*pharmacology, Cell Line, Tumor ; Cyclooxygenase 2/drug effects ; Cytokines/metabolism ; Esters/pharmacology ; Halogenation ; Humans ; MCF-7 Cells ; Structure-Activity Relationship ; Triterpenes/chemistry |
| مستخلص: | Betulin ( BE ) is a pentacyclic triterpenes, obtained from natural sources and with several biological activities described, such as anti-tumoral and anti-inflammatory activities. The BE esterification at hydroxyl group (C-3 and C-28) resulted in five new ester derivatives with different numbers of carbons or halogens (chlorine and fluorine). Among these BE derivatives, two ( 2a e 2c ) were able to significantly decrease IFN-g (*p = 0.0391; **p = 0.0156) and 2c modulated the expression of COX-2 better than Dexamethasone ( DEXA ). Regarding to cytotoxic assay, the best results were obtained for BE without modifications, with emphasis on tumoral cell lines Raji and MCF-7. The derivatives 2a and 2c showed immunomodulation activity (for the cytokines IFN-g). The presence of chorine in BE seems to be important for the ability of modulate COX-2 expression, since the ester chloride derivative 2c at 100 μM is more powerful inhibitor of COX-2 than DEXA . |
| فهرسة مساهمة: | Keywords: Betulin; cyclooxygenase-2; cytokines; cytotoxicity; derivatives |
| المشرفين على المادة: | 0 (Anti-Inflammatory Agents) 0 (Antineoplastic Agents) 0 (Cytokines) 0 (Esters) 0 (Peptide Fragments) 0 (Triterpenes) 0 (interferon gamma (1-39)) 6W70HN7X7O (betulin) 82115-62-6 (Interferon-gamma) EC 1.14.99.1 (Cyclooxygenase 2) |
| تواريخ الأحداث: | Date Created: 20181225 Date Completed: 20200720 Latest Revision: 20200720 |
| رمز التحديث: | 20231215 |
| DOI: | 10.1080/14786419.2018.1528581 |
| PMID: | 30580627 |
| قاعدة البيانات: | MEDLINE |
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Full Text Finder | تدمد: | 1478-6427 |
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| DOI: | 10.1080/14786419.2018.1528581 |