Oleanolic acid modulates the immune-inflammatory response in mice with experimental autoimmune myocarditis and protects from cardiac injury. Therapeutic implications for the human disease

Topical Anti-inflammatory Activity of New Hybrid Molecules of Terpenes and Synthetic Drugs

“…All the new compounds showed a better effect in the TPA assay, with best activity for compounds 12, 14 and 15. (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14)(15) or reference drugs at the equimolar dose of 3.2 µmol/mouse for the AA and 1.4 µmol/mouse for the TPA assays, respectively.…”

“…Ferruginyl ibuprofenate (6) >1000 >1000 874 ± 34 Ferruginyl naproxenate (7) 945 ± 56 874 ± 49 >1000 Imbricatol-15-yl ibuprofenate (8) 34 ± 2 23 ± 1 79 ± 8 Imbricatol-15-yl ibuprofenate methyl ester (9) 706 ± 35 623 ± 39 746 ± 38 Imbricatol-15-yl naproxenate (10) 37 ± 2 29 ± 2 69 ± 4 Imbricatol-15-yl naproxenate methyl ester (11) 907 ± 54 601 ± 25 >1000 Oleanoyl ibuprofenate (12) 616 ± 32 526 ± 19 >1000 Oleanoyl ibuprofenate methyl ester (13) 402 ± 20 454 ± 21 742 ± 48 Oleanoyl naproxenate (14) 554 ± 22 486 ± 26 >1000 Oleanoyl naproxenate methyl ester (15) 816 ± 42 593 ± 31 >1000 The diterpene 2 presents cytotoxicity with IC50 values ranging from 111 to 148 µM. The derivatives 8 and 10 (IC50 values 23-79 µM and 29-69 µM, respectively) were more cytotoxic than the starting natural product and the synthetic anti-inflammatory agents alone.…”

“…It presents strong inhibition of lipid peroxidation in erythrocytes [6] as well as on superoxide anion generated in phorbol myristate acetate-stimulated rat neutrophils [7]. The triterpene oleanolic acid has been shown to display several relevant biological activities, including the modulation of the immune-inflammatory response [8], reduction of differentiation markers in adipocytes and suppression of inflammation associated with obesity [9]. The anti-inflammatory and analgesic effect of semisynthetic oleanolic acid derivatives was recently reported [10].…”

Biologically Active Triterpenoids and Their Cardioprotective and Anti- Inflammatory Effects

“…More specifically, α-and β-amyrins (AMY) are bioactive compounds that have been identified as anti-inflammatory and anti-oxidant agent agents by multiple sources and thus used for the treatment of diverse inflammation-related diseases . The chemical formula of α-amyrin(3α-hydroxy-urs-12-en-3-ol) is C 30 H 50 O (Figure 2), and its melting point is 184-186°C [103]; the chemical formula of β-amyrin(3β-hydroxy-olean-12-en-3-ol) is C 30 H 50 O (Figure 2) [106][107][108][109][110][111][112] and its melting point is 189-191°C [84]. Quintão et al (2014) demonstrated that AMY interferes in both acute and chronic inflammatory processes in mice by reducing mechanical hypersensitivity, mechanical sensitization, and oedema development in arthritis [86].…”

“…OA was also found by Bachhav et al (2011) to confer nitric oxide releasing mechanism, significantly decreasing the level of plasma nitrate/nitrite [55]. In various studies, OA was found to inhibit COX-2 enzyme and Th1 responses, which can reduce the risk of inflammation [48,109]. Similar effects were found in maslinic acid (MA) products such as olive fruits, with a mechanism that significantly suppressed the expression of COX-2 and iNOS, in turn having an anti-inflammatory Page 8 of 11 effect [75].…”