Anti-Inflammatory Activity of Oleanolic Acid by Inhibition of Secretory Phospholipase A₂

Abstract

Oleanolic acid, a triterpenoid known for its anti-inflammatory properties, is commonly present in several medicinal plants. The present study evaluated the effect of oleanolic acid on sPLA (2), a key enzyme in inflammatory reactions. Oleanolic acid inhibited sPLA (2) activities of human synovial fluid (HSF), human pleural fluid (HPF) and VIPERA RUSSELLI (VRV-PL-V) and NAJA NAJA (NN-PL-I) snake venoms in a concentration-dependent manner. The IC (50) values of sPLA (2) from these sources ranged from 3.08 to 7.78 muM. Increasing calcium (Ca (2+)) concentrations from 2.5 to 15 mM and substrate concentration up to 180 nM did not affect the level of inhibition. Oleanolic acid enhanced the relative intrinsic fluorescence intensity of sPLA (2) (VRV-PL-V). In the presence of oleanolic acid, an apparent shift in the far UV-CD spectrum of sPLA (2) was observed. These studies indicate direct interaction with the enzyme and formation of an sPLA (2)-oleanolic acid complex. The complex formed resulted in irreversible inhibition of sPLA (2). Oleanolic acid inhibited indirect hemolytic activity and mouse paw edema induced by sPLA (2). Inhibition of IN VITRO and IN VIVO sPLA (2) activity by oleanolic acid explains the observed anti-inflammatory properties of several oleanolic acid-containing medicinal plants.

Anti-Inflammatory and Membrane-Stabilizing Properties of Two Semisynthetic Derivatives of Oleanolic Acid

“…Indeed, OA has been shown to inhibit the hyperpermeability and leukocyte migration from blood vessels into tissues [22,23] which occur in the first phase of inflammation. It is also known to inhibit the activity of phospholipase A [20], the membrane-bound enzyme responsible for releasing arachidonic acid from membranebound phospholipids. The current study showed that both derivatives of OA suppressed the early and later phases of albumin-and serotonin-induced inflammation.…”

“…OA and its two semisynthetic derivatives inhibited both the early and late phases of albumin-/serotonin-induced inflammation. Indeed, steroid-like compounds have been shown to inhibited both the early and later phases of inflammation [20]. In his review on the pharmacological properties of oleanolic acid, Liu, 1995 [21] discussed the inhibitory effects of oleanolic acid on histamine and serotonin secretion during inflammation.…”

Antimicrobial Activity of Oleanolic Acid for Foodborne Bacteria

“…Oleanolic acid는 pentacyclic triterpene으로 유리산이나 triterpenoid saponin의 아글리콘 형태로 자연계에 흔히 존 재하면서 3) , 항산화 11,12) , 염증반응 억제 13) , 간 보호 14) , 위 보 호 15) , 암세포에 대한 독성 16) , 항 궤양 17) , 항고지혈증 18) 등 에 대한 생리활성을 가지고 있다 [19][20][21] . , 특히 정향 잎(Syzygium aromaticum; 1.65 g/100 g 건조중량) 24) , 올리브 잎(Olea europaea; 3.1 g/100 g 건조중량) [25][26][27] , 로즈마리 잎(Rosmarinus officinalis; 1.23/100 g 건조중량) [28][29][30] 등에서 추출 된다.…”

Biotransformation using Mucor rouxii for the production of oleanolic acid derivatives and their antimicrobial activity against oral pathogens

“…1) is a pentacyclic triterpene widespread in the plant kingdom in the form of free acid or aglycone for triterpenoid saponins [27]. It is reported to possess interesting bioactivities including anti-inXammatory [10], hepatoprotective [23], antitumor [21], antiviral [29], and antimicrobial activities [19]. Previous studies from our laboratory and others have shown that oleanolic acid and its derivatives display antibacterial activity against oral pathogens [8,31,34].…”