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1.
Antioxidants (Basel) ; 11(7)2022 Jun 25.
Article in English | MEDLINE | ID: mdl-35883742

ABSTRACT

Human Group IIA secreted phospholipase A2 (sPLA2-IIA) enzyme plays a crucial role in several chronic inflammatory diseases such asasthma, atherosclerosis, gout, bronchitis, etc. Several studies showed that the antioxidants exert an anti-inflammatory function by inhibiting the sPLA2-IIA enzyme. Hence, the present study evaluated an antioxidant molecule, sinapic acid, for sPLA2-IIA inhibition as an anti-inflammatory function. Initially, the antioxidant efficacy of sinapic acid was evaluated, and it showed greater antioxidant potency. Further, sinapic acid inhibited 94.4 ± 4.83% of sPLA2-IIA activity with an IC50 value of 4.16 ± 0.13 µM. The mode of sPLA2-IIA inhibition was examined by increasing the substrate concentration from 30 to 120nM and the calcium concentration from 2.5 to 15 mM, which did not change the level of inhibition. Further, sinapic acid altered the intrinsic fluorescence and distorted the far UltraViolet Circular Dichroism (UV-CD) spectra of the sPLA2-IIA, indicating the direct enzyme-inhibitor interaction. Sinapic acid reduced the sPLA2-IIA mediated hemolytic activity from 94 ± 2.19% to 12.35 ± 2.57% and mouse paw edema from 171.75 ± 2.2% to 114.8 ± 1.98%, demonstrating the anti-inflammatory efficiency of sinapic acid by in situ and in vivo methods, respectively. Finally, sinapic acid reduced the hemorrhagic effect of Vipera russelli venom hemorrhagic complex-I (VR-HC-I) as an anti-hemorrhagic function. Thus, the above experimental results revealed the sinapic acid potency to be an antioxidant, anti-inflammatory and anti-hemorrhagic molecule, and therefore, it appears to be a promising therapeutic agent.

2.
Article in English | MEDLINE | ID: mdl-25515170

ABSTRACT

OBJECTIVE: Investigation of the pharmacological potential of Tetrahydrofurano/pyrano quinoline and Benzo [b]furoindolyl derivatives in acute inflammation, pain and oxidative stress. METHODS: Tetrahydrofurano/ pyrano quinoline and Benzo[b]furoindolyl were evaluated for anti-inflammatory activity by carrageenan-induced hind paw edema in rats. Analgesic activity in mice was assessed by both peripheral and central analgesic models. The free radical scavenging activity of the synthetic compound was analyzed by the in vivo antioxidant assays, by measuring the antioxidant enzymes such as Superoxide dismutase (SOD), Catalase and Peroxidase from the liver homogenate and the in vitro antioxidant activity was evaluated by DPPH photometric assay, Hydroxyl radical scavenging and Lipid Peroxidation assay. RESULTS: The compounds had substantially inhibited the inflammation induced by subcutaneous carrageenan injection. The same compounds had demonstrated remarkable central and peripheral analgesic activity with potent free radical scavenging activity as evident from both in vitro and in vivo antioxidant assays. CONCLUSION: Tetrahydrofurano/pyrano quinoline and Benzo[b]furoindolyl derivatives exhibit varied pharmacological activities that include anti-inflammatory, analgesic and antioxidant activity.


Subject(s)
Analgesics/pharmacology , Anti-Inflammatory Agents/pharmacology , Antioxidants/pharmacology , Benzofurans/pharmacology , Edema/prevention & control , Furans/pharmacology , Indoles/pharmacology , Oxidative Stress/drug effects , Pain/prevention & control , Quinolines/pharmacology , Analgesics/chemical synthesis , Animals , Anti-Inflammatory Agents/chemical synthesis , Antioxidants/chemical synthesis , Antioxidants/metabolism , Benzofurans/chemical synthesis , Carbon Tetrachloride , Carrageenan , Chemical and Drug Induced Liver Injury/etiology , Chemical and Drug Induced Liver Injury/metabolism , Chemical and Drug Induced Liver Injury/prevention & control , Disease Models, Animal , Drug Design , Edema/chemically induced , Furans/chemical synthesis , Indoles/chemical synthesis , Lipid Peroxidation/drug effects , Liver/drug effects , Liver/metabolism , Mice , Pain/etiology , Quinolines/chemical synthesis , Rats
3.
Anc Sci Life ; 35(2): 70-8, 2015.
Article in English | MEDLINE | ID: mdl-26865738

ABSTRACT

BACKGROUND: Polyalthia cerasoides is a medicinal plant known for its ethnopharmacological importance. Despite this, investigation related to its therapeutic benefit is still unexplored. AIM: To evaluate the stem bark extracts of Polyalthia cerasoides for pharmacological activities relating to inflammation, nociception and oxidative stress using in vivo and in vitro models. MATERIALS AND METHODS: Pet ether, ethyl acetate and chloroform fractions of the stem bark were evaluated for anti-inflammatory activity by carrageenan-induced hind paw edema in rats. Anti-nociceptive activity in mice was assessed using thermally and chemically induced analgesic models. The free radical quenching potential of the extracts was initially analyzed using the in vitro DPPH photometric assay, Hydroxyl radical scavenging and Lipid Peroxidation assays. Then modulatory effect of the extracts on in vivo antioxidant system was evaluated by carbon tetrachloride induced hepatotoxicity and subsequent measurements of antioxidant enzymes such as Superoxide dismutase, Catalase and Peroxidase from the liver homogenate. RESULTS: Among the tested fractions, ethyl acetate extract had substantially inhibited the inflammation by 68.5% that was induced by subcutaneous carrageenan injection whereas pet ether and chloroform extract showed only minimal inhibitory effect. Investigation of the anti-nociceptive activity revealed that the ethyl acetate fractions had significantly repressed the algesia in both the analgesic experimental models. In vitro and in vivo individual antioxidant assays demonstrated that the ethyl acetate fraction has strong free radical quenching potential which also restores the endogenous hepatic enzymes. CONCLUSION: The ethyl acetate fraction enriched with flavinoids and steroids from Polyalthia cerasoides stem bark has potent bioactivity to combat inflammation, ROS and pain. This needs further characterization for potential therapeutic applications.

4.
Inflammopharmacology ; 18(1): 25-31, 2010 Feb.
Article in English | MEDLINE | ID: mdl-19894024

ABSTRACT

OBJECTIVES: Some of the legumes, spices and medicinal herbs rich in genistein are known for their anti-inflammatory properties. Anti-inflammatory property of these herbs is determined by subjecting secretory phospholipase A(2) (sPLA(2)) inhibition, a key enzyme in the inflammatory reactions by genistein. MATERIALS AND METHODS: Genistein was assessed for inhibition of sPLA(2) activity using (14)C-oleate radiolabelled Escherichia coli membrane as substrate. The enzyme-inhibitor interaction was established by intrinsic fluorescence and circular dichroism studies. The in vivo anti-inflammatory activity was tested by injecting sPLA(2), Vipera russelli venom phospholipase-V (VRV-PL-V) with different concentrations of genistein in the range of 3-21 muM into intra plantar surface of right hind footpad of mice. Systemic effect was tested by administering the genistein (21 muM) i.p. 30 min before and immediately after sPLA(2) injection. RESULT: Genistein inhibited sPLA(2) enzymes of inflammatory exudates (human synovial fluid and human pleural fluid) and snake venoms (VRV-PL-V and Naja naja phospholipase-I) in a concentration dependent manner with IC(50) values ranging from 5.75 to 11.75 muM. Increasing the calcium (Ca(2+)) concentration from 2.5 to 15 mM and substrate concentration up to 120 nM did not alter the level of inhibition. Genistein alters the intrinsic fluorescence intensity and shown apparent shift in far ultra violet-circular dichroism spectra of VRV-PL-V, indicating the direct interaction with enzyme. Genistein also inhibited the VRV-PL-V induced mouse paw oedema in a concentration dependent manner. The genistein at 21 muM concentration administered immediately after the VRV-PL-V injection, effectively neutralized the oedema inducing activity. CONCLUSION: Genistein inhibited sPLA(2) activity of both inflammatory exudates and snake venoms in a concentration dependent manner and sPLA(2) induced mouse paw oedema. The study partially explains the observed anti-inflammatory property of several medicinal herbs which containing genistein.


Subject(s)
Down-Regulation/physiology , Genistein/pharmacology , Inflammation Mediators/pharmacology , Phospholipases A2, Secretory/antagonists & inhibitors , Protein Kinase Inhibitors/pharmacology , Animals , Dose-Response Relationship, Drug , Down-Regulation/drug effects , Genistein/therapeutic use , Humans , Inflammation/drug therapy , Inflammation/enzymology , Inflammation Mediators/therapeutic use , Mice , Phospholipases A2, Secretory/metabolism , Protein Kinase Inhibitors/therapeutic use , Snake Venoms/antagonists & inhibitors , Snake Venoms/enzymology
5.
Planta Med ; 75(3): 211-5, 2009 Feb.
Article in English | MEDLINE | ID: mdl-19085684

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.


Subject(s)
Anti-Inflammatory Agents/pharmacology , Inflammation/drug therapy , Oleanolic Acid/pharmacology , Phospholipases A2, Secretory/antagonists & inhibitors , Plant Extracts/pharmacology , Synovial Fluid/drug effects , Animals , Anti-Inflammatory Agents/therapeutic use , Calcium/pharmacology , Dose-Response Relationship, Drug , Edema/drug therapy , Hemolysis/drug effects , Humans , Mice , Oleanolic Acid/pharmacokinetics , Oleanolic Acid/therapeutic use , Plant Extracts/pharmacokinetics , Plant Extracts/therapeutic use , Pleura/drug effects , Snake Venoms/enzymology
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