Anti-inflammatory, analgesic and antipyretic activities of Physalis minima Linn

In our present investigation, the crude methanol extract and chloroform fraction of the whole plant of Physalis minima Linn (Solanaceae) was investigated for anti-inflammatory, analgesic and antipyretic activities in NMRI mice and Wistar rats of either sex at 200 and 400 mg/kg, respectively. Various established in-vivo model's were used during the study. Both crude extract and chloroform fraction showed marked anti-inflammatory and analgesic activities as compared to a control at tested doses. The antipyretic potential of the crude extract and chloroform were insignificant in the Brewer's yeast fever model. Therefore, the whole plant of Physalis minima Linn could be considered as a potential candidate for bioactivity-guided isolation of natural anti-inflammatory and analgesic agents.     

Anti-inflammatory,analgesic and antipyretic activities of Physalis minima Linn

In our present investigation, the crude methanol extract and chloroform fraction of the whole plant of Physalis minima Linn (Solanaceae) was investigated for anti-inflammatory, analgesic and antipyretic activities in NMRI mice and Wistar rats of either sex at 200 and 400 mg/kg, respectively. Various established in-vivo model's were used during the study. Both crude extract and chloroform fraction showed marked anti-inflammatory and analgesic activities as compared to a control at tested doses. The antipyretic potential of the crude extract and chloroform were insignificant in the Brewer's yeast fever model. Therefore, the whole plant of Physalis minima Linn could be considered as a potential candidate for bioactivity-guided isolation of natural anti-inflammatory and analgesic agents.     

枸杞多糖的抗炎镇痛作用研究

为研究枸杞多糖的抗炎镇痛效应及其潜在分子机制,采用小鼠热板实验、小鼠福尔马林炎症疼痛模型和原代培养的背根神经节神经元细胞对疼痛指标和炎症相关分子进行了检测。实验结果显示枸杞多糖能显著缓解后足注射福尔马林引起的动物II相痛表现(P <0. 05),减少动物两后足重量差值(P <0. 001)和血液(P <0. 001)、脊髓(P <0. 05)组织中白细胞介素6的含量,而对小鼠热板潜伏期无明显影响;枸杞多糖降低原代培养的DRG细胞膜上TRPV1介导的钙信号(P <0. 05)。结果证明枸杞多糖具有良好的抗炎镇痛作用,其镇痛机制可能与降低炎症因子白细胞介素6表达及其引起的TRPV1活性增加有关。     

Anti-inflammatory and analgesic activity of Indian Hypericum perforatum L

A standardised 50% aqueous ethanolic extract of the Indian variety of Hypericum perforatum (IHp) was examined for its putative anti-inflammatory and analgesic activity at the doses of 100 and 200 mg/kg, po. The experimental paradigms used were carrageenan induced pedal edema and cotton pellet induced granuloma for anti-inflammatory activity, whereas the tail flick, hot plate and acetic acid induced writhing methods were used to asses analgesic activity. Indomethacin (20 mg/kg, ip) was used as the standard anti-inflammatory drug. Pentazocine (10 mg/kg, ip) and aspirin (25 mg/kg, ip), both clinically used analgesics, were used as standard analgesics for comparison. IHp extract showed significant anti-inflammatory and analgesic activity at both dose levels, in all the paradigms used. Additionally, IHp potentiated the anti-inflammatory activity of indomethacin and analgesic activities of pentazocine and aspirin.     

Synthesis, anti-inflammatory, analgesic and antioxidant activities of some tetrasubstituted thiophenes

Sets of tetrasubstituted thiophene esters 4a-4g, 5a-5f and 6a-6e were synthesized by reaction of 1-(alpha-Carbomethoxy-beta-aminothiocrotonoyl)-aryl/aroyl amines (3) with 3-(bromoacetyl)coumarin, 1,4-dibromodiacetyl and chloroacetone respectively. The compound 3 were synthesized by nucleophilic addition of aryl/aroylisothiocyanate and enamine (2). The synthesized targeted compounds (4a-4g, 5a-5f and 6a-6e) were evaluated for their in vivo anti-inflammatory activity in carrageenin-induced rat hind paw oedema model at three graded doses employed at 10, 20 and 40 mg/kg body weight using mefanamic acid, ibuprofen and in vivo analgesic activity in acetic acid induced writhing response model at 10 mg/kg dose using ibuprofen as standard drug. The compounds 4a-4f, 5c, 5f, 6c and 6e were evaluated for their in vitro antioxidant nitric oxide radical scavenging assay at the concentrations of 5, 10, 15, 20, 25, 30 and 35 microg/mL using ascorbic acid as standard drug. Among all the targeted compounds 4c showed maximum anti-inflammatory activity of 71% protection at 10 mg/kg and 77% protection at 20 mg/kg to inflamed paw and analgesic activity of 56% inhibition and also maximum in vitro nitric oxide radical scavenging activity having IC(50) value 31.59 microg/mL.     

Synthesis,anti-inflammatory,analgesic and antioxidant activities of some tetrasubstituted thiophenes

Sets of tetrasubstituted thiophene esters 4a-4g, 5a-5f and 6a-6e were synthesized by reaction of 1-(α-Carbomethoxy-β-aminothiocrotonoyl)-aryl/aroyl amines (3) with 3-(bromoacetyl)coumarin, 1,4-dibromodiacetyl and chloroacetone respectively. The compound 3 were synthesized by nucleophilic addition of aryl/aroylisothiocyanate and enamine (2). The synthesized targeted compounds (4a-4g, 5a-5f and 6a-6e) were evaluated for their in vivo anti-inflammatory activity in carrageenin-induced rat hind paw oedema model at three graded doses employed at 10, 20 and 40 mg/kg body weight using mefanamic acid, ibuprofen and in vivo analgesic activity in acetic acid induced writhing response model at 10 mg/kg dose using ibuprofen as standard drug. The compounds 4a-4f, 5c, 5f, 6c and 6e were evaluated for their in vitro antioxidant nitric oxide radical scavenging assay at the concentrations of 5, 10, 15, 20, 25, 30 and 35 μg/mL using ascorbic acid as standard drug. Among all the targeted compounds 4c showed maximum anti-inflammatory activity of 71% protection at 10 mg/kg and 77% protection at 20 mg/kg to inflamed paw and analgesic activity of 56% inhibition and also maximum in vitro nitric oxide radical scavenging activity having IC₅₀ value 31.59 μg/mL.     

Anti-inflammatory,antioxidant, anti-cholinesterase activity and mutagenicity of South African medicinal orchids

While the role of various processes in inflammatory-related degenerative disorders is still being researched, many avenues of research have concentrated on the treatment and/or prevention of these disorders. Inflammatory-responses, the cholinergic system and oxidative stress have often been linked to the symptoms prevalent in aged persons and Alzheimer's patients. The current research explored the selective inhibition of cyclooxygenase (COX) enzymes, antioxidant and anti-cholinesterase activities of selected South African orchid extracts, currently traded in herbal markets along the east coast of South Africa. Out of a total of 53 evaluated extracts, significant anti-inflammatory activity was observed in nearly 40% of extracts in the COX-1 assay and 25% of extracts in the COX-2 assay. Overall, the DCM root extract of Ansellia africana was the most potent, the DCM tuber extract of Eulophia hereroensis was the only extract to significantly inhibit both COX enzymes, while all Bulbophyllum scaberulum organic root extracts exhibited COX-2 selective inhibitory activity. Bulbophyllum scaberulum DCM root extract was also the most effective anti-cholinesterase extract, performing better than galanthamine. In the single electron transfer (SET) (2,2′-diphenylpicrylhydrazyl (DPPH) free radical scavenging assay and ferric reducing antioxidant power (FRAP) reaction based assays, E. petersii pseudobulb and A. africana root extracts performed better than other extracts. In the hydrogen atom transfer (HAT) (β-carotene/linoleic acid assay) reaction-based assay, the leaf extract of Tridactyle tridentata and root extracts of Cyrtorchis arcuata and E. hereroensis exhibited the best antioxidant effects. The mutagenicity (Salmonella/microsome assay) was also determined. Organic leaf and root extracts of C. arcuata produced no genotoxic effects in comparison to the other tested species. None of the crude extracts tested demonstrated mutagenic effects using S. typhimurium strain TA98 with metabolic activation. The results obtained in this study validate the use of certain orchid species in South African traditional medicine for inflammation-related degenerative disorders.     

Anti-inflammatory and antioxidant effects of Croton celtidifolius bark.

Croton celtidifolius Baill commonly known as "sangue-de-adave" is a tree found in the Atlantic Forest of south of Brazil, mainly in Santa Catarina. The bark and leaf infusions of this medicinal plant have been popularly used for the treatment of inflammatory diseases. In this study we evaluated the anti-inflammatory and antioxidant properties of crude extract (CE), aqueous fraction (AqF), ethyl acetate fraction (EAF), butanolic fraction (BuF) and catechin, gallocatechin and sub-fractions, 19SF, 35SF and 63SF that contained a mixture of proanthocyanidins and were derived from the EAF fraction. The CE, AqF, EAF, BuF, catechin and sub-fractions 35SF and 63SF reduced paw edema induced by carrageenan. The CE, fractions, sub-fractions and isolated compounds showed antioxidant properties in vitro, all were able to scavenge superoxide anions at a concentration of 100 microg ml(-1). The EAF, catechin and gallocatechin were most effective in the deoxyribose assay, IC50 0.69 (0.44-1.06), 0.20 (0.11-0.39), 0.55 (0.28-1.08) microg x ml(-1) respectively. The CE and other fractions and sub-fractions inhibited deoxyribose degradation up to 1 microg x ml(-1). In the hydrophobic system only AqF did not show lipid peroxidation inhibition. The CE, other fractions, sub-fractions and isolated compounds inhibited lipidid peroxidation only at a concentration of 100 microg x ml(-1). In summary, this study demonstrates that Croton celtidifolius bark has significant anti-inflammatory and antioxidant activity.     

Anti-inflammatory, antioxidant and antimicrobial activity of Ophthacare brand, an herbal eye drops.

In the present study, the herbal preparation of Ophthacare brand eye drops was investigated for its anti-inflammatory, antioxidant and antimicrobial activity, using in vivo and in vitro experimental models. Ophthacare brand eye drops exhibited significant anti-inflammatory activity in turpentine liniment-induced ocular inflammation in rabbits. The preparation dose-dependently inhibited ferric chloride-induced lipid peroxidation in vitro and also showed significant antibacterial activity against Escherichia coli and Staphylococcus aureus and antifungal activity against Candida albicans. All these findings suggest that Ophthacare brand eye drops can be used in the treatment of various ophthalmic disorders.     

Anti-inflammatory and analgesic activities of SKLJI, a highly purified and injectable herbal extract of Lonicera japonica

The parenteral route has many merits over the oral route, including greater predictability, reproducibility of absorption, and rapid drug action, but injectable phytomedicines are uncommon due to protein precipitating tannin and hemolytic saponin components. In this study, in an effort to develop a safe injectable analgesic phytomedicine, we prepared a tannin and saponin-free Lonicera japonica extract, SKLJI, through fractionation and column purification, and evaluated its anti-inflammatory and analgesic activities in in vivo experimental models of inflammation and pain. The removal of tannin and saponin resulted in loganin and sweroside-enriched SKLJI and it showed reduced hemolysis and protein precipitation. In efficacy tests, SKLJI inhibited croton oil- and arachidonic acid-induced ear edema, acetic acid-induced writhing, and carrageenan-induced rat hind paw hyperalgesia. Inhibition of cylcooxygenase-2 (COX-2), inducible nitric oxide synthase (iNOS), and 5-lipoxyfenase (5-LO) activities by SKLJI appeared to be the mechanism underlying anti-inflammatory and analgesic efficacy. Loganin and sweroside also showed anti-inflammatory and analgesic activities, suggesting that they might be active principles in the efficacy of SKLJI. These results suggest that SKLJI is a viable candidate for a new anti-inflammatory and analgesic phytomedicine that can be administered by the parenteral route.     

Anti-inflammatory, antiarthritic and analgesic activity of a herbal formulation (DRF/AY/4012)

Anti-inflammatory, antiarthritic and analgesic effect of a herbal product (DRF/AY/4012) was evaluated in animal models. Herbal product treatment induced a dose dependent anti-inflammatory activity in acute inflammatory models (carrageenin and egg-albumin induced rat hind paw edema). It also elicited promising anti-inflammatory activity in chronic inflammatory models (cotton pellet granuloma and Freund's adjuvant induced polyarthritis in rats). Further, the product inhibited the increased level of serum lysosomal enzyme activity viz. serum glutamic oxaloacetic transaminase, serum glutamic pyruvic transaminase, alkaline phosphatase and the lipid peroxidation in liver. In Freund's adjuvant induced polyarthritis, herbal product reduced the increased level of hydroxy proline, hexosamine and total protein content in edematous tissue. The product also exhibited mild to moderate analgesic activity in acetic acid induced writhing in mice. The LD50 value of the herbal product was more than 16 gm/kg by oral route in mice. The product has distinct advantages over the existing agents and deserves further developmental studies.     

Design,synthesis of novel isoindoline hybrids as COX-2 inhibitors: Anti-inflammatory,analgesic activities and docking study

A group of novel isoindoline hybrids incorporating oxime, hydrazone, pyrazole, chalcone or aminosulfonyl pharmacophores (9–14) was designed and characterized by spectral data and elemental analyses results. All newly synthesized compounds were evaluated as COX-2 inhibitors, anti-inflammatory and analgesic agents. Six hybrid derivatives (10b, 10c, 11a, 11d, 13, 14) were moderate COX-2 inhibitors (IC₅₀ = 0.11–0.18 µM) close to standard celecoxib (IC₅₀ = 0.09 µM). The most active compounds showed outstanding in vivo anti-inflammatory activity (% edema inhibition = 41.7–50, 1 h; 40.7–67.4, 3 h; 20–46.7, 6 h) better than reference drug diclofenac (% edema inhibition = 29.2, 1 h; 22.2, 3 h; 20, 6 h). Most compounds showed significant peripheral and/or central analgesic activity. The moderate selective COX-2 inhibitor; dimethoxychalcone 11d (SI = 103) displayed excellent anti-inflammatory activity (% edema inhibition = 45.8–59.3) and increased thermal pain threshold (50–92.85%) comparable to piroxicam (75%). Molecular docking studies have been established.     

Anti-inflammatory,antioxidant and antihepatotoxic effects of Spirulina platensis against d-galactosamine induced hepatotoxicity in rats

Spirulina platensis has been advocated as safe food for human use by several investigators. In this study its beneficial dietary effect against liver injuries caused by d-galactosamine (d-GalN) was studied ensuring safety to human health using animal model. Acute hepatotoxicity was induced in Wister rats with d-GalN followed by treatment with butylated hydroxytoluene (BHT) and with Spirulina aqueous extract at various concentrations. The effect of Spirulina at different concentrations were tried and compared with BHT treatment. The animals treated with d-GalN on subsequent treatment by supplementation with Spirulina (6, 9%) in the diets, led to significant reversal in the levels of the antioxidant enzymes through hepatocytes by suppression of negative effect. Spirulina aqueous extract at 9% resulted in a significant decrease in the levels of alkaline phosphatase and infalmatory markers TNFα, IL6 and IL1β and also decreased TBARS, while it showed an increase in oxidative stress marker such as GR, GSH, GST, SOD, GPX and CAT and total protein when compared to the levels recorded with that group treated with d-GalN. Results also indicated that Spirulina aqueous extract at 9% concentration was equally effective in protecting liver damage as it was observed with BHT. Histological studies on liver treated with d-GalN, BHT and Spirulina aqueous extract showed that S. platensis is effective as diet in providing beneficial protective effect. The results obtained in the present study very clearly indicated the positive beneficial protective effect of Spirulina, when used as diet, on the safety and protection of liver from injuries caused by toxicants.     

Anti-inflammatory and antioxidant activity of a medicinal tincture from Pedilanthus tithymaloides

Pedilanthus tithymaloides (L.) Poit. (Euphorbiaceae) is a low tropical American shrub with a reported wide range of healing properties such as emetic, anti-inflammatory, antibiotic, antiseptic, antihemorrhagic, antiviral, antitumoral, and abortive. In the present study, a tincture from P. tithymaloides collected in Cuba was evaluated for its in vivo anti-inflammatory activity, using the rat paw oedema assay, and for its in vitro scavenging effects on reactive oxygen species (ROS) (HO*, O2*-, HOCl, ROO* and H2O2), reactive nitrogen species (RNS) (ONOO- and *NO), and DPPH* radical. The protein, free amino acid, and phenolic contents of the tincture were also determined. Pertaining to the anti-inflammatory activity, the intraperitoneal administration of the tincture inhibited carrageenan-induced rat paw oedema, whereas in the scavenging assays the tincture showed to be effective against all the assayed ROS and RNS, specially for HO* (IC50 = 345+/-77 microg/mL), O2*- (IC50 = 143+/-7 microg/mL), HOCl (IC50 = 113+/-20 microg/mL), ONOO- (IC50 = 44+/-3 microg/mL), and *NO (IC50 = 54+/-4 microg/mL), but displayed weak activity in the DPPH* assay. The protein content of the tincture was 0.70%, and twenty free amino acids were identified and quantified. The content of total phenolics was 17.4+/-0.15 mg of gallic acid equivalents (GAE)/g dry material. These results provide scientific support for the empirical use of P. tithymaloides tincture as an anti-inflammatory medicine.     

Anti-inflammatory, analgesic and antipyretic activities of Linum usitatissimum L. (flaxseed/linseed) fixed oil

The fixed oil of L. usitatissimum (flaxseed/linseed) inhibited PGE2-, leukotriene-, histamine- and bradykinin-induced inflammation. The oil also inhibited arachidonic acid-induced inflammation, suggesting its capacity to inhibit both cyclooxygenase and lipoxygenase pathways of arachidonate metabolism. In tail immersion model, the oil raised the pain threshold to a lesser extent than morphine but showed excellent peripherally acting, analgesic activity comparable to aspirin, against acetic acid-induced writhing in mouse. In typhoid paratyphoid A/B vaccine-induced pyrexia, the oil showed antipyretic activity comparable to aspirin. The oil contains 57.38% alpha-linolenic acid. Dual inhibition of arachidonic acid metabolism, antihistaminic and antibradykinin activities of the oil could account for the biological activity and the active principle could be alpha-linolenic acid an omega-3 (18:3, n-3) fatty acid.     

Anti-inflammatory,anti-apoptotic,and antioxidant actions of Middle Eastern Phoenix dactylifera extract on mercury-induced hepatotoxicity in vivo

Molecular Biology Reports - Mercuric chloride (MC) is a complex substance which is capable to produce free radicals. Middle Eastern Phoenix dactylifera (MEPD) is a flowering plant of palm family...     

Anti-inflammatory and antioxidant activities of Sargassum horneri extract in RAW264.7 macrophages

[Purpose]In this study, we investigated whether a 70% ethanolic (EtOH) extract of Sargassum horneri had antioxidant and anti-inflammatory effects in lipopolysaccharide (LPS)-stimulated macrophage-like RAW 264.7 cells.[Methods]The proximate composition, fatty acids, amino acids, and dietary fiber of S. horneri, various biologically active compounds, and antioxidant activity were analyzed.[Results]The DPPH and ABTS free radical scavenging activities, as well as the reduction power, of the S. horneri extract used here were significantly increased in a concentration-dependent manner. This indicates that S. horneri contains bioactive compounds, such as phenols and flavonoids, that have excellent antioxidant activity. The cellular viability and metabolic activity results confirmed that the extract had no discernible toxicity at concentrations up to 100 μg/mL. The levels of nitrites and cytokines (PGE₂, TNF-α and IL-6), which mediate pro-inflammatory effect, were significantly inhibited by treatment with either 50 or 100 μg/mL S. horneri extract, whereas that of IL-1β was significantly inhibited by treatment with 100 μg/mL of the extract. Similarly, the expression of iNOS and COX-2 proteins also decreased according to 50 or 100 μg/mL extract concentrations. NF-κB binding to DNA was also significantly inhibited by treatment with 100 μg/mL of extract.[Conclusion]These results suggest that 70% EtOH extracts of S. horneri can relieve inflammation caused by disease or high intensity exercise.     

Anti-inflammatory and antioxidant activity of coumarins designed as potential fluorescent zinc sensors

A series of coumarin analogs, designed and synthesised as potential fluorescent zinc probes were evaluated for their biological activity as anti-inflammatory and antioxidant agents. The effect of the synthesised compounds on inflammation, using the carrageenin-induced rat paw oedema model, was studied. In general, the compounds were found to be potent anti-inflammatory agents (26.5-64%). Compound 5 was found to interact significantly with 1,1-diphenyl-2-picryl-hydrazyl stable free radical (DPPH) whereas the remainder were inactive in this assay. The compounds inhibit in general the soybean lipoxygenase and scavenge superoxide anion radicals. The anti-inflammatory activity seems to be connected with their reducing activity. Their RM values were determined as an expression of their lipophilicity. Theoretical calculations of their lipophilicity as clog P were performed indicating that only a poor relationship exists between their lipophilicity and anti-inflammatory activity.     

Anti-inflammatory and analgesic effects and molecular mechanisms of JCICM-6, a purified extract derived from an anti-arthritic Chinese herbal formula

The anti-inflammatory and anti-nociceptive effects and the molecular mechanisms of JCICM-6, a purified extract derived from an anti-arthritic Chinese herbal formula composed of Caulis Sinomenii, Aconiti laterralis Preparata, Rhizoma Curcumae longae, Radix Paeoniae albae, and Cortex Moutan, were examined for the first time. JCICM-6 was prepared using pharmaceutical extraction technology, purified by Amberlite XAD-7HP polymeric resin. Pharmacologically, in carrageenan-induced edema and carrageenan-evoked thermal hyperalgesia in paws of rats, the oral administration of JCICM-6 at dosages of 0.4, 0.8, and 1.6 g/kg demonstrated significant inhibition with a dose-dependent manner. Mechanistic studies showed that JCICM-6 effectively decreased the production of the pro-inflammatory cytokines of IL-6 and IL-1β and expression of COX-2 and iNOS proteins, and simultaneously elevated the level of anti-inflammatory cytokine IL-4 in the carrageenan-injected rat paw tissues and exudates. The positive reference drug, indomethacin at a dosage of 10 mg/kg, demonstrated inhibitory potency in both rat models, but it could not augment the production of IL-4, indicating JCICM-6 and indomethacin might possess different pharmacological properties and molecular mechanisms although both have anti-inflammatory and analgesic effects in rats. These results suggest that JCICM-6 would be a valuable candidate for further investigation as a new anti-arthritic drug.