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1.
Pak J Pharm Sci ; 34(5(Supplementary)): 1897-1902, 2021 Sep.
Article in English | MEDLINE | ID: mdl-34836857

ABSTRACT

Eruca sativa, member of family Brassicaceae, was evaluated for its anti-arthritic potential. Both in vitro and in vivo models were used to bring out a safe, effective and economical remedy. In vitro tests included egg albumin denaturation suppression, bovine serum albumin assay and human red blood cells maintenance assay. While in vivo formaldehyde-induced arthritic model was initiated to check effect on paw volume. Similarly, carrageenan produced inflammation was applied to check anti-inflammatory ability of the plant. Acute toxicity studies showed safety margin at 2000mg/kg. The plant showed concentration dependent denaturation protection and membrane stability in vitro assays. Likewise, the carrageenan and formaldehyde investigations revealed visible paw volume reduction in dose attributed manner, with maximum outcome at dose of 500mg/kg. Hence, it may be established on the ground of presented results that ethyl-acetate extract of Eruca sativa has significant anti-inflammatory and anti-arthritic effects and may be considered for further research to reveal the core mechanism.


Subject(s)
Arthritis, Rheumatoid/drug therapy , Fabaceae/chemistry , Inflammation/drug therapy , Plant Extracts/therapeutic use , Acetates , Animals , Anti-Inflammatory Agents/pharmacology , Arthritis, Experimental/drug therapy , Arthritis, Rheumatoid/chemically induced , Carrageenan , Dose-Response Relationship, Drug , Female , Formaldehyde , Humans , Inflammation/chemically induced , Male , Rats , Rats, Sprague-Dawley , Solvents
2.
Int J Biol Macromol ; 166: 483-495, 2021 Jan 01.
Article in English | MEDLINE | ID: mdl-33130262

ABSTRACT

Herein, we report co-encapsulation of ofloxacin with tea tree or lavender oil in gellan gum based hydrogel films by solvent casting ionotropic gelation method as wound dressing. Prepared films were transparent, flexible, and displayed antioxidant activity with superior antibacterial response against common inhabitants of wound i.e. gram positive and negative bacteria. Solid-state characterization of optimized formulation (OL3 and OT3) revealed successful incorporation of drug and oils in hydrogel structure without any noticeable interaction. In vitro release studies showed an initial burst release but remaining portion released in controlled manner over 48 h from the films and furthermore, presence of oils did not affected the ofloxacin release. Optimized formulation containing ofloxacin and 25% w/w lavender/tea tree oil showed 98% wound contraction in rats after ten days of treatment. Histological images displayed completely healed epidermis. Taken together, our prepared hydrogel films demonstrated favorable features with appreciable antibacterial, wound healing activity and could be useful for the treatment of full thickness wounds.


Subject(s)
Methylgalactosides/chemistry , Ofloxacin/pharmacology , Oils, Volatile/pharmacology , Plant Oils/pharmacology , Polysaccharides, Bacterial/chemistry , Tea Tree Oil/pharmacology , Wound Healing/drug effects , Animals , Antioxidants/pharmacology , Calorimetry, Differential Scanning , Drug Liberation , Escherichia coli/drug effects , Kinetics , Lavandula , Microbial Sensitivity Tests , Rats , Spectroscopy, Fourier Transform Infrared , Staphylococcus aureus/drug effects , Thermogravimetry , X-Ray Diffraction
3.
Nat Prod Res ; 35(17): 2982-2986, 2021 Sep.
Article in English | MEDLINE | ID: mdl-31674843

ABSTRACT

The present study aims at phytochemical profiling and valuating the effect of crude extract of Delphinium brunonianum on fructose mediated rise in blood pressure and metabolic abnormalities in rats. Therefore, rats were fed on fructose (10%w/v) for 6 weeks. Rats in treatment groups received amlodipine 250, 500 and 1000 mg/kg of DB-Cr separately in concurrent to fructose. Various parameters of metabolic perturbations were assessed at the end of study. Further, DB-Cr was analyzed using LC-MS technique. DB-Cr exerted remarkable antihypertensive effect whereas, sympathetic hyperactivity and hyperinsulinemia in these rats was significantly blunted, further, endothelium functionality was successfully restored. LC-MS analysis of DB-Cr revealed the presence of a variety of chemical constituents (41) including quinic acid, scopolin, gingerol, Robinetin 3-rutinoside, KAPA and maleic acid. In conclusion, D. brunonianum possess the potential to combat the fructose mediated hypertension and metabolic perturbations, which may partially be due to its chemical constituents.


Subject(s)
Delphinium , Hypertension , Phytochemicals/pharmacology , Plant Extracts/pharmacology , Animals , Blood Pressure , Delphinium/chemistry , Fructose , Hypertension/chemically induced , Hypertension/drug therapy , Phytochemicals/chemistry , Rats
4.
J Cardiovasc Pharmacol ; 75(6): 573-583, 2020 06.
Article in English | MEDLINE | ID: mdl-32187164

ABSTRACT

This study investigated the preventive effect of an aqueous extract of the whole plant of Phyllanthus amarus (AEPA) on blood pressure, cardiac, and endothelial function in the deoxycorticosterone acetate (DOCA) salt-induced hypertensive rat model. Male Wistar rats were assigned into 5 groups receiving either vehicle (control and DOCA salt), DOCA salt combined with AEPA at 100 or 300 mg/kg, or AEPA (100 mg/kg) alone for 5 weeks. In addition, DOCA salt-treated rats were allowed free access to water containing 1% NaCl. Systolic blood pressure, left ventricle parameters, vascular reactivity of primary mesenteric artery rings, the vascular level of oxidative stress, and the level of target proteins were determined, using respectively tail-cuff sphygmomanometry, echocardiography, organ chambers, dihydroethidium staining, and immunofluorescence methods. After 5 weeks, AEPA treatments (100 or 300 mg/kg per day) significantly prevented the increase in systolic blood pressure in DOCA salt-treated rats, respectively, by about 24 and 21 mm Hg, improved cardiac diastolic function, and reduced significantly the increased posterior and septum diastolic wall thickness and the left ventricle mass in hypertensive rats. Moreover, the DOCA salt-induced endothelial dysfunction and the blunted nitric oxide- and endothelium-dependent hyperpolarization-mediated relaxations in primary mesenteric artery were improved after the AEPA treatments. AEPA also reduced the level of vascular oxidative stress and the expression level of target proteins (eNOS, COX-2, NADPH oxidase subunit p22) in DOCA salt rats. Altogether, AEPA prevented hypertension, improved cardiac structure and function, and improved endothelial function in DOCA salt rats. Such beneficial effects seem to be related, at least in part, to normalization of the vascular level of oxidative stress.


Subject(s)
Antihypertensive Agents/pharmacology , Blood Pressure/drug effects , Endothelium, Vascular/drug effects , Hypertension/prevention & control , Hypertrophy, Left Ventricular/prevention & control , Phyllanthus , Plant Extracts/pharmacology , Vasodilation/drug effects , Ventricular Function, Left/drug effects , Ventricular Remodeling/drug effects , Animals , Antihypertensive Agents/isolation & purification , Cyclooxygenase 2/metabolism , Desoxycorticosterone Acetate , Disease Models, Animal , Endothelium, Vascular/metabolism , Endothelium, Vascular/physiopathology , Hypertension/chemically induced , Hypertension/metabolism , Hypertension/physiopathology , Hypertrophy, Left Ventricular/chemically induced , Hypertrophy, Left Ventricular/metabolism , Hypertrophy, Left Ventricular/physiopathology , Male , NADPH Oxidases/metabolism , Nitric Oxide Synthase Type III/metabolism , Oxidative Stress/drug effects , Phyllanthus/chemistry , Plant Extracts/isolation & purification , Rats, Wistar , Sodium Chloride, Dietary
5.
Phytomedicine ; 66: 153134, 2020 Jan.
Article in English | MEDLINE | ID: mdl-31812101

ABSTRACT

PURPOSE: Matrix metalloproteinases, zinc dependent proteolytic enzymes, have significant implications in extracellular matrix degradation associated with tissue damage in inflammation and Rheumatoid arthritis. Numerous orchestrated pathways affects instigation and blockade of metalloproteinases as well as various factors that increase the expression of MMPs including inflammatory cytokines, hormones and growth factors. Direct inhibition of these proteolytic enzymes or modulation of these pathways can provide protection against tissue destruction in inflammation and rheumatoid arthritis. Inclination towards use of plant derived phytochemicals to prevent tissue damage has been increasing day by day. Diversity of phytochemicals have been known to directly inhibit metalloproteinases. Hence, thorough knowledge of phytochemicals is very important in novel drug discovery. METHODS: Present communication evaluates various classes of phytochemicals, in effort to unveil the lead molecules as potential therapeutic agents, for prevention of MMPs mediated tissue damage in inflammation and rheumatoid arthritis. Data have been analyzed through different search engines. RESULTS: Numerous phytochemicals have been studied for their role as MMPs inhibitors which can be processed further to develop into useful drugs for the treatment of inflammation and rheumatoid arthritis. CONCLUSION: In search of new drugs, phytochemicals like flavonoids, glycosides, alkaloids, lignans & terpenes offer a wide canvas to develop into valuable forthcoming medicaments.


Subject(s)
Arthritis, Rheumatoid/drug therapy , Inflammation/drug therapy , Matrix Metalloproteinase Inhibitors/pharmacology , Matrix Metalloproteinases/metabolism , Phytochemicals/pharmacology , Alkaloids/pharmacology , Flavonoids/pharmacology , Glycosides/pharmacology , Humans , Lignans/pharmacology , Phytochemicals/chemistry , Signal Transduction/drug effects , Terpenes/pharmacology
6.
Inflammopharmacology ; 27(4): 781-797, 2019 Aug.
Article in English | MEDLINE | ID: mdl-30446927

ABSTRACT

Clematis orientalis Linn has long been used as ethnopharmacy for the treatment of arthritis. This study is intended to evaluate the curative efficacy of Clematis orientalis in treating polyarthritis in rats. Aqueous ethanolic extract and fractions (hexane, butanol and aqueous) were administered orally at 200 mg/kg for 28 days after CFA immunization. Paw swelling, paw diameter, arthritic score, body weight, hematological parameters, radiographic and histological analysis of ankle joints were evaluated. Moreover, levels of various inflammatory markers through RT-PCR and ELISA were measured. DPPH and reducing power assays were used to appraise antioxidant capacity. Qualitative phytochemical analysis, determination of total phenolic and flavonoid contents were also carried out. Aqueous ethanolic extract and fractions significantly (p < 0.001) reduced paw volume, paw thickness and arthritic score and considerably prevented decrease in body weight along with anomalous alterations in hematological parameters in comparison with arthritic control. X-ray and histological examination revealed no significant structural changes in ankle joints of treated rats. Expression levels of IL-1ß, TNF-α, IL-6, COX-2 and NF-Kß were significantly (p < 0.05-0.001) suppressed as well as noteworthy increase in the levels of IL-4 and IL-10 among treated animals has been detected. Overproduction of TNF-α and PGE2 was substantially prevented in animals given different treatments. Aqueous ethanol extract and its fractions demonstrated significant and concentration-dependent antioxidant potential. In general, among fractions aqueous fraction exhibited a greater anti-arthritic effect. Phytochemical analysis of aqueous fraction confirmed the presence of flavonoids and glycosides, 215.29 mgGAE/ml phenolic content and 633.03 µgQE/ml flavonoid content. Thus, we suggest Clematis orientalis as a potent strategy for the treatment of rheumatoid arthritis.


Subject(s)
Antirheumatic Agents/pharmacology , Arthritis, Experimental/chemically induced , Arthritis, Experimental/drug therapy , Arthritis, Rheumatoid/drug therapy , Clematis/chemistry , Freund's Adjuvant/pharmacology , Plant Extracts/pharmacology , Animals , Anti-Inflammatory Agents/pharmacology , Antioxidants/pharmacology , Arthritis, Experimental/metabolism , Arthritis, Rheumatoid/chemically induced , Arthritis, Rheumatoid/metabolism , Biomarkers/metabolism , Cytokines/metabolism , Ethanol/chemistry , Female , Flavonoids/pharmacology , Male , Phytotherapy , Rats , Rats, Sprague-Dawley
7.
Pak J Pharm Sci ; 30(5): 1779-1781, 2017 Sep.
Article in English | MEDLINE | ID: mdl-29084701

ABSTRACT

The rational use of plants as medicine is traced back over five epochs to ancient documents of early civilizations and is certainly as old as mankind. These medicines originally developed from crude drugs like tinctures and tinctures. Minimum 119 chemical substances are derived from 90 plant species and used all over the world as medicines, several of them containing compounds derived from or modelled after naturally occurring lead molecules and 74% of these derived from orthodox medicinal plants. 252 drugs (11%) are believed to be basic and essential by the WHO and are exclusively of plant origin. We have examined anti-urease activity of ethyl alcohol (Et-OH) and methyl alcohol (Me-OH) extracts of H. rhamnoides and Cassia fistula. Berthelot assay was used for the determination of anti-urease activity. The enzyme activity and inhibition was measured through catalytic effects of urease on urea by measuring change in absorbance in the absence and in the presence of inhibitor at 625nm using UV spectrophotometer. In the study, both Et-OH and Me-OH extracts of H. rhamnoides (91.69%±1.21) and C. fisstula (79.44%±0.55) showed stronger action against urease activity. An overview on the medicinal uses of H. rhamnoides and C. fisstula showing anti-urease activity may predict their possible alternative use for stomach problems. This study may help to explain the beneficial effects of these plants against stomach infection associated with pathogenic strains of H. pylori as Urease is the most prominent protein component of H. pylori.


Subject(s)
Cassia/chemistry , Enzyme Inhibitors/pharmacology , Hippophae/chemistry , Plant Extracts/pharmacology , Urease/antagonists & inhibitors , Catalysis , Enzyme Inhibitors/isolation & purification , Ethanol/chemistry , Methanol/chemistry , Plant Extracts/isolation & purification , Solvents/chemistry , Urea/metabolism , Urease/metabolism
8.
Hypertens Res ; 40(12): 966-975, 2017 Dec.
Article in English | MEDLINE | ID: mdl-28878301

ABSTRACT

Eicosapentaenoic acid:docosahexaenoic acid (EPA:DHA) 6:1, an omega-3 polyunsaturated fatty acid formulation, has been shown to induce a sustained formation of endothelial nitric oxide (NO) synthase-derived NO, a major vasoprotective factor. This study examined whether chronic intake of EPA:DHA 6:1 prevents hypertension and endothelial dysfunction induced by angiotensin II (Ang II) in rats. Male Wister rats received orally corn oil or EPA:DHA 6:1 (500 mg kg-1 per day) before chronic infusion of Ang II (0.4 mg kg-1 per day). Systolic blood pressure was determined by tail cuff sphingomanometry, vascular reactivity using a myograph, oxidative stress using dihydroethidium and protein expression by immunofluorescence and western blot analysis. Ang II-induced hypertension was associated with reduced acetylcholine-induced relaxations of secondary branch mesenteric artery rings affecting the endothelium-dependent hyperpolarization (EDH)- and the NO-mediated relaxations, both of which were improved by the NADPH oxidase inhibitor VAS-2870. The Ang II treatment induced also endothelium-dependent contractile responses (EDCFs), which were abolished by the cyclooxygenase (COX) inhibitor indomethacin. An increased level of vascular oxidative stress and expression of NADPH oxidase subunits (p47phox and p22phox), COX-1 and COX-2, endothelial NO synthase and Ang II type 1 receptors were observed in the Ang II group, whereas SKCa and connexin 37 were downregulated. Intake of EPA:DHA 6:1 prevented the Ang II-induced hypertension and endothelial dysfunction by improving both the NO- and EDH-mediated relaxations, and by reducing EDCFs and the expression of target proteins. The present findings indicate that chronic intake of EPA:DHA 6:1 prevented the Ang II-induced hypertension and endothelial dysfunction in rats, most likely by preventing NADPH oxidase- and COX-derived oxidative stress.


Subject(s)
Antihypertensive Agents/chemistry , Antihypertensive Agents/pharmacology , Endothelium, Vascular/drug effects , Fatty Acids, Omega-3/chemistry , Fatty Acids, Omega-3/pharmacology , Hypertension/prevention & control , Oxidative Stress/drug effects , Angiotensin II , Animals , Drug Evaluation, Preclinical , Hypertension/chemically induced , Male , NADPH Oxidases/metabolism , Nitric Oxide/metabolism , Random Allocation , Rats, Wistar
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