Due to its appreciable diversity in biological actions, thiazole and its substituted components, a significant class of heterocyclic compounds has developed as an influential scaffold in the field of chemical sciences. The variability of thiazole core has been expressed through the effective instigation of its anticancer (Dasatinib, Tiazofurin), antiretroviral (Ritonavir, Brecanavir), antimicrobial (Sulfathiazole, Ravuconazole) and anti-inflammatory (Fenclozic acid, Meloxicam) derivatives. This reasonable diversity in the physiological reaction pattern led many scientists to refine and develop new structural alternatives with much more efficient pharmacological action. This review is crucial for previous studies and projects to survey the antimicrobial activity of thiazole and thiazole related compounds to the mid of 2019.

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ObjectivesIn Indo China, carrots have been reported to regulate the functions of the stomach and intestines. The objective of the present investigation was to unravel the therapeutic potential of 50% ethanol extract from Daucus carota roots (EDC) on antisecretory, gastroprotective, and in vitro antacid capacity using experimental rats.MethodsAssessment of EDC antisecretory and in vivo antacid capacities was carried out using a pyloric ligation induced ulcer model. The gastroprotective effect was assessed with an absolute ethanol induced ulcer model. The integrity of gastric mucosa was evaluated using the estimation of glutathione and gastric mucus level and with histopathological examination of gastric mucosal cells. The in-vitro antacid capacity was evaluated using a titration method. The effect of the extract on the liver was assessed by measuring serum biochemical parameters.ResultsThe EDC significantly (p < 0.01–0.001) reduced gastric lesions in both models. Furthermore, the EDC also significantly (p < 0.05–0.001) reduced the volume of gastric content whereas the total acidity was significantly (p < 0.05–0.001) reduced with the doses of 100 mg/kg and 200 mg/kg EDC. Moreover, the mucus content and glutathione level increased significantly (p < 0.05) in the absolute alcohol-induced ulcer. The EDC also showed in-vitro antacid capacity. Histopathological studies further confirmed the potential of EDC by inhibiting congestion, edema, hemorrhage, and necrosis in gastric mucosa.ConclusionThe EDC exerted antisecretory, gastroprotective, and in vitro antacid potential. These activities could be attributed due to the presence of glycosides, phenolics, tannins, alkaloids, and flavonoids.

The data obtained indicate that the EDSL has antidiarrhoeal and antiperistalsis activities and thus supports its traditional use. The data also show that the plant material given p.o. may be safe and/or non-toxic in mice.

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BackgroundLagerstroemia speciosa (SEL) leaves are a popular folk medicine for diabetes treatment due to presence of corosolic acid. It has low water solubility resulting poor absorption after oral administration. Self micro-emulsified drug delivery system is the way by which we can improve the oral absorption of drug.ObjectiveThe objective of this study was to develop the self micro-emulsifying formulation of standardized extract of SEL leaves and evaluate its pharmacodynamic performance for antidiabetic activity.Materials and methodsThe SME formulation was prepared by using sefsol-218 as oil, cremophor-EL as surfactant and transcutol-P as co-surfactant. The ratio of surfactant and co-surfactant was determined by pseudoternary phase diagram. SME formulations were characterized for dilution at different pH, self emulsification, optical clarity, globule size and thermodynamic stability. Pharmacodynamic evaluation of formulations was assessed in Wistar rats by using parameters viz. blood glucose level and serum lipid profile.ResultsSEL loaded SME formulation was successfully developed by using sefsol-218, cremophor-EL and transcutol-P with a droplet size 23.53 nm. Pharmacodynamic results showed a higher reduction in blood glucose by SME formulation than SEL without SMES respectively at 50 mg/kg dose while reduction produced at dose of 100 mg/kg was found significant and better on 15th day of study. The percentage reduction produced by SME formulation on serum lipid profile was also significant and was more prominent than SEL.ConclusionThis study confirms that the formulation elevates the pharmacodynamic performance of SEL approximately two fold.

Phytopharmaceuticals have always reported vital roles in the field of medicine hence the need to investigate safe and efficient drugs for treating metabolic disorders is very significant. Roots of Selinum vaginatum have therapeutic benefits and are widely used by the people of the Rohtang region for treating diabetes and its associated complications. The present study focusses on the isolation of the bioactive from the S. vaginatum roots for estimating acute toxicity studies, anti-diabetic and diabetic neuropathy protective action along with the mechanism of action in STZ induced Wistar rats. The Selinum vaginatum roots were collected from the Rohtang region, Himalayas. Chlorogenic acid was isolated and underwent identification by UV, HPLC, 1 H NMR, C13 NMR, Mass, and FTIR spectroscopy methods. Chlorogenic acid was dosed at 10 and 20 mg/kg to observe the effects on experimentally induced diabetes and with time generated diabetic neuropathic complications. Biomarkers TNF-α, superoxide dismutase, nitrosative stress, lipid peroxide profile, and membrane-bound inorganic phosphate were analyzed. Histopathological evaluation of the liver and sciatic nerve was performed for all groups. Parameters like blood glucose levels, body weight, food intake, Thermal Hyperalgesia, Writhing, Cold Hyperalgesia Responses, Mechanical hyperalgesia, Grip Strength, Spontaneous Locomotor (Exploratory) Test, Neuromuscular Coordination tests, and lipid profile analysis showcased the anti-diabetic and diabetic neuropathy protective action of the drug. Inflammation, degradation, and necrosis were found to be reduced in the liver and sciatic nerve cells of treated groups. All the biomarkers used to analyze the oxidative pathway were significantly replenished indicates that chlorogenic acid produces these effects through this pathway.

Background: Aegle marmelos Corr. (Rutaceae) commonly known as ‘Indian Bael’ has been used as a brain tonic traditionally. However, despite this traditional use, not enough scientific report is present that can confirm the use of this plant in neurological disorders. Thus, the total sterols fraction and stigmasterol from the leaves of Aegle marmelos were investigated for antidepressant-like effect along with their possible mechanism(s) of action by primarily performing acute toxicity study of total sterols. Methods: An acute toxicological study was carried out at a single oral dose of 2000 mg/kg. Sign of toxicity was observed by estimating biochemical and performing histopathological analysis. For the antidepressant-like effect, different doses of total sterols (50-200 mg/kg, p.o. for seven days) and stigmasterol (5- 20 mg/kg, i.p. acute) were administered in mice using TST and FST models. To evaluate the mechanism of action, mice were pretreated with GABA, 5-HT, DA, adrenergic antagonists, and glutamate agonists. Furthermore, a neurochemical study was performed following TST and molecular docking study was also performed to determine the binding affinity of stigmasterol. Results: Total sterols fraction presents no sign of toxicity up to the oral dose of 2000 mg/kg. Oral treatment of total sterols and acute intraperitoneal treatment of stigmasterol (except 5 mg/kg) reduced the immobility time significantly. Pretreatment with pCPA (5-HT synthesis inhibitor) and NMDA (an agonist of the glutamate site) effectively reversed the immobility time of total sterols and stigmasterol (except pCPA) in TST. However, bicuculline (competitive GABA antagonist), haloperidol (D2 dopaminergic antagonist) and prazosin (α1 adrenergic antagonist) could not reverse the immobility time. Meanwhile, total sterols also effectively altered the hippocampus 5-HT and Glu levels. Also, the result of the molecular docking study depicted that stigmasterol has an affinity to the NMDA receptor. Conclusions: The present study suggests that the total sterols fraction did not produce any acute toxicity in rats. Also, we reported that total sterols, stigmasterol and sub-effective stigmasterol co-administration with fluoxetine significantly reduced the time of immobility in TST and FST confirmed the antidepressant-like effect of total sterols fraction and stigmasterol. Moreover, further findings suggest that the antidepressant-like effect of total sterols might be mediated by the serotonergic and glutamatergic systems. Whereas only the glutamatergic system was involved in the antidepressant activity of stigmasterol.