Enhanced antihyperlipidemic potential of gemfibrozil under co-administration with piperine.

Gemfibrozil is a well-known potent antihyperlipidemic drug with the capacity to lower triglyceride and cholesterol levels, which are responsible for most cardiovascular and cerebrovascular diseases. In addition, gemfibrozil has a potent activity at elevating the high density lipoprotein levels. However, this drug has a very short half-life of about 2 â€‹h and toxicity is observed in the liver as the dose increases. The drug piperine has the capacity to enhance the bioavailability of other drugs without altering their basic properties as well as improving their activity. In this study, we aimed to enhance the bioavailability of gemfibrozil as well as making it more potent and less toxic by applying piperine as a bio-enhancer. Thus, piperine was co-administered to rats with gemfibrozil and the antihyperlipidemic activity was tested when fed on a high fat diet. The results showed that co-administration of gemfibrozil with piperine decreased the elevated triglyceride and cholesterol levels to normal, and they performed significantly better than the individual drugs. Weight gain was controlled effectively by drug administration together with piperine compared with other groups. Hepatic function analyses demonstrated that the potentiation of gemfibrozil did not alter the hepatic function but instead it improved significantly by normalizing the elevated serum glutamic oxaloacetic transaminase, serum glutamic pyruvic transaminase, and alkaline phosphatase levels. The plasma drug concentration of gemfibrozil was studied over time, where the enhanced activity of the drug reached its Cmax within 1 â€‹h of administration and the activated drug level was observed in the blood for 4 â€‹h.

Promising upshot of silver nanoparticles primed from Gracilaria crassa against bacterial pathogens.

BACKGROUND: The study on newer antimicrobial agent from metal based nano materials has augmented in recent years for the management of multidrug resistance microorganisms. In our present investigation, we synthesized silver nanoparticles (AgNP's) from red algae, Gracilaria crassa as beginning material which effectively condensed the silver ions to silver nanoparticles with less price tag and no risk. METHODS: Silver nanoparticles were prepared by simple reaction of 1 mM AgNO3 with G. crassa extracts at room temperature. The fabricated AgNP's were subjected for characterization and screened against various microorganisms for antibacterial activity. RESULTS: UV-Vis spectroscopy (200-800 nm), XRD, FESEM and EDAX, were performed for AgNP's. UV-Vis spectroscopy demonstrated the absorption edge at 443 nm and EDAX pattern is purely due to the particle size and face centered cubic (fcc) symmetry of nanoparticles. Average size lays at 122.7 nm and zeta potential was found to be -34.9 mV. The antibacterial outcome of synthesized AgNP's (at the dose of 20 and 40 µg/ml) was evaluated against Escherichia coli, Proteus mirabilis, Bacillus subtilis and Pseudomonas aeruginosa. The mechanism of synthesized AgNP's bactericidal bustle is discussed in terms of interaction with the cell membrane of bacteria. The activity was found to be sky-scraping in a dose dependent manner. CONCLUSION: Thus, environmental friendly, cost effective, non hazardous stable nanoparticles were prepared by green synthesis using red algae, G. crassa. Synthesized G. crassa AgNP's were in acceptable size and shape. Further, it elicits better bactericidal activity against microorganism. This will assure the out put of superior antibacterial formulation for near future.

Formulation and comparative evaluation of poly herbal anti-acne face wash gels.

CONTEXT: Rauvolfia serpentina (L). Benth. ex Kurz. (Apocynaceae) possessing antibacterial properties are widely used in modern herbal medicines. Curcuma longa L. (Zingiberaceae), a readily available antiseptic, possess antioxidant, antibacterial, blood purifying and antiinflammatory properties and used in various skin creams. Azadirachta indica A. Juss. (Meliaceae) possess astringent, antiviral, discutient, stimulant and antibacterial properties and works excellently well against acne and keeps the skin healthy. OBJECTIVE: Acne is the common skin problem that 85% of the teenagers face today. In this study, poly herbal anti-acne face wash gels were prepared using two polymers Carbopol and hydroxy propyl methyl cellulose (HPMC) along with the extracts of plants Rawvolfia serpentina, Curcuma longa, and Azadiracta indica. MATERIALS AND METHODS: The gel formulations were prepared in four different concentrations of 50, 100, 200 mg/ml as Gel-CRB 100, Gel-HPMC 50, Gel-HPMC 100, Gel-HPMC 200, respectively. The formulations were tested for the anti-acne activity by turbidimetric method. RESULTS: RESULTS showed that the gels were non-irritant, stable and posses anti-acne activity. The efficacy when tested with a standard was almost same to that of Clindamycin gel. DISCUSSION AND CONCLUSION: From this study, Gel-HPMC 100 was proved to be stable and considered as an effective herbal formulation for acne treatment.

Tyrosine and glycine derivatives as potential prodrugs: design, synthesis, and pharmacological evaluation of amide derivatives of mefenamic acid.

This study deals with the synthesis, pharmacological activity, and kinetic studies of mefenamic acid (MA) prodrugs of tyrosine and glycine. The synthesis involved a series of protection and deprotection reactions. The hydrolysis of these prodrugs in the intestine was confirmed by hydrolysis kinetics studies in simulated gastric fluid, simulated intestinal fluid, and 80% plasma. The prodrugs were also evaluated for analgesic, anti-inflammatory, and ulcerogenic activities. The glycine prodrug showed maximum analgesic activity of 86%, and both tyrosine and glycine prodrugs showed better anti-inflammatory activity of 74% and 81%, respectively, when compared to the 40% of MA. Further, the prodrugs showed fewer gastric ulcers compared to MA; tyrosine and glycine prodrugs had an average ulcer index of 9.1 and 4.5, respectively, while an average ulcer index of 24.2 was observed with MA. These findings suggest that both prodrugs are better in action as compared to MA, and are advantageous in having fewer gastrointestinal side effects.

Antimicrobial, wound healing and antioxidant activities of Anthocephalus cadamba.

Anthocephalus cadamba (Roxb.) Miq. Syn A. chinensis (Lamk) A. Rich (Rubiaceae) is ethnomedicinally widely used in the form of paste by tribe in western Ghats for treating skin diseases. In this context, antimicrobial potential of A. cadamba against a wide range of microorganisms was studied. To validate the ethnotherapeutic claims of the plant in skin diseases, wound healing activity was studied, besides antioxidant activity to understand the mechanism of wound healing. The alchoholic and aqueous extract of this plant showed significant antibacterial and antifungal activity against almost all the organisms: Micrococcus luteus, Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, and four fungi Candida albicans, Trichophyton rubrum--dermatophyte fungi, Aspergillus niger, Aspergillus flavus and Aspergillus nidulans--systemic fungi, with especially good activity against the dermatophyte (Trichophyton rubrum) and some infectious bacteria (Escherichia coli, Proteus mirabilis and Staphylococcus aureus) with an MIC of 2.5 microg/disc. The results show that A. cadamba extract has potent wound healing capacity as shown from the wound contraction and increased tensile strength. The results also indicated that A. cadamba extract possesses potent antioxidant activity by inhibiting lipid peroxidation and increase in the superoxide dismutase (SOD) and catalase activity.

Evaluation of anti-inflammatory potential of Pavetta indica Linn. leaf extract (family: Rubiaceae) in rats.

The anti-inflammatory potential of methanol extract of Pavetta indica Linn. leaves (Family: Rubiaceae) was evaluated against several models of inflammation such as carragenin, histamine and dextran induced pedal inflammation in rats. The extract showed 48.41%, 41.10% and 24.22% inhibition respectively; when compared to that of control animals. The effect was comparable with that of the standard drug indomethacin, a standard non-steroidal anti-inflammatory drug. Simultaneous subplantar administration of the extract and carrageenin in a mixture helps in differentiating true anti-inflammatory action from an apparent anti-inflammatory effect due to counter-irritant activity. The methanol extract also effectively and significantly reduced cotton pellet induced granuloma. The percentage of inhibition was 62.78 at the dose 500 mg/kg, thereby suggesting its activity in the proliferative phase of the inflammatory process.

Studies on anti-diarrhoeal activity of Ficus hispida. Leaf extract in rats.

Methanol extract of Ficus hispida L. showed significant inhibitory activity against castor oil-induced diarrhoea and PGE(2)-induced enteropooling in rats. It also showed a significant reduction in gastro-intestinal motility on charcoal meal test in rats. The results obtained establish the F. hispida leaf extract as an anti-diarrhoeal agent.