Fourier transform infrared spectrometer analysis and antimicrobial screening of ethanolic extract of Operculina terpathum from cholistan desert.

Aim of present study was to assess pharmacological (antioxidant, antibacterial & antifungal) potential of Operculina terpathum seeds. Ethanolic extract was prepared and its phytochemical evaluation show the different chemical compounds such as carbohydrates, phenols, tannin, flavonoids, cardiac glycosides, steroids, alkaloids and proteins. FTIR spectra showed the presence of organic acids, hydroxyl and phenolic compounds, amino groups, aliphatic compounds, functional groups such as amide, ketone, aldehyde, aromatics and halogen compounds. Antioxidant activity of the Operculina terpathum alcoholic extract was performed by DPPH method and it showed 97.13%whereas IC50±SEM (µg/ml) was 1.425±0.16. Antibacterial activity was performed against different bacterial strains and results were comparable with that of standard. Maximum antibacterial activity was exhibited by Bacillus subtillis (28.33±2 mm) and Bacillus pumilus (25.33±2 mm) respectively. Antifungal activity was also performed and it showed maximum activity against Aspergillus flavous and Candida albicans6±1, 5±1mm respectively. These results showed that Operculina terpathum has good antibacterial and antifungal activity against different microbes and it could be used as an alternative to antibiotics, as the antibiotics resistance is very common now a days.

Fourier transform infrared spectrometer analysis and antimicrobial screening of ethanolic extract of Operculina terpathum from cholistan desert

Aim of present study was to assess pharmacological (antioxidant, antibacterial & antifungal) potential of Operculina terpathum seeds. Ethanolic extract was prepared and its phytochemical evaluation show the different chemical compounds such as carbohydrates, phenols, tannin, flavonoids, cardiac glycosides, steroids, alkaloids and proteins. FTIR spectra showed the presence of organic acids, hydroxyl and phenolic compounds, amino groups, aliphatic compounds, functional groups such as amide, ketone, aldehyde, aromatics and halogen compounds. Antioxidant activity of the Operculina terpathum alcoholic extract was performed by DPPH method and it showed 97.13%whereas IC50±SEM (μg/ml) was 1.425±0.16. Antibacterial activity was performed against different bacterial strains and results were comparable with that of standard. Maximum antibacterial activity was exhibited by Bacillus subtillis (28.33±2 mm) and Bacillus pumilus (25.33±2 mm) respectively. Antifungal activity was also performed and it showed maximum activity against Aspergillus flavous and Candida albicans6±1, 5±1mm respectively. These results showed that Operculina terpathum has good antibacterial and antifungal activity against different microbes and it could be used as an alternative to antibiotics, as the antibiotics resistance is very common now a days. (AU)

Organic anion­transporting polypeptides contribute to the uptake of curcumin and its main metabolites by human breast cancer cells: Impact on antitumor activity.

Curcumin is a natural polyphenolic compound with pronounced anticancer properties, despite its low bioavailability caused by extensive glucuronidation and sulfation. Information on the cellular uptake mechanisms and their contribution to the anticancer effects of curcumin and its biotransformation products is limited. The present study, therefore, investigated the role of organic anion­transporting polypeptides (OATPs) in the cellular uptake of curcumin and its major metabolites in OATP­expressing Chinese hamster ovary (CHO) and human ZR­75­1 breast cancer cells. The uptake rates for curcumin in OATP1B1­, OATP1B3­ and OATP2B1­transfected CHO cells were 2­ to 3­fold higher than wild­type cells. Curcumin sulfate was transported by all three OATPs, although to a much lesser extent, while uptake of tetrahydrocurcumin was the highest but only via OATP1B1 and OATP1B3. Notably, curcumin glucuronide did not exhibit any affinity for these OATPs. The increased mRNA levels of OATP1B1 in wild­type human breast cancer ZR­75­1 cells compared with OATP1B1 knockdown cells was associated with a higher initial uptake of curcumin and tetrahydrocurcumin leading to decreased IC50 values. In conclusion, our data revealed that OATPs act as cellular uptake transporters for curcumin and its major metabolites, and this may also be applicable to patients undergoing cancer therapy.

Formulation and in vitro evaluation of sustained release matrix tablets using cross-linked natural gum.

Polysaccharide gums because of their biocompatibility, biodegradability and non-immunogenic properties are considered as the best choice for preparing sustained release tablets as compared to their synthetic counterpart. The cross linking of natural gums in matrix tablets increase the sustained release property of matrix tablets. Isoniazid is a first line therapy of tuberculosis, belongs to BCS I with half-life of 3-4 hours. These characteristics make isoniazid a good candidate for sustained release dosage form. Karaya gum crossed linked with trisodium tri metaphosphate was used as release rate retardant for preparing isoniazid cross-linked matrix tablet. Total 8 sustained release formulations were prepared. Both granules and tablets were evaluated under in vitro condition against different parameters. Dissolution studies were performed with all eight formulations for 12 hours using USP apparatus I. Four formulations designated as F1, F2, F3, F4 have drug and karaya gum while other four formulations F5, F6, F7, F8 have drug and crossed linked polymer in ratios of 1:1, 1:2, 1:3 and 1:4 respectively. Dissolution data was analyzed by using different kinetic models. Best fit model for most efficient formulation was zero order while release mechanism was super case I. Formulation 8 showed sufficiently slow release kinetics and about 83% of drug was released in 10 hours, indicating that cross-linked karaya gum proved efficient in preparing sustained release tablets.