Effect of Boswellia on Adjuvant Induced Rheumatoid Arthritis in Experimental Animals

Arthritis is the most common systemic connective tissue disease. About 1% of the world's population is affected by RA; women are three times more often than men. Onset is most frequent between the ages of 40 and 50 years, but people of any age can be affected. Rheumatoid arthritis (RA) is a chronic, systemic inflammatory disorder that may affect many tissues and organs, but principally attacks flexible joints. Although the cause of rheumatoid arthritis is unknown, autoimmunity plays an important role in both its chronicity and progression.The new trend of medical treatment of rheumatoid arthritis seeks new drugs with more efficacy and fewer side effects. Since tumor necrosis factor alpha (TNF-α) as well as other cytokines act as key players in the development of arthritis.Studies in the United States and Europe have shown that their use is less common in clinical settings, but has become increasingly more in recent years as scientific evidence about the effectiveness of herbal medicine has become more widely available.  The present work investigates the effect of Boswellia on Adjuvant induced RA in Experimental Animals

FORMULATION AND EVALUATION OF IN SITU OCULAR GEL OF LEVOFLOXACIN

Total of 8 formulations of in situ gels of Levofloxacin hydrochloride were prepared by pH triggered in situ gelling system using different polymers like sodium alginate as gelling agent, Noveon AA-1 polycarbophil and HPMC E50LV as viscosity enhancing agent and benzalkonium chloride as preservative. All the prepared formulations were clear and the visual appearance was found to be transparent. The pH of the prepared formulations was ranged between 6.50and 7.00. The drug content varied between 96.84 ± 0.396 and 99.65±0.489 % which indicated that the uniform distribution of drug was found in all the prepared formulations. Among all the formulations, the formulations A4 and A8 showed better gelling capacity. The shear rate on the preparation was large during the blinking stage. From the in vitro drug release profile the formulations A4 and A8 was selected as the best formulations and these formulations were used for further studies such as mechanism of drug release, sterility, antimicrobial efficacy, ocular irritation and accelerated stability. Both formulations provided good fit to the Higuchi model. According to this model, the drug release from these gels may be controlled by diffusion through the micro-pores. The selected formulations showed good anti-microbial action against the organisms and ocular irritation studies revealed that the selected formulations were good with non-irritation and there were no ocular damage or abnormal clinical signs. During and at the end of the accelerated stability study, the selected formulations did not undergo any chemical changes/interaction and remained stable during the study period and showed almost similar physical stability and drug content. Key Words: Levofloxacin hydrochloride, in situ gels, in vitro drug release, Higuchi model, accelerated stability study. Â

Magnetic nanoparticles for hyperthermia in cancer treatment: an emerging tool

International audienceAccording to a statistical survey conducted by the Global Cancer Observatory (a division of the World Health Organization),cancer remains as the major cause of death worldwide. The main reason why available therapies fail is that a “vicious cycle” inestablished which initiates multiple pathways and recurrence after metastasis. Hyperthermic treatment, which involves heating tumor tissues to a moderate temperature of 40–43 °C, has emerged as an effective strategy for treating tumors. This method ishighly efficient at destroying tumor cells and does not induce the side effects of conventional cancer treatments. On the otherhand, hyperthermic treatment method can be co-administered with conventional treatments. Nanotechnology had created hugeopportunities in almost all areas of research, including the field of hyperthermic treatment. The utilization of magnetic nanopar-ticles (MNPs) offers functionalities not possible using conventional magnetic materials. In this review, we detail recent devel-opments and applications of MNPs for hyperthermic treatment and discuss future possibilities

Screening and Molecular Docking of Bioactive Metabolites of the Red Sea Sponge <i>Callyspongia siphonella</i> as Potential Antimicrobial Agents

Marine sponges create a wide range of bioactive secondary metabolites, as documented throughout the year. Several bioactive secondary metabolites were isolated from different members of Callyspongia siphonella species. This study aimed for isolation and structural elucidation of major metabolites in order to investigate their diverse bioactivities such as antimicrobial and anti-biofilm activities. Afterwards, a molecular docking study was conducted, searching for the possible mechanistic pathway of the most bioactive metabolites. Extraction, fractionation, and metabolomics analysis of different fractions was performed in order to obtain complete chemical profile. Moreover, in vitro assessment of different bioactivities was performed, using recent techniques. Additionally, purification, structural elucidation of high features using recent chromatographic and spectroscopic techniques was established. Finally, AutoDock Vina software was used for the Pharmacophore-based docking-based analysis. As a result, DCM (dichloromethane) fraction exerted the best antibacterial activity using disc diffusion method; particularly against S. aureus with an inhibition zone of 6.6 mm. Compound 11 displayed a considerable activity against both MRSA (Methicillin-resistant Staphyllococcus aureus) and Staphyllococcus aureus with inhibition ratios of 50.37 and 60.90%, respectively. Concerning anti-biofilm activity, compounds 1 and 2 displayed powerful activity with inhibition ratios ranging from 39.37% to 70.98%. Pharmacophore-based docking-based analysis suggested elongation factor G (EF-G) to be a probable target for compound 11 (siphonellinol C) that showed the best in vitro antibacterial activity, offering unexplored potential for new drugs and treatment candidates

The anticancer and EGFR-TK/CDK-9 dual inhibitory potentials of new synthetic pyranopyrazole and pyrazolone derivatives: X-ray crystallography, in vitro, and in silico mechanistic investigations

Treatment options for the management of breast cancer are still inadequate. This inadequacy is attributed to the lack of effective targeted medications, often resulting in the recurrence of metastatic disorders. Cumulative evidence suggests that epidermal growth factor receptor (EGFR-TK) and cyclin-dependent kinases-9 (CDK-9) overexpression correlates with worse overall survival in breast cancer patients. Pyranopyrazole and pyrazolone are privileged options for the development of anticancer agents. Inspired by this proven scientific fact, we report here the synthesis of two new series of suggested anticancer molecules incorporating both heterocycles together with their characterization by IR, 1H NMR, 13C NMR, 13C NMR-DEPT, and X-ray diffraction methods. An attempt to get the pyranopyrazole-gold complexes was conducted but unexpectedly yielded benzylidene-2,4-dihydro-3H-pyrazol-3-one instead. This unexpected result was confirmed by X-ray crystallographic analysis. All newly synthesized compounds were assessed for their anti-proliferative activity against two different human breast cancer cells, and the obtained results were compared with the reference drug Staurosporine. The target compounds revealed variable cytotoxicity with IC50 at a low micromolar range with superior selectivity indices. Target enzyme EGFR-TK and CDK-9 assays showed that compounds 22 and 23 effectively inhibited both biological targets with IC50 values of 0.143 and 0.121 µM, respectively. Molecular docking experiments and molecular dynamics simulation were also conducted to further rationalize the in vitro obtained results