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Eleven highly functionalized diterpenes have been isolated from two Pacific marine sponges, Acanthella spp. Each bears two or three isocyano functions, a tertiary alcohol, a tetrahydropyranyl or tetrahydrofuranyl moiety, and occasionally chlorine or isothiocyano substituents. Two representative structures were determined by X-ray diffraction studies, and the others by spectral correlation. All kalihinols inhibit the growth of three test organisms, Bacillus subtilis, Staphylococcus aureus, and Candida albicans.In two preliminary communications3,4 we reported the structures of five isocyano diterpenoid antibiotics, kalihinols A, B, C, E, and F (Chart I), isolated from a Guam sponge, Acanthella sp. This paper provides detailed data for these compounds and for six additional kalihinols, the trace constituents D, G, and H from the Guam Acanthella, and kalihinols X, Y, and Z from a Fiji Acanthella sp. Common to all eleven kalihinols is a trans-decalin bearing a tertiary alcohol at C-4 and in all but three cases isocyano functions at C-5 and C-10. The kalihinols differ in their C8 moiety,

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Ethnomedical reports on these traditional medicinal plants have been rationalised through an insight into the anti-inflammatory as well as anticancer potential of four constituents, characterised to be prospective candidates for designing novel therapeutic agents.

BackgroundQuercetin (QCT), a naturally occurring flavonoid has a wide array of pharmacological properties such as anticancer, antioxidant and anti-inflammatory activities. QCT has low solubility in water and poor bioavailability, which limited its use as a therapeutic molecule. Polymeric micelles (PMs) is a novel drug delivery system having characteristics like smaller particle size, higher drug loading, sustained drug release, high stability, increased cellular uptake and improved therapeutic potential. In the present study, we have formulated and characterized mixed PMs (MPMs) containing QCT for increasing its anticancer potential.MethodsThe MPMs were prepared by thin film hydration method, and their physicochemical properties were characterized. The in vitro anticancer activity of the MPMs were tested in breast (MCF-7 and MDA-MB-231, epithelial and metastatic cancer cell lines, respectively), and ovarian (SKOV-3 and NCI/ADR, epithelial and multi-drug resistant cell lines, respectively) cancer.ResultsThe optimal MPM formulations were obtained from Pluronic polymers, P123 and P407 with molar ratio of 7:3 (A16); and P123, P407 and TPGS in the molar ratio of 7:2:1 (A22). The size of the particles before lyophilization (24.83±0.44 nm) and after lyophilisation (37.10±4.23 nm), drug loading (8.75±0.41%), and encapsulation efficiency (87.48±4.15%) for formulation A16 were determined. For formulation A22, the particle size before lyophilization, after lyophilization, drug loading and encapsulation efficiency were 26.37±2.19 nm, 45.88±13.80 nm, 9.01±0.11% and 90.07±1.09%, respectively. The MPMs exhibited sustained release of QCT compared to free QCT as demonstrated from in vitro release experiments. The solubility of QCT was markedly improved compared to pure QCT. The MPMs were highly stable in aqueous media as demonstrated by their low critical micelle concentration. The concentration which inhibited 50% growth (IC50) values of both micellar preparations in all the cancer cell lines were significantly less compared to free QCT.ConclusionBoth the MPMs containing QCT could be used for effective delivery to different type of cancer and may be considered for further development.

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In the present study, we have synthesized silver nanoparticles (AgNPs) using Pueraria tuberosa aqueous extract (PTAE) in a straightforward manner without involvement of toxic chemicals. Various reaction parameters (reaction time, AgNO concentration, pH, reaction temperature and PTAE concentration) were optimizeded for the synthesis of AgNPs through visual observation of colour change and absorption peak by UV-Vis spectroscopy. The green synthesized AgNPs were analyzed by DLS, FTIR, SEM, TEM, EDS and XRD for their bio-physical characteristics. The AgNPs were screened for their antioxidant activity by determining total antioxidant capacity (TAC) and anticancer potential by MTT assay. The average particle size of AgNPs was 162.72 ± 5.02 nm with zeta potential of -30.14 ± 2.08 mV. The spherical shape of the AgNPs was confirmed by SEM and TEM. FTIR spectra showed the involvement of different phytoconstituents as capping and stabilizing agents in the synthesis of AgNPs. The TAC of the optimized synthesized AgNPs was more than PTAE. The IC of synthesized AgNPs against MCF-7, MDA-MB-231, SKOV-3, U-87 and NCI/ADR cell lines was 3.859, 1.128, 29.36, 6.053 and 25.49 µg/ml, respectively. The green synthesized AgNPs has potential for use in the treatment of different types of cancer.

VO(acac)(2)-CeCl(3) combo catalyst has been developed for chemoselective cyclocondensation cum oxidation under mild reaction conditions toward synthesis of a new class of optically pure compounds, 2-(2'-C-3',4',6'-tri-O-benzyl/methyl-glycal)-1H-benzimidazoles. It involves an operationally simple synthetic protocol efficient for the syntheses of a wide range of chiral benzimidazoles in high yields without formation of undesired 1,2-disubstituted and pseudoglycal byproducts. Vanadium(V) is found as active oxidant for the chemical processes which is investigated by UV absorption spectroscopy. Highly ordered one-dimensional low molecular mass organic nanostructured materials are fabricated by nanocrystallization of the chiral nanoscale building blocks. Theoretical calculation by the B3LYP/6-31G** level of theory of the glycal-based chiral benzimidazoles shows out of planar geometry of the 1H-anthra[1,2-d]imidazole-6,11-dione moiety, which is responsible for the strong self-aggregation to generate ultralong nanostructured materials. We have also found nice agreement between the theoretical results with the experimental observation in 2D-NOESY experiments. The photophysical property of the solid nanostructured materials is also reported.