In pursuit of new anti-malarial candidates: novel synthesized and characterized pyrano-benzodioxepin analogues attenuated Plasmodium berghei replication in malaria-infected mice.

Malaria, a parasitic disease, is one of the major causes of morbidity and mortality, particularly in the tropics. Following the increased resistance of the primary causative parasite, Plasmodium sp, to the mainstream drug, artemisinin combination therapies (ACTs), combating malaria incidences, morbidity and mortality have remained elusive. Novel pyrano-benzodioxepin derivatives (DHA-PABA and DHA-LEVO) were synthesized and characterized using Fourier transform infrared (FT-IR) and nuclear magnetic resonance (NMR) spectroscopies. The compounds were subjected to standard in vivo antimalarial screening (using chloroquine-sensitive strain) in mice, and the toxicity was also determined using a standard assay. The observed elevation in serum alkaline phosphatase and acid phosphatase activity in the untreated and the group administered lower doses of DHA-LEVO is an indication of the hepatic stage of the parasite in the experimental animal, which is accompanied by significant perturbation in the membrane of the hepatocyte leading to leakage of this enzyme out of the liver cells. The semisynthetic pyrano-benzodioxepin derivatives act rapidly by clearing the parasite load from the blood. The novel pyrano-benzodioxepin candidates containing endoperoxide functionality hold promise in the pursuit of new monotherapy drug candidates against the virulent strain of the plasmodium.

New n-nonadecanoyl-ß-sitosterol and other constituents from the stem-bark of Anacardium occidentale.

A new steroidal ester bearing n-nonadecanoyl moiety (1) and a mixture of isomeric cerebrosides (2) along with two known compounds were isolated from the methanol extract of the stem-bark of Anacardium occidentale. The structure of the new steroidal ester was determined as 3-n-nonadecanoyl-ß-sitosterol on the basis of modern spectroscopic techniques (IR, ESI-MS, HR-ESIMS, 1D and 2D NMR) and chemical degradation studies. The structures of the known compounds were identified as gallic acid and tanacetene by comparison of the spectroscopic data with those of reported data. The mixture of cerebrosides was confirmed based on the analysis of 1D and 2D NMR. These compounds were evaluated for cytotoxicity against human cancer cell lines A549, SCOV3 and rat normal cell line NRK49f.

Porous starch citrate biopolymer for controlled release of carbofuran in the management of root knot nematode Meloidogyne incognita.

The undesirable environmental impacts of inappropriate application of pesticides have brought about research into new matrices for controlled release of pesticides. Porous starch citrate biopolymer was designed for the release of carbofuran in this experiment and characterized using Fourier Transform Infrared Spectroscopy (FTIR), Scanning Electron Microscopy (SEM) and Thermo-Gravimetric Analysis (TGA) for functional group, surface morphology and thermal stability properties respectively. The SEM revealed highly stabilized porous starch citrate biopolymers with porous structures and gradients suitable for controlled release studies. The transmittance bands at 3347, 1714 and 1073 cm-1 for OH, CO and COC-[bond, double bond]-- stretching vibrations further confirms the successful synthesis of the biopolymer. TGA showed an increase in the thermal stability after citric acid modification with one-step decomposition from 290 ᵒC to 500 ᵒC. From Korsemeyer-Peppas model, the carbofuran-porous starch citrate (CBFN/PRS/STH/CTRT) followed a lower diffusion release model with gradual increment in all the quantity of carbofuran loaded. An accelerated rate of diffusion percentage was seen in direct application of carbofuran. Egg hatch and mortality of juveniles were recorded on daily basis for seven days. Direct application of carbofuran (CBFN/DRT) and carbofuran-porous starch citrate biopolymer gave the best results with significant (p < 0.05) reduction in egg hatch and higher percentage mortality. The rate of release of carbofuran from the starch citrate bio polymer matrix was significantly lower than the direct application, and in spite of the slow rate of release, higher juvenile mortality and reduction in egg hatch was achieved.

Sweet Potato Peels and Cancer Prevention.

A bioassay-guided fractionation of an alcoholic extract from the peels of Ipomoea batatas Lam has been carried out. Sulforhodamine B and 2,2-diphenyl-1-picrylhydrazyl (DPPH) assays were used to evaluate the anticancer and antioxidant potential, respectively, while silica gel column chromatography (CC) was used to isolate compounds that were characterized using 1D- and 2D-NMR (Nuclear Magnetic Resonance) and mass spectrometry. The alcoholic extract was fractionated into n-hexane, ethyl acetate, n-butanol, and water. The n-hexane fraction which showed the most promising anticancer activity was further fractionated via silica gel CC into IB-F002A, IB-F002B, and IB-F002C. Of these, IB-F002C was the most active with IC50 values 24.75, 47.91, 52.37, 34.17, 46.07, and 25.89 µg/ml against breast, colon-1, colon-2, ovary, lung, and head/neck cancer cell lines, respectively. The bioassay-guided isolation from IB-F002C afforded a glucocerebroside, which showed 10.51%, 12.19%, 16.14%, and 34.05% inhibition of head and neck, breast-1, colon-1, and ovarian cancer cell lines, respectively. Octadecyl coumarate, 7-hydroxycoumarin, and 6-methoxy-7-hydroxycoumarin that showed different antioxidant potentials were also identified in this study. Sweet potato peel, which is usually discarded as waste, contains constituents that can serve as dietary components to prevent the development of different types of cancer.