Strategies for developing retinoic acid receptor alpha-selective antagonists as novel agents for male contraception.

Reported here are the synthesis and in vitro evaluation of a series of 26 retinoic acid analogs based on dihydronaphthalene and chromene scaffolds using a transactivation assay. Chromene amide analog 21 was the most potent and selective retinoic acid receptor α antagonist identified from this series. In vitro evaluation indicated that 21 has favorable physicochemical properties and a favorable pharmacokinetic PK profile in vivo with significant oral bioavailability, metabolic stability, and testes exposure.

Energy generation from bioelectrochemical techniques: Concepts, reactor configurations and modeling approaches.

The process industries play a significant role in boosting the economy of any nation. However, poor management in several industries has been posing worrisome threats to an environment that was previously immaculate. As a result, the untreated waste and wastewater discarded by many industries contain abundant organic matter and other toxic chemicals.

Hydrothermal carbonization of Typha australis: Influence of stirring rate.

According to existing literature, there are no conclusive results on the impact of stirring on hydrothermal carbonization (HTC); some studies report a significant impact on the product's properties, while others indicate no influence. This study investigates the influence of stirring rate on several responses and properties of HTC products, including solid mass yield, solid carbon fraction, surface area, surface functional groups, morphology, and the fate of inorganic elements during HTC. Waste biomass was introduced as a feedstock to a 2 L HTC reactor, where the effects of temperature (180-250 °C), residence time (4-12 h), biomass to water (B/W) ratio (1-10%), and stirring rate (0-130 rpm) were investigated.

Investigation of selective retinoic acid receptor alpha antagonist ER-50891 and related analogs for male contraception.

Retinoic acid receptor alpha (RARα) antagonist ER-50891 and 15 analogs were prepared and tested in vitro for potency and selectivity at RARα, RARβ, and RARγ using transactivation assays. Minor modifications to the parent molecule such as the introduction of a C4 tolyl group in place of the C4 phenyl group on the quinoline moiety slightly increased the RARα selectivity but larger substituents significantly decreased the potency. Replacement of the pyrrole moiety of ER-50891 with triazole, amides, or a double bond produced inactive compounds.

Nutritional status of under-five aged children of ready-made garment workers in Bangladesh: A cross-sectional study.

Background: The ready-made garment (RMG) sector is a significant contributor to the economic growth of Bangladesh, accounting for 10% of the country's GDP and more than 80% of its foreign exchange earnings. The workforce in this sector is predominantly made up of women, with 2.5 million women working in the industry.

Evaluation of (L.) Roxb. leaves as source of bioactive molecules with antioxidant, anti-inflammatory and antibacterial potential.

(L.) Roxb. is an ethno-medicinal herb used by rural and tribal people of the Satpura region of Madhya Pradesh in India and the Phatthalung Province of Thailand for treating rheumatism, bronchitis, ringworm, itches, leprosy, dyspepsia, liver disorders and heart disorders.

Cytotoxicity of phenylpironetin analogs and the metabolic fate of pironetin and phenylpironetin.

To improve pironetin's metabolic stability we prepared four analogs by replacing its C12-14 segment with an aryl group. The antiproliferative activity of phenyl analog 4 was reduced two-fold and dihydroxy-4-fluorophenyl analog 5 was slightly more effective against OVCAR5 and A2780 ovarian cancer cell lines compared with the parent compound pironetin (1). The activity of 4-fluorophenyl analog 6 was reduced 3-fold in both cell lines.

Curcuma longa L. Prevents the Loss of β-Tubulin in the Brain and Maintains Healthy Aging in Drosophila melanogaster.

Loss of tubulin is associated with neurodegeneration and brain aging. Turmeric (Curcuma longa L.) has frequently been employed as a spice in curry and traditional medications in the Indian subcontinent to attain longevity and better cognitive performance.

Elucidating genetic diversity and population structure of Pyricularia oryzae isolates causing wheat blast in Bangladesh.

Wheat blast, caused by Pyricularia oryzae pathotype Triticum, is one of the most notorious diseases of wheat. In this study, a total of twenty-four monoconidial isolates representing four major wheat blast affected districts, namely Chuadanga, Meherpur, Kustia and Jhenaidah of Bangladesh were analyzed. Eight RAPD and four ISSR primers being used for genetic diversity assay produced a total of 94 bands of which 85% were polymorphic.

Computational assessment of MCM2 transcriptional expression and identification of the prognostic biomarker for human breast cancer.

Minichromosome maintenance protein 2 (MCM2) is a highly conserved protein from the MCM protein family that plays an important role in eukaryotic DNA replication as well as in cell cycle progression. In addition, it maintains the ploidy level consistency in eukaryotic cells, hence, mutations or alteration of this protein could result in the disintegration of the fine-tuned molecular machinery that can lead to uncontrolled cell proliferation. Moreover, MCM2 has been found to be an important marker for progression and prognosis in different cancers.

Reusing greywater for cultivation of Capsicum frutescens and Calendula officinalis.

This study investigated the impact of greywater application for home yard gardening. Greywater was collected and treated using screening, sedimentation and solar disinfection methods. Finally, a field experiment was conducted to investigate the impact of untreated and treated greywater on a selected vegetable, Capsicum frutescens and flowering plant, Calendula officinalis for 2 months.

Retinoic acid receptor antagonists for male contraception: current status†.

Retinoic acid receptor alpha (RARA), a nuclear receptor protein, has been validated as a target for male contraception by gene knockout studies and also pharmacologically using a pan-retinoic acid receptor antagonist. Retinoic acid receptor alpha activity is indispensable for the spermatogenic process, and therefore its antagonists have potential as male contraceptive agents. This review discusses the effects of systematic dosing regimen modifications of the orally bioavailable and reversible pan-antagonist BMS-189453 as well as studies with the alpha-selective antagonists BMS-189532 and BMS-189614 in a murine model.

Crispenes F and G, cis-Clerodane Furanoditerpenoids from Tinospora crispa, Inhibit STAT3 Dimerization.

Two new cis-clerodane-type furanoditerpenes, crispenes F and G (1 and 2), together with seven known compounds, were isolated from the stems of Tinospora crispa. Crispenes F and G (1 and 2) inhibited STAT3 dimerization in a cell-free fluorescent polarization assay and were found to have significant cytotoxicity against a STAT3-dependent MDA-MB 231 breast cancer cell line, while being inactive in a STAT3-null A4 cell line. These two compounds share structural similarities with a previously reported STAT3 inhibitor, crispene E, isolated from the same plant.