Discovery and prospects of new heterocyclic Isatin-hydrazide derivative with a novel role as estrogen receptor α degrader in breast cancer cells.

Isatin, a heterocycle scaffold, is the backbone of many anticancer drugs and has previously been reported to engage multiple cellular targets and mechanisms, including angiogenesis, cell cycle, checkpoint pathways and multiple kinases. Here, we report that a novel isatin derivative, 5i, degrades estrogen receptor alpha (ERα) in estrogen-dependent breast cancer cells. This effect of the isatin nucleus has not been previously reported.

The in vitro study of interaction between antacids and anti-diabetic drug sitagliptin in the treatment of type II diabetes.

Hyperglycemia is a long-lasting syndrome that occurs either when the pancreas cannot produce enough insulin, or the body cannot effectively utilize that insulin to regulate blood sugar levels. Non-insulin-dependent hyperglycemia, also known as type II diabetes, causes a common consequence of severe damage to many of the body's organs mainly the blood vessels and nerves. The majority of people around the world are suffering from non-insulin-dependent diabetes.

Comparison of Microscopy, Card Agglutination Test for , and Real-time PCR in The Diagnosis of Trypanosomosis in Dromedary Camels of The Abu Dhabi Emirate, UAE.

Introduction: Trypanosomosis is an important disease of dromedary camels caused by the pathogenic protozoan . This study aimed to compare three different tests for its diagnosis in this species: conventional microscopy, the card agglutination test for trypanosomosis/ (CATT/) and real-time PCR.

Material And Methods: Whole blood and serum samples collected from 77 dromedary camels of Abu Dhabi, United Arab Emirates, were analysed with the test methods stated.

Systematic evidence of health economic evaluation of drugs for postmenopausal osteoporosis: A quality appraisal.

This paper systematically and critically reviewed all published economic evaluations of drugs for the treatment of postmenopausal osteoporosis. A systematic search was conducted using relevant databases for economic evaluations to include all relevant English articles published between January 2008 to January 2020. After extracting the key study characteristics, methods and outcomes, we evaluated each article using the Quality of Health Economic Studies (QHES) and the Consolidated Health Economic Evaluation Reporting Standards (CHEERS) instruments.

Recurrent aseptic meningitis: A rare clinical presentation of Sjogren's syndrome.

Sjogren's syndrome most commonly presents with dry eyes, dry mouth, joint pain and fatigue. However, recurrent aseptic meningitis, reported as the most uncommon initial symptom, was the presenting feature in our case. We present the case of a 19-year-old female with recurrent episodes of aseptic meningitis.

Effect of anti-diabetic drugs on bone metabolism: Evidence from preclinical and clinical studies.

Diabetes mellitus is associated with abnormal bone health and an increased risk of fracture even though patients have normal or higher BMD. The mechanisms behind diabetes mellitus- induced various skeletal disorders remain unclear. Anti-diabetic drugs may have negative or positive impact on bone metabolism.

Effect of orlistat on periostin, adiponectin, inflammatory markers and ultrasound grades of fatty liver in obese NAFLD patients.

Orlistat is recommended in the treatment of obesity, which is an independent risk factor for nonalcoholic fatty liver disease (NAFLD). The reported findings of orlistat in NAFLD are divisive. Recently, periostin is identified as an important regulatory molecule in the pathogenesis of obesity-induced fatty liver.

Neuroprotective Role of Steroidal Sex Hormones: An Overview.

Progesterone, estrogens, and testosterone are the well-known steroidal sex hormones, which have been reported to have "nonreproductive "effects in the brain, specifically in the neuroprotection and neurotrophy. In the last one decade, there has been a surge in the research on the role of these hormones in neuroprotection and their positive impact on different brain injuries. The said interest has been sparked by a desire to understand the action and mechanisms of these steroidal sex hormones throughout the body.

Nematicidal natural products from the aerial parts of Buddleja crispa.

Studies on the aerial parts of Buddleja crispa yielded 13 known compounds, nonyl benzoate, hexyl p-hydroxy-cinnamate, ginipin, gardiol, 1-heptacosanol, steroidal galactoside (22 R)-stigmasta-7,9 (11)-dien-22 beta-ol-3beta-O-beta-D-galactopyranoside, 3-methoxy benzoic acid, beta-sitosterol and ursolic acid. Besides this two iridoid galactosides buddlejosides A, buddlejosides B and a benzofuran-type sesquiterpene buddlejone have been isolated from the ETOAC fraction of B. crispa.

2,2-Bis(hy-droxy-meth-yl)-2,3-dihydro-1H-pyrrolizin-1-one.

The title compound, C(9)H(11)NO(3), was prepared by an Aldol reaction of 2,3-dihydro-1H-pyrrolizin-1-one with formaldehyde. The asymmetric unit contains six mol-ecules. The pyrrolizine ring system in each mol-ecule is planar, the maximum atomic deviation being 0.

Antimicrobial activity of various parts of Polyalthia longifolia var. pendula: isolation of active principles from the leaves and the berries.

Methanol extracts of leaves, stem, twigs, green berries, flowers, roots, root-wood and root-bark of Polyalthia longifolia var. pendula, were tested for their antibacterial and antifungal potentials. Bioassay monitored isolation work on the methanol extract of leaves and berries which possess promising antibacterial activity led to the isolation of seven clerodane diterpenoids, 16(R and S)-hydroxy-cleroda-3,13(14)Z-dien-15,16-olide (1), 16-oxo-cleroda-3,13(14)E-dien-15-oic acid (2), methyl-16-oxo-cleroda-3,13(14)E-dien-15-oate (3), 2-oxo-kolavenic acid (4), 16 (R and S)-hydroxy-cleroda-3,13(14)Z-dien-15,16-olide-2-one (5), (4-->2)-abeo-16(R and S)-hydroxy-cleroda-2,13(14)Z-dien-15,16-olide-3-al (6), 3beta,16alpha-dihydroxy-cleroda-4(18), 13(14)Z-dien-15,16-olide (7), while kolavenic acid (8) and solidagonal acid (9) were obtained from the root-wood.

Hypotensive activity and toxicology of constituents from root bark of Polyalthia longifolia var. pendula.

A defatted extract of Polyalthia longifolia var. pendula root bark (PRB) in 50% methanol showed a significant ability to reduce blood pressure. It caused a 22% and 47% fall in mean arterial blood pressure (MABP) in rats at doses of 3 mg/kg and 30 mg/kg, respectively.

Evaluation of the antimicrobial property of Polyalthia longifolia var. pendula: isolation of a lactone as the active antibacterial agent from the ethanol extract of the stem.

Bioassay guided fractionation of the ethanolic extract of Polyalthia longifolia var. pendula stem, which showed promising antibacterial activity against thirteen Gram-positive and nine Gram-negative organisms, furnished (3S,4R)-3,4,5-trihydroxypentanoic acid-1,4-lactone (1) as the active principle. The structure of (1) was established by UV, IR, mass, 1H and 13C NMR as well as 2D NMR spectral studies and the formation of its acetate (1a).

New antimicrobial alkaloids from the roots of Polyalthia longifolia var. pendula.

Bioassay-guided isolation studies on the root extract of Polyalthia longifolia var. pendula possessing significant antibacterial activity led to the isolation of three new alkaloids pendulamine A (1), pendulamine B (2) and penduline (3) along with stigmasterol 3-O-beta-D-glucoside, allantoin, the known diterpenoid kolavenic acid, and the azafluorene alkaloid isoursuline. The structures of these compounds have been elucidated with the help of spectroscopic studies including 2D NMR experiments.