Synthesis and characterization of gold(I) thiolate derivatives and bimetallic complexes for HIV inhibition.

The human immunodeficiency virus (HIV) remains a significant global health concern, with a reported high infection rate of 38.4 million cases globally; an estimated 2 million new infections and approximately 700,000 HIV/AIDS-related deaths were reported in 2021. Despite the advent of anti-retroviral therapy (ART), HIV/AIDS persists as a chronic disease.

Alkaloidal Extracts from P. Beauv. (Avicenniaceae) Leaf: An Antiplasmodial, Antioxidant, and Erythrocyte Viable.

Background: The emergence of drug-resistant parasites impedes disease management and eradication efforts. Hence, a reinvigorated attempt to search for potent lead compounds in the mangroves is imperative.

Aim: This study evaluates antiplasmodial activity, antioxidant properties, and cytotoxicity of leaf alkaloidal extracts.

In Vitro and In Vivo Toxicological Evaluation of P: Beauv. (Avicenniaceae) Leaf Extract in a Rat Model.

is an important ethnomedicinal plant that has long been used to treat malaria and several other diseases. Despite the plant's antimalarial and other therapeutic properties, there is limited evidence-based data on its potential toxicity. Hence, the purpose of the current study was to assess the safety of leaf ethanolic extract (AAE).

and antimalarial activities of P. Beauv. (Avicenniaceae) ethanolic leaf extract.

Background: The emergence of widespread drug-resistant strains of the malaria parasites militates against strives for more potent antimalarial drugs.

Aim: The present study evaluated the antimalarial activity of ethanolic crude extract and against -infected mice in anticipation of acquiring scientific evidence for it used by mangrove dwellers to treat malaria in Ghana.

Methodology: The pulverized dried leaves were extracted with 70% ethanol (v/v) and screened for phytochemicals using standard protocols.

Glyco disulfide capped gold nanoparticle synthesis: cytotoxicity studies and effects on lung cancer A549 cells.

Glyco disulfide gold nanoparticles (GDAuNPs) were prepared by three methods: direct, photochemical irradiation and ligand substitution. Glyco disulfide acted as reducing and capping agents of gold ions, to produce AuNPs . Shorter chains of glyco disulfides (n = 1 and 2) offered monodispersed and stable GDAuNPs in physiological pH, while longer chains (n = 3) furnished unstable nanoparticles.

Antidepressant and Anxiolytic Effects and Subacute Toxicity of the Aerial Parts of J.B.Hall (Rubiaceae) in Murine Models.

Background: The present study aimed at validating the traditional use and toxicity profile of a methanolic extract of the aerial parts of in alleviating depression and anxiety disorders.

Method: The antidepressant effect of methanolic extract of (PAE 30, 100, and 300 mg/kg, .) was assessed in mice using the forced swim test (FST) and the tail suspension test (TST).

Alkaloidal extract from stimulates insulin secretion in normoglycemic and nicotinamide/streptozotocin-induced diabetic rats.

Introduction: Increase in the prevalence of type-2 diabetes in Sub-Sahara Africa has created the need for robust treatment and management programs. However, an effective diabetes management program requires a high annual budget that most countries in this region cannot afford. That said, various plants and plant products in this region have either been confirmed and/or ethnopharmacologically used for the management of type-2 diabetes.

Seed Extract Attenuates the Ethanol-Induced Gastric Ulcer in Rats via the Inhibition of TNF- and INF- Levels and Modulation in the Expression of Ki67 Protein.

has been used to treat an upset stomach in African traditional medicine, but its efficacy and safety have not been scientifically studied. The present research is aimed at assessing the antiulcer property of the seed extract of the plant to validate its traditional claim. Rats were pretreated with three doses of aqueous extract of .

Development and characterization of functionalized glyco thiolate capped gold nanoparticles for biological applications.

Glyco-gold nanoparticles (AuNPs) in aqueous dispersions were prepared by two approaches, namely direct reduction and ligand substitution methods. In the direct method, potassium salts of glyco thiols, with the general formula (CHO)NH(CH) CHSK (where , = 1; , = 2; , = 3, , = 4; , = 5), were used as reducing and capping agents to give the glyco thiolate capped gold nanoparticles (AuNPs -); meanwhile in the ligand exchange experiments, - and their acetylated forms (-) replaced citrate ions in citrate-capped gold nanoparticles to give additional AuNPs -. UV-visible spectroscopy, surface charge (-potential,) measurements and transmission electron microscopy (TEM) were used for physical and chemical characterization of all the resultant AuNPs.

Structural elucidation and in vivo anti-arthritic activity of β-amyrin and polpunonic acid isolated from the root bark of Ziziphus abyssinica HochstEx. A Rich (Rhamnaceae).

Two natural products, compounds 1 and 2 were isolated from the root bark of Ziziphus abyssinica for the first time and were structurally elucidated as β-amyrin and polpunonic acid, respectively. Both compounds were further subjected to an in vivo study in rats to evaluate their anti-arthritic potency. Compared to the arthritic control group, rats treated with different doses of 1 or 2 (3, 10, and 30 mg/kg) exhibited significantly higher total change in body weight as well as lower arthritic scores and total change in paw edema and erythema.

Therapeutic potential of dithiocarbamate supported gold compounds.

Chrysotherapy or aurotherapy, the use of gold as medicine, is two thousand years old. Hitherto, numerous diverse gold stabilizing ligands for instance vitamins, pyridine, phosphines, naphthylamine and xanthanes have been developed and their 'chelating effect' in addition to their anti-proliferative properties have been extensively studied. Recent advances in the field of bioinorganic chemistry have led to the design of biologically relevant metal complexes with appropriate fine-tuned ligands such as metallic conjugates of dithiocarbamates (DTCs).

Histoprotective Effect of Essential Oil from in Testosterone-Induced Benign Prostatic Hyperplasia Rat.

Background: Benign prostatic hyperplasia (BPH) is a common urological disorder reported among ageing men.

Objective: The study assessed histoprotective effect of lime essential oil (LEO) in a rat model of testosterone-induced benign prostatic hyperplasia (BPH) and evaluated its ability to reverse testosterone-mediated changes in the testis, kidney, and liver.

Materials And Methods: Adult Sprague Dawley (aged 12 weeks, 240-390 g) male rats were intramuscularly injected with testosterone enanthate (TE) (10 mg/kg) reconstituted in olive oil for ten days to establish benign prostatic hyperplasia (serum PSA level ≥ 1.

Chemical profile and toxicity evaluation of unripe essential oil.

(Christm.) Swingle (syn. C.

Anti-inflammatory, anti-nociceptive and antipyretic activity of young and old leaves of Vernonia amygdalina.

Background: Both young and old leaves of Vernonia amygdalina (VA) are traditionally used to treat inflammation, pain and fever. However, the efficacy of young and old leaves for treating these ailments have not been compared till date.

Aim: To ascertain the effect of young and old leaves of VA in managing inflammation, pain and fever.

Relating High Insecticide Residues in Larval Breeding Habitats in Urban Residential Areas to the Selection of Pyrethroid Resistance in Anopheles gambiae s.l. (Diptera: Culicidae) in Akim Oda, Ghana.

The main objective of this study was to assess insecticide contamination in Anopheles breeding habitats in urban residential areas and pyrethroid susceptibility status of mosquitoes found in the habitats. A larval survey was conducted in Akim Oda between July and October 2016. The larvae that were reared to adult were used for susceptibility test against four different pyrethroid insecticides (deltamethrin 0.

Immunotherapy for acute myeloid leukemia (AML): a potent alternative therapy.

The standard therapy of AML for many years has been chemotherapy with or without stem transplantation. However, there has not been any tangible improvement in this treatment beyond induction through chemotherapy and consolidation with allogeneic stem cell transplantation or chemotherapy. Residual AML cells which later cause relapse mostly persist even after rigorous standard therapy.

Leishmanicidal activity of the root bark of Erythrophleum Ivorense (Fabaceae) and identification of some of its compounds by ultra-performance liquid chromatography quadrupole time of flight mass spectrometry (UPLC-QTOF-MS/MS).

Ethnopharmacological Relevance: Leishmaniasis is one of the neglected tropical disease caused by a protozoan of the genus Leishmania transmitted by sandflies. High cost and lack of oral formulation of existing drugs, rapid developments of resistance by the parasite coupled with serious side effects require new treatments to augment or replace currently available therapies. The major merits of herbal medicine seem to demonstrate perceived efficacy, low incidence of serious adverse effects and low cost.

Recent development and biomedical applications of self-healing hydrogels.

Introduction: Hydrogels are of special importance, owing to their high-water content and various applications in biomedical and bio-engineering research. Self-healing properties is a common phenomenon in living organisms. Their endowed property of being able to self-repair after physical/chemical/mechanical damage to fully or partially its original properties demonstrates their prospective therapeutic applications.

Bispecific Antibodies (bsAbs): Promising Immunotherapeutic Agents for Cancer Therapy.

Antibodies have become the preferred therapeutic treatment option for cancers. Antibody therapy is associated with low toxic profile and specific in its activity, unlike chemotherapy and radiotherapy. Types of tumor are known to express multiple receptors that cross-talk to activate perpetual growth, proliferation and metastasis, and inhibit apoptosis in such tumors.

Synthetic Approach to Glycopolymer Base Nanoparticle Gold(I) Conjugate: A New Generation of Therapeutic Agents.

Advances in nanotechnology have led to the fabrication of nano-constructs of organic or inorganic origins with well-defined structures, surface properties, and can be made to respond to physical or chemical stimuli. These nano-constructs can provide a shift in the way diagnostic and therapeutic drugs are delivered to achieve target specificity and increased retention of therapeutic doses for considerable improvement in the overall treatment of the tumors. In this case we describe here a synthetic approach to glycopolymer base nanoparticle gold(I) conjugate for cancer therapy.

Synthetic Approach to Biotinylated Glyco-Functionalized Quantum Dots: A New Fluorescent Probes for Biomedical Applications.

Technological advances that allow deeper penetration in live tissues, such as the development of confocal and the generation of ever-new fluorophores that facilitate bright labeling of cells and tissue components have made imaging of vertebrate model organisms efficient and highly informative. Recently, high luminescence, single-excitation narrow emission, low photo bleaching properties, and low toxicity of high-quality water-soluble QDs have attracted attention for in vivo labeling/imaging of cells. Herein we describe a synthetic approach to biotinylated glycopolymer functionalized quantum dots, with special emphasis on the development of high-quality water-soluble and bioactive QDs with low toxicity for fluorescent probes in biomedical applications.

Synthesis and evaluation of glycopolymeric decorated gold nanoparticles functionalized with gold-triphenyl phosphine as anti-cancer agents.

In this study, statistical glyco-dithiocarbamate (DTC) copolymers were synthesized by reversible addition-fragmentation chain transfer polymerization (RAFT) and subsequently used to prepare glyconanoparticles and conjugated glyconanoparticles with the anticancer drug, gold(I) triphenylphosphine. These glyconanoparticles and the corresponding conjugates were then tested for their in vitro cytotoxicity in both normal and cancer cell lines using Neutral Red assay. The glyconanoparticles and their Au(I)PPh3 conjugates were all active against MCF7 and HepG2 cells, but galactose-functionalized glyconanoparticles {P(GMA-EDAdtc(AuPPh3)-st-LAEMA)AuNP} were found to be the most cytotoxic to HepG2 cells (IC50 ∼ 4.

Regiospecific synthesis of 2-halo-3-(2'-glucalyl)benzo[b]thiophenes.

A regiospecific synthetic strategy for the synthesis of 2-chloro-3-substituted benzo[b]thiophenes is developed via a dichlorocarbene insertion and sigmatropic rearrangement of an in situ generated ylide. The current protocol provides a reversed regiochemistry to the commonly employed electrophilic cyclization reaction for the synthesis of benzo[b]thiophenes and access to their hitherto under-represented chlorinated derivatives.

Therapeutic potential of carbohydrate-based polymeric and nanoparticle systems.

Introduction: Carbohydrates are key participants in many biological processes including reproduction, inflammation, signal transmission and infection. Their biocompatibility and ability to be recognized by cell-surface receptors illustrate their potential therapeutic applications. αYet, they are not ideal candidates because they are complex and tedious to synthesize.