Isolation of Lessertiosides A and B and Other Metabolites from and Their Neuroprotection Activity.

(synonym ) is an important South African medicinal plant used traditionally to treat different human pathologies and is considered an adaptogenic plant. This study sought to isolate compounds from the plant and determine their protective potentials using SH-SY5Y cells and MPP (1-methyl-4-phenylpyridinium) to mimic Parkinson's disease. The phytochemical analysis of a 70% aqueous methanolic extract of leaves resulted in the isolation and identification of 11 pure compounds (-), among which compounds and were identified as new metabolites.

Neuroprotective Effects of Total Extract and Isolated Compounds.

L. is a plant commonly utilized in herbal medicine and stands out as one of the more extensively researched medicinal plants globally. It has been documented with respect to several pharmacological activities, notably, neuroprotective effects, among others.

A Systematic Review and Meta-Analysis of the Prevalence of Triplex Infections (Combined Human Immunodeficiency Virus, Hepatitis B Virus, and Hepatitis C Virus) among Pregnant Women in Nigeria.

Objective: We systematically identified the prevalence of triplex infections (combined human immunodeficiency virus (HIV), hepatitis B virus (HBV), and hepatitis C virus (HCV)) in pregnancy.

Methods: To gather information on the frequency of triplex infections, we searched the databases of PubMed, CINAHL, and Google Scholar. Without regard to language, we utilized search terms that covered HIV, HBV, HCV, and pregnancy.

Fractions of Hoslundia opposita Vahl and hoslundin induced apoptosis in human cancer cells via mitochondrial-dependent reactive oxygen species (ROS) generation.

Background: Cancer remains one of the leading causalities of several morbidity and mortality with negative impact on global economy due to low workforce and management/treatment cost. A number of conventional therapies have been explored in the management/treatment of cancer including chemotherapeutic intervention, radiotherapy, and surgery. Among these treatment modalities, chemotherapy remains the most popular first line of intervention in management/treatment of cancer, and natural products have been implicated as the main source of antineoplastic agents with phenomenal efficacy.

Mother-to-child transmission of human immunodeficiency virus, hepatitis B virus and hepatitis C virus among pregnant women with single, dual or triplex infections of human immunodeficiency virus, hepatitis B virus and hepatitis C virus in Nigeria: A systematic review and meta-analysis.

To systematically review literature and identify mother-to-child transmission rates of human immunodeficiency virus, hepatitis B virus, and hepatitis C virus among pregnant women with single, dual, or triplex infections of human immunodeficiency virus, hepatitis B virus, and hepatitis C virus in Nigeria. PRISMA guidelines were employed. Searches were on 19 February 2021 in PubMed, Google Scholar and CINAHL on studies published from 1 February 2001 to 31 January 2021 using keywords: "MTCT," "dual infection," "triplex infection," "HIV," "HBV," and "HCV.

Pregnant women's hepatitis B vaccination coverage in Nigeria: a national pilot cross-sectional study.

Objective: To determine the hepatitis B vaccination coverage, full-dose (⩾3) coverage and the associated factors affecting uptake among pregnant women.

Methods: This was a cross-sectional study among pregnant women attending antenatal care in six tertiary hospitals across all the geopolitical zones of Nigeria. Pregnant women who consented to the study completed screening questions about their hepatitis B vaccination status and coverage.

Design, synthesis, and evaluation of 3,7-substituted coumarin derivatives as multifunctional Alzheimer's disease agents.

Multitarget directed ligands (MTDLs) are emerging as promising treatment options for Alzheimer's disease (AD). Coumarin derivatives serve as a good starting point for designing MTDLs due to their inherent inhibition of monoamine oxidase (MAO) and cholinesterase enzymes, which are complicit in AD's complex pathophysiology. A preliminary series of 3,7-substituted coumarin derivatives were synthesised and evaluated for enzyme inhibitory activity, cytotoxicity as well as neuroprotective ability.

Awareness and prevalence of hepatitis C virus infection among pregnant women in Nigeria: A national pilot cross-sectional study.

Background: There are no national data on hepatitis C virus awareness and burden among pregnant women to justify its routine screening.

Objectives: To investigate awareness, seroprevalence and risk factors for hepatitis C virus infection among pregnant women in Nigeria.

Methods: A total of 159 pregnant women from antenatal clinics across six geopolitical zones in Nigeria consented to anti-hepatitis C virus testing which was confirmed using polymerase chain reaction technique.

Neuroprotective Activities of Bulbs and Amaryllidaceae Alkaloids: Implications for Parkinson's Disease.

Parkinson's disease (PD) is one of the most common neurodegenerative diseases and affects approximately 6.3 million people worldwide. To date, the treatment of PD remains a challenge, as available treatment options are known to be associated with serious side effects; hence, the search for new treatment strategies is critical.

Neuroprotective Activities of (Amaryllidaceae) Extract and Its Chemical Constituents.

Parkinson's disease (PD) is a neurodegenerative condition that progresses as age increases, and some of its major symptoms include tremor and postural and movement-related difficulties. To date, the treatment of PD remains a challenge because available drugs only treat the symptoms of the disease or possess serious side effects. In light of this, new treatment options are needed; hence, this study investigates the neuroprotective effects of an organic extract (BHE) and its bioactive compounds using an in vitro model of PD involving the toxin 1-methyl-4-phenylpyridinium (MPP) and SH-SY5Y neuroblastoma cells.

4-Oxatricyclo[5.2.1.0]dec-8-ene-3,5-dione Derivatives as NMDA Receptor- and VGCC Blockers with Neuroprotective Potential.

The impact of excitotoxicity mediated by -methyl-D-aspartate (NMDA) receptor overactivation and voltage gated calcium channel (VGCC) depolarization is prominent among the postulated processes involved in the development of neurodegenerative disorders. NGP1-01, a polycyclic amine, has been shown to be neuroprotective through modulation of the NMDA receptor and VGCC, and attenuation of MPP-induced neurotoxicity. Recently, we reported on the calcium modulating effects of tricycloundecene derivatives, structurally similar to NGP1-01, on the NMDA receptor and VGCC of synaptoneurosomes.

Prevalence, seroconversion and mother-to-child transmission of dual and triplex infections of HIV, hepatitis B and C viruses among pregnant women in Nigeria: study protocol.

Background: Nigeria contributes significantly to the global burden of HIV, Hepatitis B and C infections, either singly or in combinations, despite progress in HIV care regionally and globally. Although some limited data on mono infection of HIV, Hepatitis B and C virus infections do exists, that of dual and triplex infections, including seroconversion and mother-to-child transmission (MTCT) rates necessary for planning to address the scourge of infections in pregnancy are not available.

Objectives: To determine the seroprevalence, rate of new infections, MTCT of dual and triple infections of HIV, Hepatitis B and C viruses and associated factors, among pregnant women in Nigeria.

Open and rearranged norbornane derived polycyclic cage molecules as potential neuroprotective agents through attenuation of MPP- and calcium overload-induced excitotoxicity in neuroblastoma SH-SY5Y cells.

The neuroprotective effects of closed polycyclic cage molecules such as NGP1-01, memantine and amantadine have been extensively explored. These effects are mostly linked to the antagonism of the N-methyl-d-aspartate (NMDA) receptor- and the blockage of voltage gated calcium channels (VGCC). The synthesis of structurally related open and rearranged cage derivatives has been studied in depth.

Exploitation of a novel phenothiazine derivative for its anti-cancer activities in malignant glioblastoma.

Glioblastoma remains the most malignant of all primary adult brain tumours with poor patient survival and limited treatment options. This study adopts a drug repurposing approach by investigating the anti-cancer activity of a derivative of the antipsychotic drug phenothiazine (DS00329) in malignant U251 and U87 glioblastoma cells. Results from MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) and clonogenic assays showed that DS00329 inhibited short-term glioblastoma cell viability and long-term survival while sparing non-cancerous cells.

GRP78/BIP/HSPA5 as a Therapeutic Target in Models of Parkinson's Disease: A Mini Review.

Parkinson's disease (PD) is a common neurodegenerative disorder characterized by selective loss of dopamine neurons in the substantia nigra pars compacta of the midbrain. Reports from postmortem studies in the human PD brain, and experimental PD models reveal that endoplasmic reticulum (ER) stress is implicated in the pathogenesis of PD. In times of stress, the unfolded or misfolded proteins overload the folding capacity of the ER to induce a condition generally known as ER stress.

Design, synthesis and evaluation of pentacycloundecane and hexacycloundecane propargylamine derivatives as multifunctional neuroprotective agents.

The multifactorial pathophysiology of neurodegenerative disorders remains one of the main challenges in the design of a single molecule that may ultimately prevent the progression of these disorders in affected patients. In this article, we report on twelve novel polycyclic amine cage derivatives, synthesized with or without a propargylamine function, designed to possess inherent multifunctional neuroprotective activity. The MTT cytotoxicity assay results showed the SH-SY5Y human neuroblastoma cells to be viable with the twelve compounds, particularly at concentrations less than 10 μM.

Design, synthesis and evaluation of indole derivatives as multifunctional agents against Alzheimer's disease.

A series of indole derivatives was designed and synthesised to improve on activity and circumvent pharmacokinetic limitations experienced with the structurally related compound, ladostigil. The compounds consisted of a propargylamine moiety (a known MAO inhibitor and neuroprotector) at the 1 position and a ChE inhibiting diethyl-carbamate/urea moiety at the 5 or 6 position of the indole ring. In order to prevent or slow down the hydrolysis and deactivation associated with the carbamate function of ladostigil, a urea moeity was incorporated into selected compounds to obtain more metabolically stable structures.

Versatility of 7-Substituted Coumarin Molecules as Antimycobacterial Agents, Neuronal Enzyme Inhibitors and Neuroprotective Agents.

A medium-throughput screen using H37Rv was employed to screen an in-house library of structurally diverse compounds for antimycobacterial activity. In this initial screen, eleven 7-substituted coumarin derivatives with confirmed monoamine oxidase-B and cholinesterase inhibitory activities, demonstrated growth inhibition of more than 50% at 50 µM. This prompted further exploration of all the 7-substituted coumarins in our library.

Long-term consumption of fermented rooibos herbal tea offers neuroprotection against ischemic brain injury in rats.

Stroke is the second leading cause of death worldwide, affecting about 240 people a day in South Africa and leaving survivors with residual disabilities. At the moment, there is no clinically approved neuroprotective product for stroke but the consumption of plant polyphenols has been suggested to offer some protection against stroke. In this study, we investigated the effects of long-term consumption of fermented rooibos herbal tea (FRHT) on ischemia/reperfusion (I/R)-induced brain injury in adult male Wistar rats.

Pharmacokinetic interactions between ritonavir and quinine in healthy volunteers following concurrent administration.

Aims: To evaluate the pharmacokinetic interactions between ritonavir and quinine in healthy volunteers.

Methods: Ten healthy volunteers were each given 600-mg single oral doses of quinine alone, ritonavir alone (200 mg every 12 h for 9 days), and quinine in combination with ritonavir, in a three-period pharmacokinetic nonrandomized sequential design study. Quinine was co-administered with the 15th dose of ritonavir.

Effects of concurrent administration of nevirapine on the disposition of quinine in healthy volunteers.

Objectives: Nevirapine and quinine are likely to be administered concurrently in the treatment of patients with HIV and malaria. Both drugs are metabolised to a significant extent by cytochrome P450 (CYP)3A4 and nevirapine is also an inducer of this enzyme. This study therefore evaluated the effect of nevirapine on the pharmacokinetics of quinine.

Simultaneous liquid chromatographic analysis of ritonavir, quinine and 3-hydroxyquinine in human plasma.

In regions with high prevalence of HIV and malaria, co-infection of both diseases is common; hence, there is a high possibility of concurrent administration of antiretroviral and antimalarial drugs. This study describes a new ion-pair reversed-phase high-performance liquid chromatographic (HPLC) method for simultaneous determinations of ritonavir (RTV), quinine (QN), and its major metabolite, 3-hydroxyquinine (3-HQN), in human plasma. Following a simple extraction with diethyl-ether under alkaline conditions, chromatographic separation was achieved on a 5-mum particle size C-18 column (200 mm x 4.

Dissolution properties and characterization of halofantrine-2-hydroxypropyl-beta-cyclodextrin binary systems.

Halofantrine (HF) is a poorly water-soluble antimalarial drug with low bioavailability. Complex formation of HF.HCl and 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CD) in aqueous solution and in solid state as well as the possibility of improving the solubility and dissolution rate of the drug though complexation with the cyclodextrin were investigated.