The Polypharmacological Effects of Cannabidiol.

Cannabidiol (CBD) is a major phytocannabinoid present in (Linneo, 1753). This naturally occurring secondary metabolite does not induce intoxication or exhibit the characteristic profile of drugs of abuse from cannabis like Δ-tetrahydrocannabinol (∆-THC) does. In contrast to ∆-THC, our knowledge of the neuro-molecular mechanisms of CBD is limited, and its pharmacology, which appears to be complex, has not yet been fully elucidated.

Computationally Assisted Lead Optimization of Novel Potent and Selective MAO-B Inhibitors.

A series of dietary flavonoid acacetin 7--methyl ether derivatives were computationally designed aiming to improve the selectivity and potency profiles against monoamine oxidase (MAO) B. The designed compounds were evaluated for their potential to inhibit human MAO-A and -B. Compounds , , , and were the most potent with a Ki of 37 to 68 nM against MAO-B.

Identification of Human Kinin-Forming Enzyme Inhibitors from Medicinal Herbs.

The goal of this study was to assess the pharmacological effects of black tea ( var. assamica) water extract on human kinin-forming enzymes in vitro. Tea is a highly consumed beverage in the world.

Trichodermin Induces G0/G1 Cell Cycle Arrest by Inhibiting c-Myc in Ovarian Cancer Cells and Tumor Xenograft-Bearing Mice.

Ovarian cancer is a fatal gynecological cancer because of a lack of early diagnosis, which often relapses as chemoresistant. Trichodermin, a trichothecene first isolated from , is an inhibitor of eukaryotic protein synthesis. However, whether trichodermin is able to suppress ovarian cancer or not was unclear.

Proposed Mechanism for the Antitrypanosomal Activity of Quercetin and Myricetin Isolated from Lam.: Phytochemistry, In Vitro Testing and Modeling Studies.

The in vitro activity of (promastigotes, axenic amastigotes and intracellular amastigotes in THP1 cells) and , from the fractions obtained from the hydroalcoholic extract of the aerial part of and the isolated compounds, has been evaluated. The chloroform, ethyl acetate and -butanol extracts showed significant antitrypanosomal activity towards , with IC values of 12.35, 13.

On the Relationship between Hearing and Cognitive Limitations: Evidence from 51 Countries.

This study extends prior findings by looking at the relationship between hearing acuity and cognitive difficulties in 51 nations. We draw on data from the Integrated Public Use Microdata International Series available at the Institute for Social Research and Data Innovation at the University of Minnesota. For all countries where data are available, bivariate relationships between hearing and cognitive problems are examined using correlation coefficients () and multivariate relationships using linear regression techniques (betas), controlling for age, gender, marital status, and education.

Total Phenolic and Flavonoid Content and Biological Activities of Extracts and Isolated Compounds of Pourr.

The aim of this study was to evaluate the total phenolic and flavonoid content, and the in vitro antioxidant, anti-inflammatory, antibacterial, antifungal, antimalarial, cytotoxicity, and antiprotozoal activities of the Algerian plant Pourr. (Syn. L'Hérit.

Comparative Pharmacokinetics of Mitragynine after Oral Administration of Mitragyna speciosa (Kratom) Leaf Extracts in Rats.

Kratom () has been examined for its opioid activity, especially for the treatment of opioid withdrawal and pain. Mitragynine, the most abundant alkaloid in kratom, is thought to be the major psychoactive alkaloid. An HPLC method was developed for the quantification of mitragynine in kratom leaf extracts.

Computationally aided stereochemical assignment of undescribed bisabolenes from Calea urticifolia.

Calea urticifolia (Mill.) DC. (Compositae) is a medicinal plant found in El Salvador.

Secondary metabolites from the aerial parts of Pourr.

Phytochemical investigation of the aerial parts of Pourr. resulted in the isolation and characterization of a new isoflavan, ()-2',4'-dihydroxy-3'-methoxy-6,7-methylenedioxyisoflavan- 4-ol (), and a new monoterpene, ()-4-hydroxy-2,2,6-trimethyl-9-oxabicyclo [4.2.

Evaluation of Triazole and Isoxazole Derivatives as Potential Anti-infective Agents.

A series of isoxazole and triazole derivatives, with interesting bioactive scaffolds, were examined for their antibacterial, antifungal, and antiprotozoal activities. These compounds exhibited antitrypanosomal activity comparable to difluoromethylornithine (DMFO), a drug used in the treatment of human African trypanosomiasis. Isoxazole analogues , and , and triazole derivatives , , , , and showed the highest antitrypanosomal activity with IC values of 17.

The Relationship Between Psychosocial Status and Hypertensive Condition.

Purpose Of Review: The aim of the paper is to test the influence of social status and psychological well-being (independent variables) on hypertensive condition (dependent variable), when adjusting for traditional risk factors of cardiovascular disease (control variables). The analysis is based on data collected from SEPHAR III, a nationally representative epidemiologic study of the Romanian adult population.

Recent Findings: Understanding the social roots of health issues is of considerable importance in developing effective strategies and policies.

Structure-Based Identification of Potent Natural Product Chemotypes as Cannabinoid Receptor 1 Inverse Agonists.

Natural products are an abundant source of potential drugs, and their diversity makes them a rich and viable prospective source of bioactive cannabinoid ligands. Cannabinoid receptor 1 (CB1) antagonists are clinically established and well documented as potential therapeutics for treating obesity, obesity-related cardiometabolic disorders, pain, and drug/substance abuse, but their associated CNS-mediated adverse effects hinder the development of potential new drugs and no such drug is currently on the market. This limitation amplifies the need for new agents with reduced or no CNS-mediated side effects.

Abuse liability and therapeutic potential of the Mitragyna speciosa (kratom) alkaloids mitragynine and 7-hydroxymitragynine.

Kratom, derived from the plant Mitragyna speciosa, is receiving increased attention as an alternative to traditional opiates and as a replacement therapy for opiate dependence. Mitragynine (MG) and 7-hydroxymitragynine (7-HMG) are major psychoactive constituents of kratom. While MG and 7-HMG share behavioral and analgesic properties with morphine, their reinforcing effects have not been examined to date.

Inhibition of human monoamine oxidase A and B by flavonoids isolated from two Algerian medicinal plants.

Background: Monoamine oxidases (MAOs) are outer mitochondrial membrane flavoenzymes. They catalyze the oxidative deamination of a variety of neurotransmitters. MAO-A and MAO-B may be considered as targets for inhibitors to treat neurodegenerative diseases and depression and for managing symptoms associated with Parkinson's and Alzheimer's diseases.

Bioactive products from singlet oxygen photooxygenation of cannabinoids.

Photooxygenation of Δ tetrahydrocannabinol (Δ-THC), Δ tetrahydrocannabinol (Δ-THC), Δ tetrahydrocannabinolic acid (Δ-THCA) and some derivatives (acetate, tosylate and methyl ether) yielded 24 oxygenated derivatives, 18 of which were new and 6 were previously reported, including allyl alcohols, ethers, quinones, hydroperoxides, and epoxides. Testing these compounds for their modulatory effect on cannabinoid receptors CB and CB led to the identification of 7 and 21 as CB partial agonists with Ki values of 0.043 μM and 0.

Interactions of Desmethoxyyangonin, a Secondary Metabolite from , with Human Monoamine Oxidase-A and Oxidase-B.

(Zingiberaceae), a medicinal plant of tropical rainforests, is used to treat snakebites and other injuries and also as a febrifuge, analgesic, antiemetic, antiulcer, and anticonvulsant. The dichloromethane extract of leaves showed potent inhibition of human monoamine oxidases- (MAOs-) A and B. Phytochemical studies yielded six known compounds, including pinostrobin , 4'-methyl ether sakuranetin , sakuranetin , pinostrobin chalcone , yashabushidiol A , and desmethoxyyangonin .

Do Worries About Cognitive Functioning and Concerns About Developing Alzheimer's Disease Affect Psychological Well-Being?

Objective: The objective of this study is to determine if cognitive worries affect psychological well-being, if these effects are long-term, and if such concerns affect well-being more so among persons with a parent having Alzheimer's disease (AD).

Method: We used structural equation models with three waves of data collected from persons ages 40 to 60 at T. We created summative scores on five indicators of concerns about cognitive functioning and worries about dementia.

3-Hydroxyterphenyllin, a natural fungal metabolite, induces apoptosis and S phase arrest in human ovarian carcinoma cells.

In the present study, we evaluated 3-Hydroxyter-phenyllin (3-HT) as a potential anticancer agent using the human ovarian cancer cells A2780/CP70 and OVCAR-3, and normal human epithelial ovarian cells IOSE-364 as an in vitro model. 3-HT suppressed proliferation and caused cytotoxicity against A2780/CP70 and OVCAR-3 cells, while it exhibited lower cytotoxicity in IOSE-364 cells. Subsequently, we found that 3-HT induced S phase arrest and apoptosis in a dose-independent manner.

New triterpenoidal saponins from .

Bioassay guided fractionation and chemical investigation of the ethanolic extract of the aerial parts of Laxm. (Sapindaceae), resulted in the isolation and identification of three new triterpenoid saponins named Paniculatosoid A-C, along with eleven known compounds. The structures of the isolated compounds were elucidated using 1D and 2D NMR experiments, HRESIMS, and comparison with literature data.

Molecular Modeling Evaluation of the Enantiomers of a Novel Adenylyl Cyclase 2 Inhibitor.

Adenylyl cyclase 2 (AC2) is one of nine membrane-bound isoforms of adenylyl cyclase that converts ATP into cyclic AMP (cAMP), an important second messenger molecule. Upregulation of AC2 is linked to cancers like pancreatic and small intestinal neuroendocrine tumors (NETs). The structures of the various isoforms of adenylyl cyclases are highly homologous, posing a significant challenge to drug discovery efforts for an effective, isoform-selective modulator of AC2.

Quantitative Determination of Betaine, Choline, Acetylcholine, and 20-Hydroxyecdysone Simultaneously from Atriplex Species by UHPLC-UV-MS.

A simple, rapid, and sensitive UHPLC-UV-MS method was developed for the quantitative determination of betaine (1), choline (2), acetylcholine (3), and 20-hydroxyecdysone (4) from various species of Atriplex. The baseline separation of the four analytes was achieved on a reversed phase C 18 column within nine minutes. The mobile phase was composed of 50 mM ammonium formate in 2% methanol-water containing 5 mM sodium dodecyl sulfate (pH = 8.

Isolation of Acacetin from Calea urticifolia with Inhibitory Properties against Human Monoamine Oxidase-A and -B.

Calea urticifolia (Asteraceae: Asteroideae) has long been used as a traditional medicine in El Salvador to treat arthritis and fever, among other illnesses. The chloroform extract of the leaves of C. urticifolia showed potent inhibition of recombinant human monoamine oxidases (MAO-A and -B).

Chemical and Biological Study of Cladosporin, an Antimicrobial Inhibitor: A Review.

. Natural antifungal agents are generally broad-spectrum compounds with low mammalian and environmental toxicity. Cladosporin is a naturally occurring fungal metabolite mainly isolated from the endophytic fungus Cladosporium cladosporioides.