Ipomoea stans (IS) has long been used as an anticonvulsant. Although the use of HPLC and nuclear magnetic resonance techniques recently have allowed some of its compounds to be identified, the anticonvulsant properties of this Convolvulaceae remained to be tested. During the course of several weeks, mice (BALB/C) were given a normal infusion of the plant instead of clean water (IS-ad lib). They also were given total lyophilized powder (IS-T), and two mixtures of compounds (IS-A and IS-B) from the plant. Their convulsive thresholds were then tested with pentylenetetrazol (PTZ: 40, 60, 85 and 100mg/kg, s.c.) and electric shock (ECS: 0.1mAmp, 60 Hz). Results showed Ipomoea stans provides protection against ECS and a low dose of PTZ (40 mg/kg). However, some data from animals who died following ECS after receiving a high regimen of IS suggests they suffered mesenteric infarct. Similar results appeared after treatments with IS-T and IS-A. All IS preparations offered protection but IS-B in particular protected mice against seizures produced by a low dose of PTZ (40 mg/kg) and delayed the onset of seizures produced by ECS. In a second set of experiments, IS-ad lib and IS-T increased the threshold for amygdala discharges produced by the cortical electrical stimulation in Wistar rats. It is concluded that IS possesses some anticonvulsant properties similar to valproic acid, that are attributable to fraction B of the plant. Fraction A seems to possess a weaker anticonvulsant activity and some toxic properties.
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Sci Rep
January 2025
Division of Human Nutrition and Health, Wageningen University, Stippeneng 4, 6708 WE, Wageningen, The Netherlands.
Cannabidiol (CBD), a specialized metabolite (phytocannabinoid) abundant in Cannabis sativa, is attracting increasing attention for its alleged health-promoting properties. The present study aimed to investigate the pharmacokinetics of CBD and its primary metabolite, 7-hydroxy-cannabidiol (7-OH-CBD), following a single oral dose of a CBD-rich Cannabis sativa extract, equivalent to 70 mg CBD, in healthy male (n=5) and female (n=6) participants. Using a randomized crossover design, the study evaluated the impact of a standardized high-fat meal compared to fasting on the oral bioavailability of CBD.
View Article and Find Full Text PDFNat Prod Res
January 2025
Krishna Institute of Pharmacy, Krishna Vishwa Vidyapeeth (Deemed to be University), Karad, India.
Linn., commonly known as the 'Tree of Sadness' belongs to Oleaceae family. In Ayurvedic, Siddha, Unani, and Homeopathic therapeutic systems, it has been used to treat various conditions, including ulcers, skin diseases, hair loss, piles, liver diseases, rheumatism, and malarial fevers.
View Article and Find Full Text PDFOrg Biomol Chem
January 2025
Catalysis Laboratory, School of Chemistry, University of Hyderabad, Hyderabad-500 046, India.
Simple and sustainable three- and four-step sequences of di-OH-protection/mono-OMe-deprotection/OrgRC and di-OH-protection/mono-OMe-deprotection/OrgRC/OMe-deprotection protocols were developed to construct biologically active natural products of irisoquin, irisoquin A, irisoquin D, irisoquin F, sorgoleone-364, embelin, rapanone, 5--methylembelin, 5--methylrapanone and their analogues from the commercially available 2,5-dihydroxy-1,4-benzoquinone, aliphatic aldehydes and Hantzsch ester (1,4-DHP) in very good to excellent yields by using organocatalytic reductive coupling (OrgRC) as key reaction. Many of these natural compounds exhibited a broad spectrum of biological activities including antioxidant, anti-inflammatory, anticonvulsant, anxiolytic, analgesic, anthelmintic, antitumor, antibacterial, and antifertility properties. At the same time, simple and readily available 2,5-dihydroxy-1,4-benzoquinone was transformed into a functionally rich library of 2,5-dihydroxy-3,6-dialkyl-1,4-benzoquinones in very good yields by using sequential OrgRC followed by deprotection reactions and resulting natural/unnatural products would be excellent targets for investigation to show their biological activities compared to known natural products.
View Article and Find Full Text PDFPharmacol Rep
January 2025
Experimental Medicine Research Center, Tehran University of Medical Sciences, P.O. Box: 13145-784, Tehran, Iran.
Background: Epilepsy, a neurological disorder characterized by recurrent seizures, presents considerable difficulties in treatment, particularly when dealing with drug-resistant cases. Dapsone, recognized for its anti-inflammatory properties, holds promise as a potential therapeutic option. However, its effectiveness in epilepsy requires further investigation.
View Article and Find Full Text PDFPharmaceuticals (Basel)
January 2025
Institute of Neurobiology, Bulgarian Academy of Sciences, 1113 Sofia, Bulgaria.
This study explores the potential for the synthesis of peptide nanosystems comprising spinorphin molecules (with rhodamine moiety: Rh-S, Rh-S5, and Rh-S6) conjugated with nanoparticles (AuNPs), specifically peptide Rh-S@AuNPs, peptide Rh-S5@AuNPs, and peptide Rh-S6@AuNPs, alongside a comparative analysis of the biological activities of free and conjugated peptides. The examination of the microstructural characteristics of the obtained peptide systems and their physicochemical properties constitutes a key focus of this study. Zeta (ζ) potential, Fourier transformation infrared (FTIR) spectroscopy, circular dichroism (CD), scanning electron microscopy (SEM-EDS), transmission electron microscopy (TEM), and UV-Vis spectrophotometry were employed to elucidate the structure-activity correlations of the peptide@nano AuNP systems.
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