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ABSTRACT Ferutinin (1), the major constituent of Ferula hermonis and other Ferula species, is a sesquiterpene ester with remarkable estrogenic activity, beside other valuable medicinal properties. To investigate the influence of chemical... more
ABSTRACT Ferutinin (1), the major constituent of Ferula hermonis and other Ferula species, is a sesquiterpene ester with remarkable estrogenic activity, beside other valuable medicinal properties. To investigate the influence of chemical modification of the ferutinin structure on its estrogenic effect and binding affinity toward the cannabinoid CB1 and CB2 receptors, twelve derivatives of 1 were prepared and evaluated in vitro, together with the parent compound, for the respective bioactivities, based on the recent evidence for estrogen–endocannabinoid interaction. Nine of the prepared derivatives (3–11) are new semisynthetic esters of 1. The parent compound ferutinin (1) exhibited the highest level of estrogenic activity (EC50 0.3 μM and a percent maximal 17β-estradiol response of 90 % at 1 µM). Compound 6 was found to be a selective agonist for CB2 receptor (EC50 0.051 μM, Ki 0.025 μM), with much less affinity for CB1 receptor (EC50 97 μM, Ki 48.5 μM). Compound 8 was a selective agonist for CB1 (EC50 62, Ki 0.031 μM) with no affinity toward CB2.
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and Mahmoud ElSohly The crux of the potency debate is the directly opposing views of pro-and anti-cannabis proponents ... Desmond Slade, Zlatko Mehmedic, Suman Chandra active ingredients (ElSohly and Slade, 2005), accumu-lating mainly in... more
and Mahmoud ElSohly The crux of the potency debate is the directly opposing views of pro-and anti-cannabis proponents ... Desmond Slade, Zlatko Mehmedic, Suman Chandra active ingredients (ElSohly and Slade, 2005), accumu-lating mainly in the glandular trichomes of the ...
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Phytochemical investigation of a high potency variety of Cannabis sativa L. resulted in the isolation of six new metabolites, (+/-)-6,7-trans-epoxycannabigerolic acid ( 2), (+/-)-6,7- CIS-epoxycannabigerolic acid ( 3), (+/-)-6,7-... more
Phytochemical investigation of a high potency variety of Cannabis sativa L. resulted in the isolation of six new metabolites, (+/-)-6,7-trans-epoxycannabigerolic acid ( 2), (+/-)-6,7- CIS-epoxycannabigerolic acid ( 3), (+/-)-6,7- CIS-epoxycannabigerol ( 4), (+/-)-6,7-trans-epoxycannabigerol ( 5), 5'-methyl-4-pentylbiphenyl-2,2',6-triol ( 7), and 7-methoxycannabispirone ( 8), along with seven known compounds namely, cannabigerolic acid ( 1), 5'-methoxycannabigerolic acid ( 6), cannabispirone ( 9), beta-cannabispiranol ( 10), dehydrocannabifuran ( 11), cannflavin B ( 12) and cannabigerol ( 13). The antimicrobial as well as the antileishmanial activities were investigated.
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Cannabis has been around for thousands of years and has been used recreationally, medicinally, and for fiber. Over 500 compounds have been isolated from Cannabis sativa with approximately 105 being cannabinoids. Of those 105 compounds,... more
Cannabis has been around for thousands of years and has been used recreationally, medicinally, and for fiber. Over 500 compounds have been isolated from Cannabis sativa with approximately 105 being cannabinoids. Of those 105 compounds, Δ(9)-tetrahydrocannabinol has been determined as the primary constituent, which is also responsible for the psychoactivity associated with Cannabis. Cannabinoid receptors belong to the large superfamily of G protein-coupled receptors. Targeting the cannabinoid receptors has the potential to treat a variety of conditions such as pain, neurodegeneration, appetite, immune function, anxiety, cancer, and others. Developing in vitro bioassays to determine binding and functional activity of compounds has the ability to lead researchers to develop a safe and effective drug that may target the cannabinoid receptors. Using radioligand binding and functional bioassays, a structure-activity relationship for major and minor cannabinoids was developed.
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Research Interests: Natural Products, Medicinal Plants, Cannabinoids, Biological Sciences, Cercopithecus aethiops, and 18 moreEscherichia coli, Animals, Candida, Aspergillus fumigatus, Pseudomonas aeruginosa, Cannabis, CHEMICAL SCIENCES, Anti-Bacterial Agents, Plasmodium falciparum, Antimalarials, Natural, Gas Chromatography/mass Spectrometry, Antifungal Agents, Microbial Sensitivity Tests, Pseudomonas Aeruginosa, Biological activity, Methicillin Resistant Staphylococcus Aureus, and Molecular Structure
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Research Interests: Statistical Analysis, Cancer, Cell Cycle, Calcium, Enzyme Inhibitors, and 22 moreOxidative Stress, Endoplasmic Reticulum Stress, Cytotoxicity, Apoptosis, Western blotting, Antioxidants, In Vitro, Humans, Correlation, Reactive Oxygen Species, Endoplasmic Reticulum, Artemisia, Heme Oxygenase, Heme, Lysine, Pharmacodynamics, Biological markers, Biological activity, N-Acetylcysteine, Antineoplastic Agents, Dimerization, and Gene expression profiling
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Research Interests: Organic Chemistry, Magnetic Resonance Spectroscopy, Cell line, Humans, Cryptococcus Neoformans, and 11 moreAntimicrobial activity, Artemisia, Antifungal Activity, Antibacterial activity, Liquid Chromatography / Electrospray Ionization Mass Spectrometry, Plasmodium falciparum, Antifungal Agents, Bioorganic and medicinal Chemistry, Biological activity, Antineoplastic Agents, and Dimerization
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The double-edged sword of antibiotic use in the fight against disease has saved countless lives at the cost of an escalation in pathogenic bacteria with increased resistance to multiple antibiotic classes. Reduction of resistance is a... more
The double-edged sword of antibiotic use in the fight against disease has saved countless lives at the cost of an escalation in pathogenic bacteria with increased resistance to multiple antibiotic classes. Reduction of resistance is a complicated multi-step endeavor that requires a sustained international effort of reduced utilization, infection control and development of effective and economical antimicrobial agents. The carbapenems are beta-lactam antibiotics that are stable to most beta-lactamases. They have potent bactericidal activity against a wide range of Gram-positive and Gram-negative aerobic bacteria as well as against anaerobic bacteria, while being safe, efficacious and tolerable. The use of carbapenems in hospitals has therefore been restricted to the empirical treatment of critical patients with a variety of serious infections, e.g., nosocomial pneumonia, septicemia, meningitis and cystic fibrosis. This article reviews patents claiming carbapenem antibacterial agents published from 2004-2008.