anti-alcohol

GET73 (Gamma hydroxybutyric acid analogue) is an negative allosteric modulator of mGluR5. GET73 is a naturally occurring neurotransmitter. GET73 has anti-alcohol and anxiolytic properties.

Vanillyl Alcohol (3-Methoxy-4-hydroxybenzyl alcohol) possesses anti-angiogenic, anticonvulsive, anti-inflammatory, anti-oxidant, neuroprotective, and anti-nociceptive activities. Vanillyl alcohol can effectively inhibit the cytotoxicity and improved cell viability in 1-methyl-4-phenylpyridinium (MPP+)-induced MN9D dopaminergic cells, it also can attenuate the elevation of reactive oxygen species (ROS) levels, decrease in the Bax Bcl-2 ratio and poly (ADP-ribose) polymerase proteolysis.

4-Hydroxybenzyl alcohol (P-Methylolphenol) exhibits beneficial effects in cerebral ischemic injury, has neuroprotective effect through upregulation of Nrf2, Prdx6, and PDI expression via the PI3K Akt pathway. 4-Hydroxybenzyl alcohol inhibit the development of new blood vessels by targeting multiple mechanisms of the angiogenic process, may as a promising candidate for the establishment of anti-angiogenic treatment strategies in cancer therapy.

(S)-(−)-Perillyl alcohol (Perillyl alcohol), a monoterpene found in lavender, inhibits Ras farnesylation, upregulates the mannose-6-phosphate receptor, induces apoptosis, and exhibits anti-cancer activity.

Schisandrin (Wuweizi alcohol-A) is a compound with anti-asthmatic, anti-cancer, and anti-inflammatory effects.

Hydroxysafflor yellow A (Safflomin A) inhibits adipogenesis by increasing HSL promoter activities, effectively protects the liver from long-term alcohol injury by enhancing antioxidant capacity and inhibiting the expression of TGF-β, prevents steroid-induced avascular necrosis of the femoral head by inhibiting primary bone marrow-derived mesenchymal stromal cells, and exhibits anti-tumor effects.

COR659 is a GABAB positive allosteric modulator (PAM) . COR659 suppresses alcohol and chocolate self-administration in rats[1]. COR659 apparently exerts its effects via a composite mechanism, including positive allosteric modulation of the GABAB receptor and an action at the cannabinoid CB1 receptor[3]. COR659 (0, 2.5, 5 and 10 mg kg) treatment is completely ineffective on lever-responding (FR10) for regular food pellets in food-deprived Wistar rats[1].COR659 is able to suppress lever-responding for a sucrose solution in sP rats and a chocolate solution in Wistar rats[2]. Animal Model: Male sP and Wistar rats[1]. [1]. Paola Maccioni, et al. Suppressing effect of COR659 on alcohol, sucrose, and chocolate self-administration in rats: involvement of the GABA B and cannabinoid CB 1 receptors. Psychopharmacology (Berl). 2017 Sep;234(17):2525-2543. [2]. Francesca Ferlenghi, et al. The GABA B receptor positive allosteric modulator COR659: In vitro metabolism, in vivo pharmacokinetics in rats, synthesis and pharmacological characterization of metabolically protected derivatives. Eur J Pharm Sci. 2020 Dec 1;155:105544. [3]. Paola Maccioni, et al. Anti-addictive properties of COR659 - Additional pharmacological evidence and comparison with a series of novel analogues. Alcohol. 2019 Mar;75:55-66.

Gamma-glutamylcysteine TFA (γ-glutamylcysteine TFA) is a precursor of glutathione (GSH) with antioxidant and anti-inflammatory properties. It alleviates oxidative stress and mitochondrial damage induced by ethanol in hepatocytes by increasing cellular GSH, SOD activity, and mitochondrial membrane potential, protecting cells from alcohol-induced liver disease (ALD) by inhibiting oxidative stress, reducing inflammation, and preventing cell apoptosis.

Isopropyl palmitate is the isopropyl alcohol and palmitic acid ester. It is a moisturizer, emollient, anti-static agent, and thickening agent.

22-Hydroxy Mifepristone (RU 42698) is an orally active hydroxylated alcohol metabolite that exhibits both anti-progestational and anti-glucocorticoid activities. This compound contains an alkyne group and is capable of undergoing copper-catalyzed azide-alkyne cycloaddition (CuAAC) with azide-containing molecules. Furthermore, 22-Hydroxy Mifepristone demonstrates a relative binding affinity of 48% to the human glucocorticoid receptor.

Patchouli alcohol (Patchoulol) is a naturally occurring tricyclic sesquiterpenoid found in patchouli oil. It is a key bioactive component known for its immunomodulatory, anti-inflammatory, antioxidant, antitumor, antibacterial, anti-atherosclerotic, antiemetic, and sedative properties.

PHYTOL (trans-Phytol) , a diterpene alcohol from chlorophyll widely used as a food additive and in medicinal fields, shows antinociceptive and antioxidant activities as well as anti-inflammatory and antiallergic effects. It is a specific activator of PPARα.

Ledol ((+)-Ledol) is a naturally occurring sesquiterpene with potential biological activities such as antioxidant, anti-inflammatory, xanthine oxidase inhibition and uric acid reduction.

Cytosolic phospholipase A2α (cPLA2α) specifically catalyzes the hydrolysis of arachidonic acid from thesn-2-ester position of membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes, both important mediators of the inflammatory process.1CAY10641 is an inactive alcohol derivative of a highly potent (IC50= 12 nM) cPLA2α inhibitor.2The parent compound demonstrates strong anti-inflammatory effects when applied topically at a dose of 0.1 mg/ear in a mouse model of acute irritant contact dermatitis.2CAY10641 is rapidly cleared from the blood stream (only 0.5 μg/ml remains 30 minutes after 10 mg/kg intravenous administration to mice).2However, no other biological effects have been reported. 1.Schaloske, R.H., and Dennis, E.A.The phospholipase A2 superfamily and its group numbering systemBiochemica et Biophysica Acta17611246-1259(2006) 2.Drews, A., Bovens, S., Roebrock, K., et al.1-(5-carboxyindol-1-yl)propan-2-one inhibitors of human cytosolic phospholipase A2α with reduced lipophilicity: Synthesis, biological activity, metabolic stability, solubility, bioavailability, and topical in vivo activityJournal of Medicinal Chemistry535165-5178(2010)

Cycloartenyl ferulate (also known as cycloartenol ferulate) is a representative triterpene alcohol with diverse biological properties, such as antioxidant, anti-allergic, anti-inflammatory, and anticancer activities.

Euphol, an alcohol tetracyclic triterpene, has a wide range of pharmacological properties and is considered to have anti-inflammatory action.

Nabumetone alcohol is the alcohol form of nabumetone, a non-steroidal anti-inflammatory drug (NSAID) that is rapidly metabolized in the liver to a major active metabolite, 6-methoxy-2-naphthyl acetic acid, which inhibits the cyclooxygenase enzyme and preferentially blocks COX-2 activity (which is indirectly responsible for the production of inflammation and pain during arthritis).

1. Schisandrol B (Besigomsin) may exert neuroprotective effects by attenuating the microglia-mediated neuroinflammatory response via inhibiting the TLR4-mediated NF-κB and MAPKs signaling pathways. 2. Schisandrol B has anti-inflammatory property, potentially result from the inhibition of COX-2, iNOS, IL-6, TNF-α and NO through the down-regulation of RIP2 and NF-κB activation. 3. Schisandrol B induces marked protective effects against hepatic and renal injury induced by CCl(4) exposure through differential regulation of the MAPK signal transduction pathway. 4. Schisandrol B significantly inhibits cell proliferation in a dose-dependent manner, due to cell cycle arrest in the G1 phase with the downregulation of cyclin D1 expression and Retinoblastoma (RB) phosphorylation.

ent-Abacavir is an enatiomer of Abacavir. Abacavir is a carbocyclic 2'-deoxyguanosine nucleoside reverse transcriptase inhibitor and an anti-HIV drug used to treat HIV infection. Intracellular enzymes convert Abacavir to its active form, carbovir-triphosphate (CBV-TP), which then selectively inhibits HIV reverse transcriptase by incorporating into viral DNA. Abacavir is metabolized in the liver by uridine diphosphate glucuronyltransferase and alcohol dehydrogenase resulting in inactive glucuronide and carboxylate metabolites, respectively.

3-Chlorogentisyl alcohol, characterized by its potent inhibitory action against E. coli β-glucuronidase with an IC(50) value of 0.74 µM and a K(i) value of 0.58 µM, demonstrates significant antiproliferative activity. This compound shows promise for use in the research of anti-cancer and anti-inflammatory therapies.

Perillic acid, a metabolite of Perillyl alcohol, exhibits properties that induce cell cycle arrest and apoptosis in lung cancer cells. Additionally, this compound demonstrates anti-HSV-1 (anti-Herpes Simplex Virus type 1) and immunomodulatory activities [1] [2] [3].

Dihydrodehydrodiconiferyl alcohol 9-O-α-L-rhamnopyranoside (Compound 1), a lignan with anti-HBV activity, selectively targets the HBV surface antigen (HBsAg) with an IC50 of 0.58 mM, while its activity against the HBV e antigen (HBeAg) is significantly lower, with an IC50 of >2.4 mM. This compound can be isolated from the plant star anise [1].

Dihydrodehydrodiconiferyl alcohol 9-O-β-D-xylopyranoside serves as an anti-hepatitis B virus (anti-HBV) agent, effectively inhibiting the secretion of HBV surface antigen (HBsAg) and HBV e antigen (HBeAg) in the Hep G2.2.15 cell line, with IC50 values of 1.67 mM for HBsAg and over 2.15 mM for HBeAg [1].

Chrysanthemol (Trans-Chrysanthemyl Alcohol) is a trans-sesquiterpene-type sesquiterpene from Chrysanthemum indicum L. It has some anti-inflammatory activity and is used in the synthesis of citrophilus mealybug sex pheromone.