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The Role of Plant-Based Natural Compounds in Inflammation
Published in Namrita Lall, Medicinal Plants for Cosmetics, Health and Diseases, 2022
Marcela Dvorakova, Premysl Landa, Lenka Langhansova
Moreover, prenylated flavonoids cannflavins A and B, isolated from industrial Cannabis sativa L. (hemp) sprouts (Figure 22.3C), were found to exert dual mPGES-1/5-LOX inhibitory activity. They potently inhibited 5-LOX in cell-free assay with IC50 values of 0.9 µM and 0.8 µM, respectively. In the cell-based assay, only cannflavin A was studied and inhibited 5-LOX with IC50 values of 1.6–2.4 µM, depending on the assay conditions. In addition, cannflavins A and B both reversibly inhibited mPGES-1 in cell-free assay with IC50 values of 1.8 µM and 3.7 µM, respectively. On the contrary, only weak inhibition of COXs by cannflavin A was observed (Werz et al., 2014).
The Role of Cannabis and Cannabinoids in Pain Management
Published in Mark V. Boswell, B. Eliot Cole, Weiner's Pain Management, 2005
Flavonoid and terpenoid essential oil components of cannabis demonstrate anti-inflammatory effects at physiologically appropriate levels (McPartland & Russo, 2001). Cannflavin A and B inhibited prostaglandin E2 production in human rheumatoid synovial cells 30 times more potently than aspirin (Barrett, Scutt, & Evans, 1986).
Cannabis Flavonoids—Antioxidant & Anti-Inflammatory Benefits
Published in Betty Wedman-St Louis, Cannabis as Medicine, 2019
Flavonoids are important in both human and animal nutrition [8] and more than 20 have been reported in cannabis [9]. Diets rich in phenolic compounds have been linked to a reduced incidence of chronic diseases—cancer, cardiovascular disease, and neurodegenerative conditions [10]. The flavones and flavonols in cannabis exert a wide range of biological effects along with terpenes and cannabinoids. The anti-inflammatory, anti-cancer, and neuroprotective properties are reviewed by Andre et al. in Current Nutrition Food Science [11] with flavones and flavonols being the primary ones [12]. A brief review of the flavonoids in cannabis has been provided as follows: Cannflavin A,B,C are methylated isoprenoid flavones with anti-inflammatory activity that inhibits the prostaglandins inflammatory pathway and enhance synergy with terpenoids [13,14].Vitexin and Isovitexin are used therapeutically for gout and inhibiting thyroid peroxidase [15].Kaempferol has been reported to have an antidepressant effect [15].Apigenin has been shown to be capable of stimulating the monoamine transporter, which alters neurotransmitter levels and acts as an anxiolytic and sedative on the GABA receptors along with cannabinoids [16].Quercetin inhibits viral enzymes and can have antiviral effects along with inhibiting prostaglandin production as an anti-inflammatory agent. It has synergistic benefits with cannabinoids to increase anti-inflammatory effects. Quercetin has also been shown to inhibit MAO (monoamine oxidase enzyme), so it can create possible interactions with some pharmaceuticals [17].Luteolin and Orientin have been shown to have pharmacological properties of antioxidants, anti-inflammatories, antibiotics, and anti-cancer [16].Liganamides/Lignans have been found in cannabis fruits and roots [18]. These phenolic amides and liganamides have health-promoting properties such as antioxidants, antivirals, antidiabetic, antitumorigenic and anti-obesity, but human studies are scarce [19]. Sun et al. [20] have shown anti-inflammatory properties in vitro while Cui-Ying et al. [21] have demonstrated cytotoxic activities of lignans that may be confirmed in cannabis.
Envelope proteins as antiviral drug target
Published in Journal of Drug Targeting, 2020
Jyoti Verma, Naidu Subbarao, Maitreyi S. Rajala
Compounds inhibiting the conformational transition of HA2 of influenza virus and inhibiting its fusion process include BMY-27709 and stachyflin [51]. BMY-27709 inhibits the fusion process of Influenza A virus with IC50 (concentration of an inhibitor where the response (or binding) is reduced by half) value between 3–8mM [52]. Another study targeting the HA trimer reports two molecules; MBX2329 and MBX2546 which inhibits HA mediated fusion [53]. Ebola virus (EBOV) envelope glycoproteins have a hydrophobic pocket (S2) at the GP1-GP2 interface, which serves as a small molecule drug target for the inhibition of Ebola virus infection. A benzodiazepine derivative was validated as an inhibitor targeting the hydrophobic pocket at GP1-GP2 interface with IC50 10 and 12 µM for EBOV and Marburg virus (MARV), respectively [54]. MBX2254 and MBX2270 are other molecules which have been identified as inhibitors of surface glycoprotein of Ebola virus [55]. Since the X-ray crystal structure of DENV envelope protein has been solved with its ligand binding pocket referred to as β-OG pocket, several fusion inhibitors are reported to be active against dengue virus. An in silico study has reported many phytochemicals namely, 2,3-dehydroxilybin, cisilandrin, isosilybins A-D, silandrins A-B, C-geranylated flavone cannflavin A from Cannabis sativa and silybin fitting into the small hydrophobic channel of DENV envelope protein. They have reported 32 compounds with excellent docking properties with the hydrophobic pore of DENV envelope protein [56]. Rolitetracycline and Doxycycline are tetracycline derived fusion inhibitors targeting the envelope protein of DENV-2 [57]. Other compounds reported to be binding to the hydrophobic pocket of the envelope protein are NITD448 (EC50: 9.8 µM , IC50: 6.8 µM), A5 (IC50: 1.2 µM), derivative of doxorubicin SA-17 (DENV-1; EC50: 12 µM , DENV-2; EC50: 1.2 µM , DENV-3; EC50: 1.7 µM) and P02 (IC50: 13 ± 3 µM) [58].