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The Worldwide Spread of ‘Herbal Highs’
Published in Ornella Corazza, Andres Roman-Urrestarazu, Handbook of Novel Psychoactive Substances, 2018
Jessica Neicun, Darshan Singh, Eduardo Cinosi
Evidence suggests that hydrophobicity, poor water solubility, high variability of drug release in simulated biological fluids, and the acid-degradable characteristics of mitragynine likely further influence the large variability of its pharmacological responses reported in the literature (Ramanathan et al., 2015). Mitragynine, 7-hydroxymitragynine and mitraphylline exhibit high plasma protein binding (>90 %) determined by equilibrium dialysis (Manda et al., 2014). The metabolism of Kratom is mainly hepatic and, while mitragynine might have unlikely significant effects on CYP3A4 activity, it may interfere with other cytochrome P450 enzyme activities, specifically CYP2D6, raising concerns of drug interactions (Azizi, Ismail, & Mansor, 2013; Hanapi et al., 2013).
Inhibiting Insulin Resistance and Accumulation of Triglycerides and Cholesterol in the Liver
Published in Christophe Wiart, Medicinal Plants in Asia for Metabolic Syndrome, 2017
Mitragyna speciosa (Korth.) Havil. elaborates indole alkaloids of which mitragynine, paynantheine, mitraphylline, and speciophylline.424 Speciophylline induced an increase of biliary flow from 7.3 to 10.5 mg/100 g/min.425 Biochemical analysis of the bile collected during biliary flow study revealed an increase in total bilirubin from 27.8 to 43.8 µmol/L and an increase in conjugated bilirubin from 12.1 to 19.2 µmol/L as well as absence of hepatotoxicity.425 This plant is becoming popular but is in fact addictive and hepatotoxic. A 25-year-old man consuming 1 to 6 tea spoons of Mitragyna speciosa (Korth.) Havil. daily for 2 weeks developed severe intrahepatic cholestasis.426 The mode of action of speciophylline is unknown. Evidence suggests that indole alkaloids have the tendency to activate farnesoid X receptor.427,428 Mitragynine given orally to male rodent at a dose of 100 mg/kg/day for 28 days induced a weight gain by 130% whereby untreated animals had a weight gain of circa 140% and mitragynine at a dose of 1 mg/kg raised the weight gain by circa 160%.429 The main food intake of rodents receiving 100 mg/kg/day for 28 days decreased from circa 300 to 220 g/kg/24 h/cage.429 Besides, this alkaloid evoked in male rodents a decrease in triglycerides from 1.1 to 0.5 mmol/L and glycaemia from 6.2 to 5/8 mmol/L, whereby chesterolaemia was unchanged.429
Catalog of Herbs
Published in James A. Duke, Handbook of Medicinal Herbs, 2018
Quite a few alkaloids have been isolated from the plant, a number of them interesting pharmacologically: ajmalicine, akuammicine, akuammine, alstonine, ammocaline, carosi-dine, carosine, catharanthine, catharicine, Catharine, catharosine, cavincidine, cavincine, cleavamine, deacetylvincaleucoblastine, deacetylvindoline, dihydrositsirikine, isoleurodine, isositsirikine, leurocristine, leurosidine (vinrosidine), leurosidine, leurosine, leurosivine, lochnericine, lochnerine, lochnerinine, lochnerivine, lochrovidine, lochrovine, maandrosine, mitraphylline, neoleurocristine, neoleurosidine, pericalline, permividine, perimivine, peri-vine, perosine, pleurosine, reserpine, rovidine, rovidine sulfate, serpentine, sitsirikine, te-trahydroalstonine, tetrahydroserpentine, vinaphamine, vinaspine, vinblastine, vincaleucob-lastine, vincamicine, vincamine, vincarodine, vincathicine, sulfate, vinceine, vincolidine, vincoline, vincristine, vindoiicine, vindolidine, vindoline, vindolinine, vindorosine, vinos-idine, vinsedecine, vinsesine, virosine, yohimbine. The root bark contains 2.0% of a phenolic resin and 0.03% d-camphor. The leaves yield an oleoresin and a small amount of volatile oil containing aldehydes, sesquiterpenes, and sulfur compounds, furfural, lochnerol and lochnerallol, two glycosides (adenosine, roseoside), deoxyloganin, loganin, tannin, carotene, sterols, ursolic acid, and a flavone derivative. Some of the alkaloids have both antitumor and tumorigenic attributes, suggesting what I have come to believe, that a given species will contain many pairs of compounds which are antagonistic. Catharanthine is diuretic, ajmalicine is antidiuretic. Will the body of the patient who needs the diuretic select catharanthine or reject ajmalicine? Ajmalicine (raubasine) has a broad application in circulatory diseases, especially in the relief of obstruction of normal cerebral blood flow. In combination with rauwolfia alkaloids it has been used to lower high blood pressure.59 Toxicity — Same as Catharanthus lanceus.
An overview of spirooxindole as a promising scaffold for novel drug discovery
Published in Expert Opinion on Drug Discovery, 2020
Li-Ming Zhou, Ren-Yu Qu, Guang-Fu Yang
Gelsemine is a representative example of indole alkaloids isolated from the genus Gelsemium. It has been found to possess antihyperlipidemic and antioxidative effects [13], as well as have repairing action against cisplatin-produced nephrotoxicity [14]. Spirotryprostatins A and B are identified as potential anticancer drugs due to their potent inhibition against the G2/M phase of cell division and mouse breast cancer cells tsFT210 [15]. Alstonisine is the first macroline-related oxindole alkaloid isolated from Alstonia muelleriana [16], showing moderate in vitro antiplasmodial activity. Besides, this natural product also can be used to design potential murine double minute 2 (MDM2) inhibitors. Naturally occurring oxindole alkaloid Citrinadin A/B and Notoamide B were isolated from Penicillium citrinum N059 strain and Aspergillus species, respectively, which have been widely studied because of their remarkable anticancer efficacy [17,18]. Pteropodine, Isopteropodine, Isomitraphylline, Mitraphylline, and Uncarine F were all obtained from Uncaria tomentosa. Except for mitraphylline, the other four kinds of alkaloids can control the proliferation of acute lymphoblastic leukemia cells (CEM-C7H2 cells) [19,20]. Besides, Mitraphylline exhibits an in vivo controlling effect against the cytokines associated with most inflammation processes. Thus, it is considered to be a novel lead compound for anti–inflammatory therapy [21]. Speciophylline isolated from Mitragyna inermis has potential in vitro antiplasmodial property [22]. Cyclopiamine A/B and C/D are fungal hexacyclic spiroindolinone alkaloid isolated from Penicillium cyclopium in 1979 and soilborne strain coded as Penicillium sp. CML 3020 in 2009, respectively. Their related bioactivities are being carried out a detailed investigation [23,24]. Beyond that, there are many other natural products bearing this characteristic structural scaffold (spirooxindole) such as Tabernoxidine, Formosainine, and Marcfortine A/B, which provide abundant structural forms and diverse bioactivities.