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  1. Mechanisms of α-mangostin-induced antinociception in a rodent model
    Sani MH, Taher M, Susanti D, Kek TL, Salleh MZ, Zakaria ZA
    Biol Res Nurs, 2015 Jan;17(1):68-77.
    PMID: 25504952 DOI: 10.1177/1099800414529648
    Elucidate the antinociceptive mechanisms of α-mangostin isolated from Garcinia malaccensis Linn.
    Matched MeSH terms: Capsaicin/administration & dosage
  2. The impact of capsaicin intake on risk of developing gastric cancers: a meta-analysis
    Pabalan N, Jarjanazi H, Ozcelik H
    J Gastrointest Cancer, 2014 Sep;45(3):334-41.
    PMID: 24756832 DOI: 10.1007/s12029-014-9610-2
    BACKGROUND: Reported associations of capsaicin with gastric cancer development have been conflicting. Here, we examine 10 published articles that explore these associations using 2,452 cases and 3,996 controls.

    METHODS: We used multiple search strategies in MEDLINE through PubMed to seek for suitable articles that had case-control design with gastric cancer as outcome.

    RESULTS: The outcomes of our study shows protection (odds ratio [OR] 0.55, P = 0.003) and susceptibility (OR 1.94, P = 0.0004), both significant with low and medium-high intake of capsaicin, respectively, although under relatively heterogeneous conditions (P(heterogeneity) = <0.0001). Outlier analysis resulted in loss of overall heterogeneity (P = 0.14) without affecting the pooled ORs. Among the subgroups, low intake elicited protection in both Korean (OR 0.37) and Mexican (OR 0.63) populations while high intake rendered these subgroups susceptible (OR 2.96 and OR 1.57, respectively). These subgroup values were highly significant (P = 0.0001-0.01) obtained in heterogeneous conditions (P(heterogeneity) capsaicin intake is significantly different from the protection that low consumption offers.

    CONCLUSIONS: This meta-analysis implies moderation in capsaicin consumption in order to derive its protective benefits.

    Matched MeSH terms: Capsaicin/administration & dosage
  3. Fulltext The α6 subunit-containing GABAA receptor: A novel drug target for inhibition of trigeminal activation
    Fan PC, Lai TH, Hor CC, Lee MT, Huang P, Sieghart W, et al.
    Neuropharmacology, 2018 09 15;140:1-13.
    PMID: 30016665 DOI: 10.1016/j.neuropharm.2018.07.017
    Novel treatments against migraine are an urgent medical requirement. The α6 subunit-containing GABAA receptors (α6GABAARs) are expressed in trigeminal ganglia (TG), the hub of the trigeminal vascular system (TGVS) that is involved in the pathogenesis of migraine. Here we reveal an unprecedented role of α6GABAARs in ameliorating TGVS activation using several pharmacological approaches in an animal model mimicking pathological changes in migraine. TGVS activation was induced by intra-cisternal (i.c.) instillation of capsaicin in Wistar rats. Centrally, i.c. capsaicin activated the trigeminal cervical complex (TCC) measured by the increased number of c-Fos-immunoreactive (c-Fos-ir) TCC neurons. Peripherally, it elevated calcitonin gene-related peptide immunoreactivity (CGRP-ir) in TG and depleted CGRP-ir in the dura mater. Pharmacological approaches included a recently identified α6GABAAR-selective positive allosteric modulator (PAM), the pyrazoloquinolinone Compound 6, two α6GABAAR-active PAMs (Ro15-4513 and loreclezole), an α6GABAAR-inactive benzodiazepine (diazepam), an α6GABAAR-selective antagonist (furosemide), and a clinically effective antimigraine agent (topiramate). We examined effects of these compounds on both central and peripheral TGVS responses induced by i.c. capsaicin. Compound 6 (3-10 mg/kg, i.p.) significantly attenuated the TCC neuronal activation and TG CGRP-ir elevation, and dural CGRP depletion induced by capsaicin. All these effects of Compound 6 were mimicked by topiramate, Ro15-4513 and loreclezole, but not by diazepam. The brain-impermeable furosemide antagonized the peripheral, but not central, effects of Compound 6. These results suggest that the α6GABAAR in TG is a novel drug target for TGVS activation and that α6GABAAR-selective PAMs have the potential to be developed as a novel pharmacotherapy for migraine.
    Matched MeSH terms: Capsaicin/administration & dosage
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