Analgesic activity of affinin, an alkamide from Heliopsis longipes (Compositae)

Rios, Marı́a Yolanda; Aguilar-Guadarrama, A. Berenice; Gutiérrez, María del Carmen

doi:10.1016/j.jep.2006.09.041

Cited by 65 publications

(57 citation statements)

References 14 publications

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“…The H. longipes extract showed the highest inhibitory potential on P450 enzymes, showing IC 50 values as 21.1, 9.9 and 3.6 μg/mL for CYP1A1/2, CYP2D6 and CYP3A4 respectively. Affinin, the plant's main bioactive compound, is the most abundant amide identified in roots of H. longipes (Table 1) (Molina-Torres et al, 2004;Rios et al, 2007). Like the extract, affinin inhibited CYP1A1/2 (IC 50 = 25 μg/mL), 2D6 (IC 50 = 16.1 μg/mL) and 3A4 (IC 50 = 13.5 μg/mL) activities.…”

Section: Resultsmentioning

confidence: 99%

Inhibition of human P450 enzymes by natural extracts used in traditional medicine

Rodeiro¹,

Donato

Jiménez

et al. 2008

Phytotherapy Research

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Different medicinal plants are widely used in Cuba and Mexico to treat several disorders. This paper reports in vitro inhibitory effects on the P450 system of herbal products commonly used by people in Cuba and Mexico in traditional medicine for decades. Experiments were conducted in human liver microsomes. The catalytic activities of CYP1A1/2, 2D6, and 3A4 were measured using specific probe substrates. The Heliopsis longipes extract exhibited a concentration-dependent inhibition of the three enzymes, and similar effects were produced by affinin (an alkamide isolated from the H. longipes extract) and two catalytically reduced alkamides. Mangifera indica L. and Thalassia testudinum extracts, two natural polyphenol-rich extracts, diminished CYP1A1/2 and 3A4 activities, but not the CYP2D6 activity. These results suggest that these herbs inhibit the major human P450 enzymes involved in drug metabolism and could induce potential herbal-drug interactions.

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Section: Resultsmentioning

confidence: 99%

Inhibition of human P450 enzymes by natural extracts used in traditional medicine

Rodeiro¹,

Donato

Jiménez

et al. 2008

Phytotherapy Research

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“…NAAs can exhibit analgesic effect through central GABA release e.g. spilanthol (1) (Rios et al, 2007), by interfering with voltage-gated sodium channels or via desensitization of the TRPV1 receptor. TRPV1 agonists initially stimulate sensory neurons and release of substance P, followed by a long-lasting refractory period, during which the previously excited neurons are no longer responsive to a broad range of stimuli (Bode and Dong, 2011;Luo et al, 2011;Pal et al, 2009).…”

Section: Othersmentioning

confidence: 99%

Alkamid database: Chemistry, occurrence and functionality of plant N-alkylamides

Boonen

Bronselaer

Nielandt

et al. 2012

Journal of Ethnopharmacology

137

109

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a b s t r a c tEthnopharmacological relevance: N-Alkylamides (NAAs) are a promising group of bioactive compounds, which are anticipated to act as important lead compounds for plant protection and biocidal products, functional food, cosmeceuticals and drugs in the next decennia. These molecules, currently found in more than 25 plant families and with a wide structural diversity, exert a variety of biologicalpharmacological effects and are of high ethnopharmacological importance. However, information is scattered in literature, with different, often unstandardized, pharmacological methodologies being used. Therefore, a comprehensive NAA database (acronym: Alkamid) was constructed to collect the available structural and functional NAA data, linked to their occurrence in plants (family, tribe, species, genus). Materials and methods: For loading information in the database, literature data was gathered over the period 1950-2010, by using several search engines. In order to represent the collected information about NAAs, the plants in which they occur and the functionalities for which they have been examined, a relational database is constructed and implemented on a MySQL back-end. Results: The database is supported by describing the NAA plant-, functional-and chemical-space. The chemical space includes a NAA classification, according to their fatty acid and amine structures. Conclusions: The Alkamid database (publicly available on the website http://alkamid.ugent.be/) is not only a central information point, but can also function as a useful tool to prioritize the NAA Q8 choice in the evaluation of their functionality, to perform data mining leading to quantitative structure-property relationships (QSPRs), functionality comparisons, clustering, plant biochemistry and taxonomic evaluations.

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“…Affinin and ethanol extract displayed an analgesic effect by delaying the reaction to pain in the mouse (paw licking and/or jumping) after being exposed to a thermal stimulus; affinin produced a higher analgesic effect than ethanol extract, by achieving longer delays in the onset of pain signals. Recently, it has been found that affinin can induce GABA (gamma-Aminobutyric acid) release in mouse brain slices (Ríos et al, 2007). Thus, the analgesic effect of affinin in the hot-plate test may be due to its action on the spinal cord, on higher central nervous system levels, or by an indirect mechanism (Yaksh & Rudy, 1977).…”

Section: Discussionmentioning

confidence: 99%