Antinociceptive Activity of Ent-Dihydrotucumanoic Acid Isolated from Gymnosperma glutinosum Spreng Less
Por:
Josabad Alonso-Castro, Angel, Martin Gonzalez-Chavez, Marco, Ramon Zapata-Morales, Juan, Karina Verdinez-Portales, Alexia, Sanchez-Recillas, Amanda, Ortiz-Andrade, Rolffy, Isiordia-Espinoza, Mario, Martinez-Gutierrez, Fidel, Antonio Ramirez-Morales, Marco, Dominguez, Fabiola, Elizabeth Juache-Flores, Maria, Martinez, Roberto
Publicada:
1 nov 2017
Categoría:
Drug discovery
Resumen:
The diterpene ent-dihydrotumanoic acid (DTA) was among the compounds
isolated from Gymnosperma glutinosum (Spreng) Less (Asteraceae). There
are no reports regarding the pharmacological effects of DTA.
Cytotoxicity against cancer cells (1-250 mu M), and the antibacterial
(50-1400 mu M) activity of DTA were evaluated using the MTT assay, and
the minimum inhibitory concentration test, respectively. The
antidiarrheal (1-100 mg/kg p.o.) and anti-inflammatory (2 mg/ear)
effects of DTA were evaluated using castor oil and
12-O-tetradecanoylphorbol-13-acetate, respectively. The antinociceptive
and sedative effects of DTA (1-100 mg/kg p.o.) were evaluated using two
models of chemically-induced nociception, and the pentobarbital-induced
sleeping time test, respectively. The antinociceptive mechanism of DTA
was evaluated using the acetic acid writhing test with inhibitors
related to pain processing pathways. The effects of DTA (10-100 mg/kg
p.o.) on locomotor activity were evaluated using the rotarod test. DTA
lacked cytotoxic activity (IC50>100 mu M) on cancer cells, possessed
moderate antibacterial effects against B. subtillis (MIC= 175 mu M),
moderate antidiarrheal and anti-inflammatory effects, and minimal
vasorelaxant effects. In the formalin test, DTA showed antinociceptive
effects in both phases. In the acetic acid test, DTA showed
antinociceptive activity (ED50= 50.2 +/- 5.6 mg/kg) with potency similar
to that of naproxen (NPX; ED50=33.7 +/- 4.5 mg/kg) an effect blocked by
naloxone implicating an opioid mechanism. DTA also exerted antidiarrheal
activity and showed no sedative effects or changes in locomotor activity
in mice. Drug Dev Res 78 : 340-348, 2017. (c) 2017 Wiley Periodicals,
Inc.
Filiaciones:
Josabad Alonso-Castro, Angel:
Univ Guanajuato, Div Ciencias Nat & Exactas, Dept Farm, Guanajuato 36050, Guanajuato, Mexico
Martin Gonzalez-Chavez, Marco:
Univ Autonoma San Luis Potosi, Fac Ciencias Quim, San Luis Potosi, San Luis Potosi, Mexico
Ramon Zapata-Morales, Juan:
Univ Guanajuato, Div Ciencias Nat & Exactas, Dept Farm, Guanajuato 36050, Guanajuato, Mexico
Karina Verdinez-Portales, Alexia:
Univ Guanajuato, Div Ciencias Nat & Exactas, Dept Farm, Guanajuato 36050, Guanajuato, Mexico
Sanchez-Recillas, Amanda:
Univ Autonoma Yucatan, Fac Quim, Yucatan, Mexico
Ortiz-Andrade, Rolffy:
Univ Autonoma Yucatan, Fac Quim, Yucatan, Mexico
Isiordia-Espinoza, Mario:
Univ Cuauhtemoc Plantel San Luis Potosi, Escuela Odontol, San Luis Potosi, San Luis Potosi, Mexico
Martinez-Gutierrez, Fidel:
Univ Autonoma San Luis Potosi, Fac Ciencias Quim, San Luis Potosi, San Luis Potosi, Mexico
Antonio Ramirez-Morales, Marco:
Univ Guanajuato, Div Ciencias Nat & Exactas, Dept Farm, Guanajuato 36050, Guanajuato, Mexico
Dominguez, Fabiola:
Inst Mexicano Seguro Social, Ctr Invest Biomed Oriente, Puebla, Mexico
Elizabeth Juache-Flores, Maria:
Univ Autonoma San Luis Potosi, Fac Ciencias Quim, San Luis Potosi, San Luis Potosi, Mexico
Martinez, Roberto:
Univ Nacl Autonoma Mexico, Inst Quim, Dept Quim Organ, Mexico City, DF, Mexico
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