TY - JOUR
T1 - Spasmolytic effect of constituents from Lepechinia caulescens on rat uterus
AU - Perez-Hernandez, Nury
AU - Ponce-Monter, Hector
AU - Medina, Jorge A.
AU - Joseph-Nathan, Pedro
N1 - Funding Information:
We are grateful to Gloria Tellez-Tellez for technical assistance. This work was partially supported by grant PROMEP/103.5/05/1919 and PROMEP/103.5/04/2936 from Universidad Autónoma del Estado de Hidalgo.
PY - 2008/1/4
Y1 - 2008/1/4
N2 - Lepechinia caulescens Ortega Epling (Lamiaceae) is a perennial herb used in Mexican folk medicine to treat diabetes, hypertension, gastrointestinal infections, dysmenorrhea and as abortifacient. In this study, a bioassay-guided fractionation of the hexanes extract of the leaves, evaluating the capacity to relax contraction of rat uterus rings induced by KCl (60 mM), was made. The results indicated that, from the four isolated terpenes, spathulenol (1) was the most potent spasmolytic agent, followed by methyl 9α,13α-epidioxyabiet-8(14)-en-18-oate (2), 9α-hydroxydehydroabietyl alcohol (4) and dehydroabietic acid (3) studied at 10 and 30 μg/mL. The spasmolytic activity of 1 was totally reverted by addition of increasing extracellular Ca2+ concentrations ([Ca2+]o), while incubation of uterus rings with 1 in calcium free solutions reduced the contraction produced by [Ca2+]o in a concentration-dependent manner. Moreover, the presence of L-NAME (100 μM) or propranolol (10 μM) did not block the spasmolytic effect. These results suggest that 1 induces a greater blocking action on voltage-operated calcium channels. EtOAc and MeOH extracts of the leaves, which showed slight relaxing activity, led to 4 and rosmarinic acid (5).
AB - Lepechinia caulescens Ortega Epling (Lamiaceae) is a perennial herb used in Mexican folk medicine to treat diabetes, hypertension, gastrointestinal infections, dysmenorrhea and as abortifacient. In this study, a bioassay-guided fractionation of the hexanes extract of the leaves, evaluating the capacity to relax contraction of rat uterus rings induced by KCl (60 mM), was made. The results indicated that, from the four isolated terpenes, spathulenol (1) was the most potent spasmolytic agent, followed by methyl 9α,13α-epidioxyabiet-8(14)-en-18-oate (2), 9α-hydroxydehydroabietyl alcohol (4) and dehydroabietic acid (3) studied at 10 and 30 μg/mL. The spasmolytic activity of 1 was totally reverted by addition of increasing extracellular Ca2+ concentrations ([Ca2+]o), while incubation of uterus rings with 1 in calcium free solutions reduced the contraction produced by [Ca2+]o in a concentration-dependent manner. Moreover, the presence of L-NAME (100 μM) or propranolol (10 μM) did not block the spasmolytic effect. These results suggest that 1 induces a greater blocking action on voltage-operated calcium channels. EtOAc and MeOH extracts of the leaves, which showed slight relaxing activity, led to 4 and rosmarinic acid (5).
KW - Abietane diterpenes
KW - Lepechinia caulescens
KW - Spasmolytic activity
KW - Spathulenol
UR - http://www.scopus.com/inward/record.url?scp=36549081526&partnerID=8YFLogxK
U2 - 10.1016/j.jep.2007.08.044
DO - 10.1016/j.jep.2007.08.044
M3 - Artículo
SN - 0378-8741
VL - 115
SP - 30
EP - 35
JO - Journal of Ethnopharmacology
JF - Journal of Ethnopharmacology
IS - 1
ER -