TY - JOUR
T1 - Identification and evaluation of agents isolated from traditionally used herbs against Ophiophagus hannah venom
AU - Salama, Rima
AU - Sattayasai, Jintana
AU - Gande, Arun Kumar
AU - Sattayasai, Nison
AU - Davis, Mike
AU - Lattmann, Eric
PY - 2012/2/1
Y1 - 2012/2/1
N2 - The aim of this study was firstly to identify active molecules in herbs, that are traditionally used for the treatment of snake bite, such as Curcuma antinaia, Curcuma contravenenum, Andrographis paniculata, and Tanacetum parthenium; secondly to test similar structurally related molecules and finally to prepare and evaluate an efficient formulation against Ophiophagus hannah venom intoxification. Three labdane based compounds, including labdane dialdehyde, labdane lactone, and labdane trialdehyde and two lactones including 14-deoxy-11,12-didehydroandrographolide and parthenolide were isolated by column chromatography and characterised. Using the isolated rat phrenic nerve-hemidiaphragm preparation, the antagonistic effect of crude extracts, isolated compounds and prepared formulations were measured in vitro on the inhibition of the neuromuscular transmission. Inhibition on muscle contraction, produced by the 5 μg/mL venom, was reversed by test agents in organ bath preparations. A labdane trialdehyde, isolated from C. contravenenum, was identified as the best antagonising agent in the low micromolar range. Tests on formulations of the most potent C. contravenenum extract showed, that the suppository with witepsol H15 was an effective medicine against O. hannah venom. This study elucidated the active compounds, accounting for the antivenin activity of traditionally used herbs and suggested the most suitable formulation, which may help to develop potent medicines for the treatment of snake bite in the future.
AB - The aim of this study was firstly to identify active molecules in herbs, that are traditionally used for the treatment of snake bite, such as Curcuma antinaia, Curcuma contravenenum, Andrographis paniculata, and Tanacetum parthenium; secondly to test similar structurally related molecules and finally to prepare and evaluate an efficient formulation against Ophiophagus hannah venom intoxification. Three labdane based compounds, including labdane dialdehyde, labdane lactone, and labdane trialdehyde and two lactones including 14-deoxy-11,12-didehydroandrographolide and parthenolide were isolated by column chromatography and characterised. Using the isolated rat phrenic nerve-hemidiaphragm preparation, the antagonistic effect of crude extracts, isolated compounds and prepared formulations were measured in vitro on the inhibition of the neuromuscular transmission. Inhibition on muscle contraction, produced by the 5 μg/mL venom, was reversed by test agents in organ bath preparations. A labdane trialdehyde, isolated from C. contravenenum, was identified as the best antagonising agent in the low micromolar range. Tests on formulations of the most potent C. contravenenum extract showed, that the suppository with witepsol H15 was an effective medicine against O. hannah venom. This study elucidated the active compounds, accounting for the antivenin activity of traditionally used herbs and suggested the most suitable formulation, which may help to develop potent medicines for the treatment of snake bite in the future.
KW - antivenin activity
KW - rat nerve-hemidiapragm
KW - labdane diadehyde
KW - labdane triadehyde
KW - parthenolide
KW - desoxy-andrographolide
UR - http://www.scopus.com/inward/record.url?scp=84865830161&partnerID=8YFLogxK
UR - http://www.ddtjournal.com/getabstract.php?id=504
U2 - 10.5582/ddt.2012.v6.1.18
DO - 10.5582/ddt.2012.v6.1.18
M3 - Article
C2 - 22460424
AN - SCOPUS:84865830161
SN - 1881-7831
VL - 6
SP - 18
EP - 23
JO - Drug Discoveries and Therapeutics
JF - Drug Discoveries and Therapeutics
IS - 1
ER -