Journal of ethnopharmacology · 2026
β-Asarone-induced vasorelaxation in isolated rat mesenteric artery: An efficacy vs toxicity paradox of Acorus calamus.
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Parashar Shweta, Singh Munmun Kumar, Singh Kavita, Shankar Uma, Mishra Suyashi, Tandon Sudeep, Verma Ram Swaroop, Chanda Debabrata
Аннотация
ETHNOPHARMACOLOGICAL RELEVANCE: Acorus calamus L., popularly called vacha or sweet flag, is used in Ayurveda, Unani, Siddha, Chinese and other traditional medicines to treat a wide range of illnesses, including neurological, gastrointestinal, respiratory, metabolic, kidney, and liver disorders.
AIM OF THE STUDY: This study aims to investigate the vasorelaxation potential of β-asarone (BA), a key biomarker of the A. calamus, as well as BA-enriched essential oil (ACRO), supercritical CO2 extract (ACRE), and BA-free fraction of A. calamus.
MATERIALS AND METHODS: The vasoreactivity of BA, ACRO, ACRE, and the BA-free fraction of A. calamus was evaluated in an ex vivo system with isolated superior mesenteric atrial rings, including elucidating the mode of action. In vitro toxicity in rat smooth muscle cells and in vivo oral toxicity in Swiss albino mice were evaluated to determine the safety profile of the test extract and the molecule.
RESULTS: BA, ACRO and ACRE exhibited promising vasorelaxation in isolated rat mesenteric arteries (1-30 μg/ml), whereas the BA-free fraction exhibited a negligible vasorelaxation response. BA-induced concentration-dependent relaxation responses were studied in rat mesenteric arteries, and it was found to be highly sensitive in modulating calcium channel function in vascular smooth muscle cells, suggesting L-type VDCC as a major putative target in vasorelaxation response. Further, BA, ACRO and ACRE were evaluated for cytotoxicity in vascular smooth muscle cells. In vitro toxicity of BA suggested its safety up to 30 μM in the MTT assay. However, ACRO and ACRE showed cytotoxicity and inhibition of cell proliferation beyond 30 μg/ml when incubated for 12h. In continuation, the results of in vivo toxicity showed that ACRO and ACRE exhibited potential toxicity and produced complete mortality with ACRO and partial mortality with ACRE within the observational period of seven days, although morbidity and observational changes were evident in all the treatment groups when given from the range of 300 mg/kg up to 2000 mg/kg.
CONCLUSIONS: This data suggests a classic case of efficacy-toxicity paradox in A.calamus, suggesting further study to retain efficacy and enhance safety.
AIM OF THE STUDY: This study aims to investigate the vasorelaxation potential of β-asarone (BA), a key biomarker of the A. calamus, as well as BA-enriched essential oil (ACRO), supercritical CO2 extract (ACRE), and BA-free fraction of A. calamus.
MATERIALS AND METHODS: The vasoreactivity of BA, ACRO, ACRE, and the BA-free fraction of A. calamus was evaluated in an ex vivo system with isolated superior mesenteric atrial rings, including elucidating the mode of action. In vitro toxicity in rat smooth muscle cells and in vivo oral toxicity in Swiss albino mice were evaluated to determine the safety profile of the test extract and the molecule.
RESULTS: BA, ACRO and ACRE exhibited promising vasorelaxation in isolated rat mesenteric arteries (1-30 μg/ml), whereas the BA-free fraction exhibited a negligible vasorelaxation response. BA-induced concentration-dependent relaxation responses were studied in rat mesenteric arteries, and it was found to be highly sensitive in modulating calcium channel function in vascular smooth muscle cells, suggesting L-type VDCC as a major putative target in vasorelaxation response. Further, BA, ACRO and ACRE were evaluated for cytotoxicity in vascular smooth muscle cells. In vitro toxicity of BA suggested its safety up to 30 μM in the MTT assay. However, ACRO and ACRE showed cytotoxicity and inhibition of cell proliferation beyond 30 μg/ml when incubated for 12h. In continuation, the results of in vivo toxicity showed that ACRO and ACRE exhibited potential toxicity and produced complete mortality with ACRO and partial mortality with ACRE within the observational period of seven days, although morbidity and observational changes were evident in all the treatment groups when given from the range of 300 mg/kg up to 2000 mg/kg.
CONCLUSIONS: This data suggests a classic case of efficacy-toxicity paradox in A.calamus, suggesting further study to retain efficacy and enhance safety.