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Mechanism of Action

Asperuloside is an iridoid monoterpene glycoside whose primary biological activity is expressed upon hydrolysis to the aglycone asperulosidic acid by plant-endogenous beta-glucosidase enzymes (activated by cell disruption) and intestinal microflora. Asperulosidic acid inhibits prostaglandin biosynthesis through COX enzyme inhibition and suppresses NF-κB-mediated transcription of inflammatory cytokines. In vitro studies demonstrate inhibition of tumor cell proliferation via G2/M cell cycle arrest and induction of apoptosis through caspase-3 activation. The compound also exerts mild cathartic effects through stimulation of intestinal peristalsis. Asperuloside is relatively heat-labile and subject to significant loss upon prolonged drying or high-temperature extraction, supporting the traditional preference for fresh-plant preparations.
Bitter principle with mild laxative and diuretic properties; characteristic iridoid of Galium species

Research Notes

CleaversWestern

Asperuloside from Galium aparine and related Rubiaceae species has demonstrated anti-inflammatory activity in LPS-stimulated RAW 264.7 macrophages, reducing TNF-α, IL-6, and NO production with IC50 values in the low micromolar range. Cytotoxic activity has been documented in HeLa, MCF-7, and HepG2 cancer cell lines with IC50 values of 20–80 µg/mL in MTT assays. In vivo anti-inflammatory data from rodent carrageenan models showed 25–35% reduction in paw edema at 100 mg/kg. No human clinical trials on isolated asperuloside from cleavers exist; efficacy data for the whole herb in its traditional lymphatic applications remain largely anecdotal.

Characteristic iridoid glycoside of Galium species with mild laxative and diuretic properties.

Found In 2 Herbs

3D Molecular Structure

Iridoid glycoside (monoterpenoid glucoside)
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Asperuloside

Iridoid glycoside (monoterpenoid glucoside)Modified terpenes with diverse biological activities

Representative pattern: C₁₁H₁₄O₆

Atoms
Carbon
Oxygen

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