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Iridoid constituents from the flower buds and inflorescences of Buddleja officinalis and their anti-pulmonary fibrosis activity
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DOI：10.1016/j.phytochem.2026.114890.png)
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Abstract
En 中文
Although the floral parts of Buddleja officinalis are traditionally employed to alleviate several pulmonary conditions, their associated bioactive constituents have yet to be identified. In our search for anti-pulmonary fibrotic agents from medicinal plants, 12 previously undescribed iridoids (1-5 and 7-13), along with one known analogue (6), were isolated from the flower buds and inflorescences of this plant. Their structures were elucidated through comprehensive spectroscopic analyses and single-crystal X-ray diffraction. Compounds 1-3 were rare chlorinated iridoids, whereas the remaining ten possessed a dihydrocatalpolgenin core. All isolates were evaluated for anti-fibrotic activity in a TGF-/31-induced NIH/3T3 fibrosis model. Among them, compound 12 exhibited the most potent activity, with an IC50 of 0.20 mu M and a favorable selectivity index (SI = 49.5), representing five-fold increase in potency over the positive control SB431542 (IC50 = 1.00 mu M). Mechanistic investigations further revealed that 12 attenuated fibroblast proliferation, migration, and myofibroblast activation, and selectively restored the dysregulated MMP/TIMP axis to re-establish extracellular-matrix homeostasis.
Keywords:
Buddleja officinalis
Scrophulariaceae
Iridoid
Anti-fibrotic activity
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