Triterpenoid Saponins with Potential Cytotoxic Activities from the Root Bark of Ilex rotunda Thunb.

Abstract

A new 19-oxo-18,19-seco-ursane-type triterpeonoid saponin, laevigin E (8), together with 17 known compounds (1 - 7 and 9 - 18) were isolated from the root bark of Ilex rotunda Thunb. Their structures were determined by various spectroscopic analysis. Among them, compounds 6, 9, 11, and 18 were isolated from this species for the first time, while compounds 10 and 12 were firstly isolated from the family Aquifoliaceae. Biological activity assay showed that all triterpenoids exhibit moderate cytotoxic activities against MCF7, A549, HeLa and LN229 cell lines. The four triterpenoid saponins (3, 4, 6, and 8) exhibit slightly better activities compared to the four triterpenoid sapogenins (1, 2, 5, and 7). Compound 8 showed the best cytotoxicity against A549, HeLa and LN229 cell lines with IC of 17.83, 22.58 and 30.98 μm, respectively.

Effects of Gut Microbiota and Ingredient-Ingredient Interaction on the Pharmacokinetic Properties of Rotundic Acid and Pedunculoside

“…Ilex rotunda Thunb., a medically woody plant in the Aquifoliaceae family, is widely distributed throughout southern China [1,2]. In the Chinese Pharmacopoeia (2015 edition) [3], its bark is officially recorded as IRC and is used for the treatment of gastrointestinal and cardiovascular diseases.…”

“…In the Chinese Pharmacopoeia (2015 edition) [3], its bark is officially recorded as IRC and is used for the treatment of gastrointestinal and cardiovascular diseases. IRC is a rich source of triterpenoids, which exhibit significant cardiovascular protection activities [1,[4][5][6][7]. Both PDC and its aglycone RA are by far the most abundant (approximately 23.5 % of the IRC extract) and are representative medicinal triterpenoids in IRC that have been selected as the quality control markers [8,9].…”

Absolute bioavailability, dose proportionality, and tissue distribution of rotundic acid in rats based on validated LC-QqQ-MS/MS method

“…Rotundic acid (RA), a plant-derived and ursane-type pentacyclic triterpene acid, was identified as a major active ingredient of IRC and has been shown to exert extensive pharmacological effects, including antimicrobial [ 3 , 4 ], anti-inflammatory [ 5 ], anticancer [ [6] , [7] , [8] , [9] , [10] , [11] , [12] , [13] ], and lipid-decreasing effects [ 14 ]. It has also been proven to alleviate type 2 diabetes and its complications by improving the composition of the gut microbiota [ 15 ].…”

UPLC-QTOF-MS Based Comparison of Rotundic Acid Metabolic Profiles in Normal and NAFLD Rats

“…Between 1981 and 2019, almost 70% of drugs approved by the FDA were natural products or corresponding derivatives [ 6 ]. “Jiubiying” is the dry leaf and bark of Ilex rotunda Thumb, which is often used to treat diarrhea, metaphysitis, bruises, colds, fever, and rheumatism [ 7 , 8 ]. Furthermore, it is currently included in the Chinese Pharmacopoeia.…”