Asprenols A-H, phenolic constituents from the stems of Ilex asprella.[Pubmed: 30031114]

Encouraged by the in vivo anti-inflammatory effect of aqueous extract of Ilex asprella stems, a further phytochemical investigation on I. asprella stems oriented by the in vitro NO production inhibition in RAW264.7 cells was conducted, which led to the isolation of eight new phenolic constituents, namely asprenols A-H (1-8), together with 12 known ones (9-20). The structures of the new compounds were established by extensive spectroscopic data analyses of HR-ESI-MS, IR, UV, and 1D and 2D NMR, and the absolute configurations were determined by comparison of experimental and calculated ECD analyses. All isolated were evaluated for the inhibition against NO production in RAW 264.7 cells, and several compounds showed moderate inhibitory effect.

Characterization and immunoregulatory activity of two polysaccharides from the root of Ilex asprella.[Pubmed: 30007662]

The polysaccharides obtained from the root of Ilex asprella, namely IAPS-1 and IAPS-2, with immunoregulatory activity were studied. Two polysaccharides were isolated and purified by Cellulose DEAE-52 and Sephadex columns. The structure of IAPS-1 was elucidated as 1,6-linked α-d-glucopyranosyl main chain with branch chain substituted at C-2 and/or C-4 position. For IAPS-2, the backbone is composed of 1, 4-linked α-d-glucose, galactose and rhamnose, and branched chains consists of arabinose, rhamnose and galacturonic acid, as confirmed by partial acid hydrolysis and NMR study. Further, the immunoregulatory activity of IAPS-1 and IAPS-2 was tested with the murine macrophages. Particularly, IAPS-2 polysaccharide can more effectively enhance the secretion of major inflammatory cytokines in macrophages, such as TNF-α, IL-1β, IL-12, compared with IAPS-1.

Ilex asprella aqueous extracts exert in vivo anti-inflammatory effects by regulating the NF-κB, JAK2/STAT3, and MAPK signaling pathways.[Pubmed: 29981433]

Ilex asprella (Hook. et Arn.) Champ. ex Benth. (IA) is a representative medicinal plant from the South of the Five Ridges of China. Its roots (RIA) and stems (SIA) have been traditionally used for the inflammation-related diseases, such as acute and chronic pharyngitis, cough, and sore throats.

Two new 18, 19-seco Triterpenoids from Ilex asprella (Hook. et Arn.) Champ. ex Benth.[Pubmed: 29698682]

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Three new triterpenoid saponins from the stems of Ilex asprella.[Pubmed: 29580098]

Three new triterpenoid saponins, namely asprellinoids A-C (1-3), featuring a sulfate substitution in sugar moiety, were isolated from the stems of Ilex asprella (Hook. et Arn.) Champ. ex Benth. Their structures were elucidated by the spectroscopic data analyses including HR-ESI-MS, IR, and NMR spectra, and chemical method.

[Chemical constituents from stems of Ilex asprella].[Pubmed: 29271154]

Phytochemical investigation on the stems of Ilex asprella by using various chromatographic techniques led to the isolation of 13 compounds. By spectroscopic analyses and comparisons the spectral data with those in literatures, these compounds were identified as salicifoneoliganol(1), rel-(7R,8S)-3,3',5-trimethoxy-4',7-epoxy-8,5'-neolignan-4,9,9'-triol 9-β-D-glucopyranoside(2),(+)-cycloolivil(3),(+)-syringaresinol-4'-O-β-D-monoglucoside(4), liriodendrin(5), caffeic acid (6), 3,4-dihydroxy-5-methoxybenzaldehyde(7), benzene-1,2,4-triol(8), 3,4,5-trimethoxyphenyl-1-O-β-D-apiofuranosyl(1″→6')-glucopyranoside(9), aeculetin(10), cryptochlorogenic acid ethyl ester(11), chlorogenic acid ethyl ester(12), and rel-5-(3S,8S-dihydroxy-1R,5S-dimethyl-7-oxa-6-oxobicyclo [3,2,1]oct-8-yl)-3-methyl-2Z,4E-pentadienoic acid(13). Among them, compounds 7, 8, 11, and 13 were isolated from genus Ilex for the first time, and 1-3, 9, 10, and 12 were isolated from this speciesfor the first time. The anti-inflammatory assay results of these compounds showed that compounds 1 and 9 showed moderate inhibitory effect against NO production in RAW 267. 4 cells with IC₅₀ values of 35.7 and 50.6 μmol•L⁻¹, in vitro respectively, whereas compound 10 showed weak inhibition(IC₅₀ value 98.7 μmol•L⁻¹).

[A phytochemical and pharmacological advance on Ilex asprella].[Pubmed: 28945020]

Ilex asprella is one of representative medicinal plants in South of the Five Ridges of China. The roots and rhizomes of I. asprella have the effects of clearing heat and detoxifying, stimulating salvia, and reducing thirst, which has been used to treat wind-heat cold, acute and chronic pharyngitis, and sore throat. Contemporary studies showed that I. asprella contains the major triterpenoids and glycosides, phenolic acids, and minor steroids. The extracts and compounds show activities of anti-inflammatory, antiviral, anti-tumor, and regulating lipid metabolism.The present paper summarizes a phytochemical and pharmacological advance on this species to provide reference for clarification of its pharmacologically active ingredients, quality evaluation, and further explorations.

[A new oleanane-type triterpenoid glycoside from roots of Ilex asprella].[Pubmed: 28840691]

A new δ-oleanane-type triterpenoid glycoside, 3-O-(3-O-sulfo)-β-D-glucopyranosiduronic acid 3β-hydroxy-13(18)-oleanen- 28-oic acid 28-β-D-glucopyranosyl ester (1), along with ten known triterpenoid glycosides, rotundinoside A (2), oblonganoside M (3), 3-O-β-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl 3β,19α-dihydroxy-20α- urs-12-en-28-oic acid 28-O-β-D- glucopyranosyl ester (4), ilexsaponin B2 (5), ilexside Ⅱ (6), rotundinoside B (7), ilekudinoside B (8), ilexpublesnin E (9), ilekudinoside D (10) and ilexpernoside D (11), was isolated from the 75% ethanol extract of the roots of Ilex asprella by various chromatographic separation. Their structures were identified on the basis of MS, NMR spectroscopic analysis and chemical methods. In addition, 2-11 were isolated from I. asprella for the first time.

Anticomplement triterpenoids from the roots of Ilex asprella.[Pubmed: 28094185]

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