ABSTRACT
In recent years, Tripterygii Radix et Rhizoma polyglycosides have been used more and more widely in clinic, mostly in the treatment of rheumatoid arthritis. Besides, it is also used as a basic immunosuppressive drug to treat various kidney diseases, such as nephrotic syndrome. However, there are many adverse reactions in clinic, as well as controversies over its medication regimen, especially its dosage and time. To make rational use of Tripterygii Radix et Rhizoma polyglycosides in clinic and further study, the pharmacological and toxicological research progress of Tripterygii Radix et Rhizoma polyglycosides was reviewed. The author collected pharmacological and toxicological research literatures of Tripterygii Radix et Rhizoma polyglycosides at home and abroad in recent years, finding that Tripterygii Radix et Rhizoma polyglycosides have the pharmacological effects of anti-inflammation, anti-tumor, kidney protection and immunosuppression, and mainly plays a pharmacological role by regulating the expression of cytokines in NF-<italic>κ</italic>B signaling pathway, mTOR signaling pathway and apoptosis-related signaling pathway. And the toxicological effects of Tripterygii Radix et Rhizoma polyglycosides mostly focused on hepatotoxicity, nephrotoxicity and reproductive system toxicity, which are mostly related to oxidative stress response and expression of inflammatory factors. The main components of Tripterygii Radix et Rhizoma polyglycosides are triptolide and celastrol. The pharmacological and toxicological studies of Tripterygii Radix et Rhizoma polyglycosides are in-depth, the results showed that the efficacy and toxicity were dose-dependent and time-dependent, with no toxicity study of Tripterygii Radix et Rhizoma polyglycosides varying with dosage and time in the context of efficacy, indicating dose-effect, time-effect, dose-toxicity, time-toxicity relationships. Relevant mechanisms still need further study.
ABSTRACT
Phytochemical investigation on Ilex asprella stems by using various chromatographic techniques led to the isolation of 18 phenolic constituents. Based on spectroscopic data analyses and/or comparison of the spectroscopic data with those in literature, these constituents were identified, including two lignans (1, 2), five phenylpropanes (3-7), six chlorogenic analogues (8-13), and five benzoic analogues (14-18). Among them, compounds 3-7, 9, 11, 13, 14, 17, and 18 were isolated from genus Ilex for the first time, and 2, 8, 10, 15, and 16 were isolated from this species for the first time. The in vitro anti-inflammatory assay results showed that compounds 8, 9, 11, 13, and 15 possessed moderate inhibition on the NO production in RAW264.7 cells with IC₅₀ values of 51.1-85.8 μmol·L⁻¹. The present study brought preliminary reference for the clarification of therapeutic ingredients of I. asprella with anti-inflammatory efficacy and its quality evaluation.
Subject(s)
Animals , Mice , Anti-Inflammatory Agents , Pharmacology , Ilex , Chemistry , Nitric Oxide , Metabolism , Phenols , Chemistry , Phytochemicals , Pharmacology , Plant Stems , ChemistryABSTRACT
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.
ABSTRACT
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).
ABSTRACT
Eight compounds were isolated from the rice fermentation of Streptomyces sp. CPCC 202950 by a combination of various chromatographic techniques including column chromatography over silica, Sephadex LH-20, flash C₁₈, and reversed-phase HPLC. Their structures were identified as 3-[(3'-amino-3'-oxoprop-1'-en-2'-yl)oxy]benzamide (1), m-hydroxybenzamide (2), leptosphaepin (3), 5-methyluracil (4), feruloylamide (5), p-hydroxyphenylacetoamide (6), vanillamide (7), cyclo (L-val-L-ala) (8). Among them, 1 was a new benzamide analogue, and 2 was a new natural product. In the preliminary assays, none of the compounds 1-8 exhibited obvious inhibition of HIV-1 protease activity, and toxic with the Hela, HepG2, and U2OS cells. (IC₅₀ > 10 μmol•L⁻¹).