Fitoterapia最新文献

Sulfuretin is widely distributed in different families of nature, such as Anacardiaceae, Compositae and Leguminosae. Since it was isolated, modern pharmacological researches revealed that this compound exhibited various bioactivities, namely neuroprotection, antioxidant, anti-cancer, hepatoprotection, anti-microbial, anti-inflammation, anti-diabetes, etc., which were attributed to many important molecular targets, such as NF-κB, PI3K/AKT/mTOR, Nrf2/HO1, MAPKs and JNK/ERK. However, there was no comprehensive and critical review of this compound searched on the Internet since it was discovered, which have been recognized for more than seventy years. Hence, this review comprehensively summarizes the pharmacological effects of sulfuretin (from 1953 to 2024) by searching Scifinder, Web of Science, CNKI, PubMed and the Plant List (www.theplantlist.org) as well as other published databases and books. By this review, we hope that further study of sulfuretin will focus on the mechanism exploration and to evaluate its toxicity, then to perform related clinical assessment.

Six new prenylated isoflavonoids, named maccosas A-F (1-6), together with ten known prenylated isoflavonoids (7-16) were isolated from the twigs and leaves of Maclura fruticosa. Compounds were isolated by various column chromatographic methods including silica gel, sephadex LH-20, and semi-preparative HPLC. Their structures were elucidated by a combination of 1D and 2D NMR techniques, mass spectrometry, and comparison of their spectral data with those in the literature. Furthermore, compounds 1 and 7 exhibited anti-inflammatory activity with IC₅₀ values of 4.11 and 1.45 μM. Detection of cellular pyroptosis and western blot assay suggested that compound 1 reduced the number of PI-positive cells and inhibited Nigericin-induced pyroptosis of J774A.

Seven compounds, comprising three anthraquinones and four stilbenoids, were isolated from the roots of Rheum palmatum L. These compounds include chrysophanol (1), aloe-emodin (2), aloe-emodin 8-O-β-D-glucopyranoside (3), desoxyrhapontigenin (4), rhapontigenin (5), desoxyrhaponticin (6), and piceatannol 3'-O-β-D-glucopyranoside (7). Among these, compound 5 showed potent β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitory activity with an IC₅₀ value of 0.256 ± 0.008 μM, making it the most effective inhibitor obtained from herbal extracts to date, followed by compounds 3 (1.164 ± 0.108 μM), 6 (1.213 ± 0.193 μM), 7 (1.270 ± 0.130 μM), and 4 (2.028 ± 0.108 μM). Furthermore, kinetic analysis revealed that compound 5 acted as a mixed type-I inhibitor with an inhibition constant K_i value of 0.28 ± 0.07 μM. Notably, compound 2 exhibited potent Aβ aggregation inhibition with an IC₅₀ value of 3.56 ± 0.19 μM, whereas compound 5 showed low Aβ aggregation inhibition with an IC₅₀ value of >40 μM. The docking simulations revealed that compound 5 had a high binding affinity and interacted with TYR132, predicting it as a key residue for inhibition via hydrophobic interaction, and with THR133 via hydrogen bonding, in the flap region of BACE1. These results suggest that stilbenoids generally exhibit higher BACE1 inhibitory activity than that of anthraquinones, and that compound 5 (rhapontigenin) could be a promising candidate for the treatment of Alzheimer's disease as a potent BACE1 inhibitor.

C₁₃-Norisoprenoid megastigmanes are a currently expanding class of secondary metabolites originating from the oxidative degradation of carotenoids such as lutein and neoxanthin. These metabolites have been isolated either in free, glycosidically bound forms or as acylated derivatives from a wide diversity of the plant kingdom. The classification of megastigmanes depends on the diversity of the oxygenation positions and the biogenetic origin. These compounds play a crucial role in imparting wine with its characteristic variant flavors, and they are potentially important flavoring agents for the food and pharmaceutical industries. Striking examples for the class are the unusually potent fragrances β-ionone, β-damascenone, and megastigmatrienone. The literature highlighted several compounds that need further development and optimization for drug discovery programs of hepatoprotective, anti-inflammatory, antioxidant, cytotoxic, anti-melanogenic, and cholesterol and triglycerides metabolism-promoting drugs. This comprehensive review focuses on classification, biosynthesis, distribution in natural sources, and chemical structures, the studied biological activities, as well as the structure-activity relationship of the new natural C₁₃-norisoprenoid megastigmanes. A total of 800 C₁₃-norisoprenoid megastigmanes were covered from the first reported isolation of megastigmanes up to December 2024 and 355 references are cited.

Capsaicin (CAP), the principal bioactive component of chili peppers (Capsicum annuum L.), is widely recognized for its anti-inflammatory properties. However, its oral bioavailability is low, likely due to extensive sulfonation metabolism. Despite the well-known pharmacological benefits of CAP, the role of sulfotransferase (SULT)-mediated sulfonation in modulating its therapeutic effects remains poorly understood. This study aims to elucidate the sulfonate metabolic profile of CAP, investigate the anti-inflammatory role of its sulfonate metabolite (CAP-S), and uncover the mechanisms underlying CAP-S's anti-inflammatory effects. In our study, the mono-sulfonate metabolite of CAP, designated as CAP-S ((E)-N-[(4-sulfo-3-methoxyphenyl)methyl]-8-methylnon-6-enamide), is identified using ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) and proton nuclear magnetic resonance (¹H-NMR). The metabolic profile of CAP was investigated in liver S9 fractions from human, rat, and mouse samples, with sulfonation of CAP examined using seven major recombinant SULT isoforms. The results demonstrate that CAP is primarily catalyzed by SULT1A subfamily and SULT1E1. The anti-inflammatory effects of CAP-S are evaluated in lipopolysaccharide (LPS)-stimulated RAW264.7 cells and an acute liver injury (ALI) mouse model. CAP-S significantly reduces inflammatory mediators and nitric oxide (NO) production in LPS-induced RAW264.7 cells. In vivo, CAP-S treatment alleviates hepatocyte necrosis, inflammatory cell infiltration, and reduces aspartate aminotransferase, alanine aminotransferase, and malondialdehyde levels, while enhancing superoxide dismutase activity and decreasing NO production. Additionally, CAP-S exerts comparable anti-inflammatory effects to CAP by suppressing NF-κB p65 phosphorylation and reducing pro-inflammatory cytokines, as evidenced by network pharmacology and western blot assays. These findings underscore the role of sulfonation in modulating CAP's therapeutic potential.