Latest ArticlesFive sesquiterpenoids were isolated from a 50% acetone extract of Cornus officinalis leaves, a traditional non-medicinal part of Cornus officinalis, using modern column chromatographic techniques such as macroporous adsorbent resins colum, silica gel colum, chromatography gel colum and semi-preparative liquid chromatography techniques. Their structures were identified by modern wave spectroscopy techniques and electronic circular dichroism (ECD) and assigned as cornurtone A (1), cornucadinoside B (2), lacinilene C (3), 3, 12-dihydroxycadalene (4), cornucadinoside C (5). Compound 1 was new compound and compounds 2-5 were first isolated from leaves of Cornus officinalis. Compounds 2 and 3 had potential neuroprotective activities.
Three new compounds were isolated from the n-butanol fraction of Zingiber officinale (Ginger) peel by MCI Gel CHP-20, Sephadex LH-20, ODS and semipreparative high performance liquid chromatography. Their structures were identified as dendranthemoside C (1), zingpyranoside E (2), zingpyranoside F (3) by 1D-NMR, 2D-NMR, HR-ESI-MS, circular dichroism (CD) and ECD calculation techniques.
It aimed to research the chemical constituents of Solidago canadensis Lour. A new sucrose derivative was isolated from the the methanol extract of Solidago canadensis Lour. with the technologies of silica gel, microporous resin, Rp-18, and Sephadex LH-20 column chromatography. It was identified as 2, 4, 6, 1′, 3′, 6′-O-hexaisovaleryl sucrose by 1D NMR, 2D NMR, high-resolution mass spectrometry, and acid hydrolysis method. Its mass spectrometry fragmentation behaviors were analyzed using high-resolution mass spectrometry and found that compound 1 was easy to break the glycosidic bond to produce the fragment at m/z 415. The ion at m/z 415 continued to eliminate the isovaleryl group as neutral or non-neutral form to generate a series of daughter ions. Compound 1 could inhibit NO production on LPS-induced neuroinflammatory responses in BV2 microglial cells at the concentrations of 5, 10, and 20 μmol·L-1 to exhibit neuroprotective effect. Its half maximal inhibition rate of NO was measured to be 13.96 ± 0.78 μmol·L-1.
A new benzoic acid derivative, spinulacid (1), together with six known compounds ascomindone A (2), ascomindone C (3), monomethylsulochrin (4), barceloneic acid A (5), flufuran (6), and 5-hydroxymethyl-furaldehyde (7) were obtained from the rice fermentation extract of an endophytic fungus Penicillium spinulosum isolated from Emmenopterys henryi Oliv. by various chromatographic techniques. Their structures were elucidated by the analysis of NMR data, MS and comparison with literature. The biological activity results showed that compounds 1, 2, 5, and 6 exhibited significant proangiogenic activity in transgenic zebrafish at concentrations of 20 and 40 μmol·L-1 (the animal experiment was approved by the Animal Ethical and Welfare Committee of Biology Institute, Shandong Academy of Science, the approval number is SWS20240611). Compounds 1 and 4 displayed moderate or strong antifungal activity against phytopathogen Fusarium graminearum with minimum inhibitory concentration (MIC) values of 12.5, and 6.25 μg·mL-1, respectively. Besides, compound 4 was also found to show obvious antibacterial activity against Staphylococcus aureus and Erwinia carotovora with MIC values of 6.25 and 12.5 μg·mL-1, respectively.
Through several chromatographic methods, such as silica gel, Sephadex LH-20 and high performance liquid chromatography (HPLC), six iridoids were isolated from the roots and rhizomes of Patrinia scabiosaefolia. By means of nuclear magnetic resonance (NMR) spectroscopy, 13C NMR calculation and mass spectrometry (MS), their structures were identified as patrinin A (1), patrinin B (2), loganin aglycone (3), isovillosol (4), 1, 3-dimethoxy-4, 7-dimethyl-octahyhro-cyclopenta[c]pyran-6, 7-diol (5) and viburnshosin A (6). Among them, compounds 1 and 2 were new compounds. Furthermore, the anti-influenza virus and anti-inflammatory activities of the isolates were evaluated.
Fourteen compounds including two new compounds were isolated from Kronopolites svenhedini (Verhoeff). These structures were identified as kronoponit A (1), kronoponit B (2), neoechinulin A (3), 2-(1, 1-dimethyl-2-propen-1-yl)-1H-indole-3-carboxaldehyde (4), uracil (5), p-hydroxy phenyl ethylamine (6), p-hydroxyphenylacetic acid (7), p-hydroxybenzoic acid (8), p-ethylbenzoic acid (9), 2-methyl-1, 4-benzenediol (10), 1, 2, 4-benzenetriol (11), gallic acid (12), gallic acid-3-methyl ether (13), and 4-methoxy-3, 5-hydroxybenzoic acid (14) by spectroscopic methods and literature. Among them, compounds 1 and 2 are new, while compounds 3-14 are reported here for the first time from K. svenhedini.
Synthetic cannabinoid N-(1-carbamoyl-2, 2-dimethylpropyl)-1-butylazole-3-formamide (ADB-BUTINACA), as a new psychoactive substance, shows strong stimulant and hallucinogenic effects. It can cause cardiovascular, renal and gastrointestinal diseases, and in severe cases, it can lead to death. However, there are few reports on toxicology studies of the ADB-BUTINACA metabolic pathway and its long-term effects on the organism and the molecular mechanisms behind it. In this study, the metabolic profile of rat serum after low, medium and high doses of ADB-BUTINACA (0.1, 1, and 5 mg·kg-1) intervention were analyzed using UHPLC coupled with a Q-Orbitrap-MS (UHPLC-Q-Orbitrap-HRMS). The results showed that the intervention of ADB-BUTINACA could cause significant changes of 50 metabolites such as L-glutamate and 3-hydroxybutyrate, and nine metabolic pathways including alanine, aspartate and glutamate metabolism, retinol metabolism, and TCA cycle were disturbed. These findings provide a novel experimental and theoretical framework for further investigation of the toxicological mechanisms underlying ADB-BUTINACA-induced dysregulation of lipid and energy metabolism. Furthermore, they offer valuable insights that could facilitate the diagnosis and prevention of ADB-BUTINACA toxicity, thereby underscoring their significant implications for public health. The study was conducted in adherence to both the Declaration of Helsinki and the National Institutes of Health's Guidelines for the Care and Use of Laboratory Animals, and received approval from the animal experimental center at the Zhejiang Chinese Medical University (Ethical number: 20220718-11).
Jinqi Jiangtang Capsule (JQJTC) is one of the commonly used dosage forms of Jinqi Jiangtang formula, derived from the classic Qianjin Huanglian Pill, which is widely used in the treatment of diabetes mellitus. However, its pharmacokinetics is not still unclear. In this study, a stable and reliable method for the quantitative analysis of multiple components from JQJTC in mouse plasma and liver was established by ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). Then, the concentration changes of 16 components from JQJTC in plasma and liver of type 2 diabetic mice were determined and the kinetics was analyzed. The results demonstrated that the established UPLC-MS/MS method met the requirements for the determination of biological samples. The alkaloids, organic acids, flavonoids, and saponins were absorbed into mouse blood after JQJTC was administered by gavage, and there were significant differences in the rates of absorption, transport into liver and elimination and exposure levels of 16 components in plasma and liver. And the exposure of alkaloids, calycosin-7-glucoside and its glycosides, formononetin, and cycloastragenol in the liver were significantly higher than that in the plasma. The results provided a basis for further research on the pharmacodynamic substances of JQJTC. The use of all experimental animals has been approved by the Ethics Committee of Laboratory Animal of Shanghai University of Traditional Chinese Medicine (No. PZSHUTCM2401310001).
In order to further distinguish the differences of compounds in different medicinal parts of Angelica (head, body and tail), our study used UHPLC-QE-MS combined with non-targeted metabolomics technology to identify the different compounds in different medicinal parts of Angelica. Principal component analysis (PCA) and OPLS-DA were used to screen the differential metabolites, and the related pathways were compared and analyzed. Eighteen types of 1 072 metabolites were identified from different medicinal parts of Angelica sinensis, mainly terpenoids, phenylpropanes, lipids and their derivatives, alkaloids, flavonoids, organic acids and their derivatives, etc. The comparison between Angelica head and Angelica body, Angelica head and Angelica tail, Angelica body and Angelica tail showed 530, 565, 474 different metabolites, among which kaempferol, cinnamic acid, chlorogenic acid, ferulic acid, ligustilide, liquiritigenin, and rutin were mainly enriched in Angelica tail, naringin, apigenin were mainly enriched in Angelica body, estradiol, ligustrazine were mainly enriched in Angelica head; differential metabolites are concentrated in flavonoid biosynthesis, phenylalanine metabolism, indole alkaloid biosynthesis, tryptophan metabolism, flavonoid and flavonol biosynthesis and other pathways. In this study, UHPLC-QE-MS non-targeted metabolomics technology can effectively analyze the differential metabolites of different medicinal parts of Angelica sinensis, providing scientific support for clinical rational and accurate application of different medicinal parts of Angelica sinensis.
Cocktail probe drug method was used to evaluate the effect of cold treatment drugs such as Gegen Decoction on cytochrome P450 (CYP450) enzyme activity in rat liver. The in vitro incubation system of rat liver microsomes was optimized. Based on LC tandem mass spectrometry (LC-MS/MS), an analytical method for simultaneous determination of the content of metabolites of each subenzyme probe in rat liver microsome CYP450 enzyme was established. Cocktail probe drug method was used to characterize the effects of Gegen Decoction, a classical prescription for the treatment of wind-cold cold, and acetaminophen, chlorpheniramine maleate, anhydrous caffeine and nacotine hydrochloride, which were commonly used in the treatment of cold, on the activity of CYP2D6, CYP2C9, CYP3A4 and other sub-enzymes in rat liver microsomes, so as to provide reference for the safety of clinical drug combination. The results showed that the established analysis method was stable and reliable, which met the requirements of biological sample determination. After optimization, the protein concentration of rat liver microsomes in the incubation system was 3.00 mg·mL-1, the incubation time was 240 min, and the terminator was acetonitrile. The Km values of three CYP subenzyme specific probe substrates dextromethorphan, testosterone and tolbutamide were 21.49, 87.33 and 354.7 μmol·L-1, respectively. The effectiveness of the established incubation system was verified by positive inhibitors. Compared with the blank control group, when the concentration of each Western medicine and the concentration of Gegen Decoction extract were within 100.00 μmol·L-1 and 3.00 mg·mL-1, respectively, Gegen Decoction extract, chlorpheniramine maleate and noscapine hydrochloride had inhibitory effects on CYP2C9 and CYP2D6 enzymes in rat liver microsomes; anhydrous caffeine had inhibitory effects on CYP2C9 and CYP3A4 enzymes in rat liver microsomes; no significant inhibitory effect on acetaminophen; the induction effect of narcotine hydrochloride on CYP3A4 enzyme in rat liver microsomes was greater than 40% of the activity of positive inducer, suggesting that there may be a certain risk of drug interaction when combined with narcotine hydrochloride, and attention should be paid to the dose of drug treatment. The experimental protocol strictly adhered to the guidelines of the Ethics Committee of Animal Research of Guangdong Pharmaceutical University (Approval: gdpulacspf2022137).
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