Latest ArticlesFour previously undescribed lanostane tetracyclic triterpenoids baoslingzhines T-W (1-4) were isolated from Ganoderma lucidum. Their structures including relative and absolute configurations were assigned by spectroscopic methods and ECD calculations.
The methanol extract of Pteris wallichiana was separated and purified by MCI gel, sephadex LH 20, flash C18 and silica gel column chromatography combined with semi-pre HPLC. The chemical structures of the isolated compounds were identified by MS, IR, NMR, etc. Five sesquiterpene compounds were isolated from Pteris wallichiana and identified as 6,7-tetrahydrofuran-(2S, 3S)-pterosin C-3-O-β-D-(6′-acetyl)-Glu (1), (2S, 3S)-pterosin C-3-O-β-D-Glu (2), (2S)-pterosin A (3) and (2S)-13-hydroxyl-pterosin A (4), (2R, 3S)-2-hydroxyl-pterosin C (5). Compound 1 is a new sesquiterpene, compounds 3-5 were isolated for the first time. In vitro bioactivity assay showed that compound 1 was able to inhibit the proliferation of 4T1 and EMT6 cells, and possessed significant anti-triple-negative breast cancer bioactivity.
Four terpenoids were isolated from the neutral portion of petroleum ether extract of Artemisia annua by several chromatographic methods, such as silica gel, MCI Gel CHP-20, ODS, Sephadex LH-20 and semi-preparative HPLC. Their structures were identified by HR-MS and nuclear magnetic resonance spectroscopy. These compounds were defined as (1S,4S,5R,6S,9R,10R)-4-ethoxy-9,10-dimethyloctahydrofuro-(3,2-i)-isochromen-11(4H)-one (1), 3a,4,5,6,6a,7-hexahydro-3,6-dimethyl-9-methyl-2H-naphtho[8a,1-b]furan-2,8(3H)-dione (2), kobusone (3) and 1,2-campholide (4). Compound 1 is a new compound, of which the absolute configuration was established by single crystal X-ray crystallographic analysis. Compound 2 is a new natural product. Compounds 3 and 4 are first isolated from the Artemisia genus.
Six compounds including three new compounds were obtained from the fruiting bodies of Ganoderma lucidum in Baoshan area. These structures were identified as baosacid A (1), baosside A (2), ethyl 2,5-dihydroxy-γ-oxobenzenebutanoate (3), australins A (4), 2,5-dihydroxy-γ-oxobenzenebutanoic acid (5), and methyl 2,5-dihydroxy-γ-oxobenzenebut anoate (6) on the basis of spectroscopic methods. In addition, compound 5 is a newly occurring natural product.
The genus Gynostemma, with abundant plant resources, is widely distributed in China. Gynostemma plants have gathered widespread attention both domestically and internationally due to their abundant contents of diverse dammarane triterpenoid saponins and various promising pharmacological activities. At present, the studies on the chemical constituents and pharmacological activities of Gynostemma plants mainly focus on G. pentaphyllum (Thunb.) Makino and G. longipes C. Y. Wu ex C. Y. Wu & S. K. Chen, with less attention given to other species within genus. In this study, the chemical constituents of G. burmanicum King ex Chakrav were systematically identified by ultra-high performance liquid chromatography-quadrupole-time of flight-mass spectrometry (UHPLC-Q-TOF-MS). Firstly, the LC-MS analysis of G. burmanicum from different sources was carried out to evaluate the consistency. According to the mass spectrometry fragmentation pattern of dammarane triterpenoid saponins from Gynostemma, the fragmentation characteristics of malonylated and acetylated saponins, combined with the self-built database and online database such as ChemSipder, SciFinder, PubChem, the chemical components of G. burmanicum were identified. The similarities and differences in the components between G. burmanicum and G. longipes were further assessed by comparing their base peak chromatogram. The experimental results indicated a good consistency in the composition of G. burmanicum samples from different sources. A total of 47 chemical components were identified from G. burmanicum, including 12 flavonoids and 35 triterpenoid saponins, among which 6 were new compounds. Saponins in G. burmanicum generally exhibited malonylation and acetylation, appearing after the corresponding prototypical saponins on a reversed phase chromatography. The base peak ion (BPI) chromatograms showed that the saponins of G. burmanicum were highly consistent with those of G. longipes, with comparable contents of the main components gypenoside XLIX and gypenoside A and their malonylated derivatives. In summary, this study comprehensively clarified the chemical composition and characteristics of G. burmanicum, which provided an experimental basis for the development and utilization of G. burmanicum.
The study aims to provide an important basis for IMH020 production process and quality control and develop an HPLC method for the determination of related substances in IMH020. The analysis was performed on a Waters Symmetry C18 column (250 mm × 4.6 mm, 5 µm). The mobile phase A was acetonitrile and the mobile phase B was water-0.2% glacial acetic acid solution with isocratic elution. The flow rate was 1.0 mL·min-1 and the column temperature was maintained at 30 ℃. The wavelength was 270 and 300 nm. The injection volume was 10 μL. The results show that all the related substances gained a completely chromatographic separation. Good linear relationships of all the related substances (I-1, I-2, I-3a, I-3b, I-4 and I-5) were obtained (r ≥ 0.998 9) and recoveries were in the range of 93.1%-97.8% (RSD ≤ 2%, n = 9). Only I-3a and I-3b were detected below the limit for specified impurities in the three batches of samples, and the largest unspecified single impurity and the total impurities were within the limit. The HPLC method established in this paper is simple, sensitive and accurate, and can be used for the determination of related substances of IMH020.
Based on mass spectrometry imaging method, we investigated the effects of Panax notoginseng in improving diabetic retinopathy (DR) and interfering with corneal, vitreous and retinal metabolites, to reveal the mechanism of Panax notoginseng's action in improving DR. All animal experiments were approved by the Experimental Animal Ethics Committee of Beijing University of Chinese Medicine (Approval No.: BUCM-2023052204-2117). Streptozotocin (STZ)-induced diabetes mellitus (DM) rat model was used, and fasting blood glucose (FBG) and glucosylated serum protein (GSP) levels were measured in each group of rats. Occludin and zonula occludens-1 (ZO-1) were detected by immunofluorescence staining; air flow-assisted desorption electrospray ionization mass spectrometry imaging (AFADESI-MSI) was used to detect endogenous metabolites in the cornea, vitreous, and retinal microregions of the eyes of rats in the DM group and Panax notoginseng group. Endogenous metabolites were detected in the cornea, vitreous, and retinal microregions of the DM and Panax notoginseng groups, and the DM and Panax notoginseng groups were screened for different metabolites by principal component analysis (PCA) and orthogonal partial least squares discriminant analysis (OPLS-DA). Differential metabolites were screened in the DM and Panax notoginseng groups, the in situ spatial information of differential metabolites in each microregion was analyzed, and the related metabolic pathways were analyzed by the Kyoto encyclopedia of genes and genomes (KEGG) database. The results showed that compared with the DM group, diabetic rats in the Panax notoginseng group showed a decreasing trend in both FBG and GSP, and an increase in the expression of ZO-1 and occludin in the retina (P < 0.001); AFADESI-MSI analysis showed that there were a total of 34 differential metabolites in the cornea, vitreous body, and retinal microregion in the Panax notoginseng group, of which Panax notoginseng called back 13 differential metabolites. In the retinal microregion, Panax notoginseng significantly regulated lysophosphatidylserine (18∶0), phosphatidylethanolamine (34∶2) and phosphatidylserine (40∶7/42∶7). The metabolic pathway enrichment results indicated that Panax notoginseng mainly regulated glycerophospholipid metabolism, glycosylphosphatidylinositol synthesis, niacin and nicotinamide metabolism as well as glycerol ester metabolic pathways. In conclusion, Panax notoginseng improves the blood-retinal barrier (BRB) in diabetic rats, and its mechanism of action may be closely related to glycerophospholipid metabolism. This study provides scientific evidence for the mechanism of action of Panax notoginseng in improving DR, and demonstrates the potential of mass spectrometry imaging technology applied to the study of pharmacological mechanisms.
Dendritic cells (DCs) play a critical role in both innate and adaptive immunity, particularly in regulating antitumor immune responses. However, immunosuppressive cytokines in the tumor microenvironment and lipid peroxidation imbalance within DCs limit their ability to activate tumor-specific T cells effectively. To address this, we developed a novel biomimetic nanodrug delivery platform using artificial intelligence (AI). This platform encapsulates curcumin nanoparticles in bacterial outer membrane vesicles (OMVs) to enhance DCs function through a dual approach: targeted drug delivery and immune activation. In vitro experiments demonstrated that curcumin reduced lipid peroxidation stress in DCs by modulating the IRE1α-XBP1 signaling pathway, thereby restoring their antigen-presenting function. Additionally, OMVs not only acted as efficient drug carriers but also as immune activators, promoting DCs maturation and enhancing tumor-specific immune responses. This study presents a promising strategy for improving antitumor immunotherapy and offers new insights into the application of AI in drug delivery systems.
Plasma exosomes (Pla-Exos) were extracted from rats by ultracentrifugation. The ultracentrifugation method extracted rat Pla-Exos at a speed of 150 000 ×g for 2.5 h. Various purification methods including ultracentrifugation, magnetic bead capture method, and ultrafiltration would be employed to purify Pla-Exos. The Pue-Exos were prepared via sonication-assisted and co-incubation methods. The influence factors and levels of the preparation of plasma exosomes carrying puerarin (Pue-Exos) were investigated by RSM plus CCD method with encapsulation rate as an index. Then the characterization, the stability, and in vitro release of Pue-Exos were determined. The particle sizes of exosomes purified by ultracentrifugation, ultrafiltration, or magnetic bead capture method were all within the range of 30-150 nm. The Western blot results showed that purified Pla-Exos and Pue-Exos contained marker proteins TSG101, CD63, and CD81. The TEM showed that purified Pla-Exos and Pue-Exos exhibited well-defined double-layered membrane vesicle structures. The optimal prescription conditions for preparing Pue-Exos were finally determined as follows: 1 h ultrasound time, 39 W ultrasound power, mass ratio of 10∶1. The prepared Pue-Exos exhibit good stability and sustained release, significantly enhancing the in vitro transpermeability of puerarin across the blood-brain barrier (P < 0.01). This study was approved by the Experimental Animal Ethics Review Committee of Hebei North University, and ethics approval number was HBNV202307012103.
Polygonatum Mill. (Asparagaceae) is a pharmaceutically important genus with many species are of significant medicinal value. Taxonomy and interspecific identification of Polygonatum species have long been controversial due to their considerable morphological variation, wide geographic distribution, complex speciation processes, and lacking of high-resolution molecular markers. To evaluate species discrimination power of 14 plastid divergence hotspot regions (candidate sequences) and their combinations in Polygonatum, a total of 166 individuals from 32 populations representing 15 medicinal Polygonatum species distributed in China were sampled for study. The interspecific and intraspecific genetic variation of each sequence and sequence combination were estimated, and tree-based and pairwise genetic distance (PWG-distance) methods were applied. The results indicated that except for trnT-trnL, the designed primers for all the other 13 candidate sequences showed good universality. Varying degrees of overlaps were detected between intraspecific and interspecific genetic distances in each of the 14 single candidate sequences and their combinations. Nonetheless, overlaps in the combined sequences were significantly lower than those in single sequences. Species resolution of the 14 single sequences were 6.67%-40% and 20%-60% based on tree-based and PWG-distance methods, separately. The combined sequences possessed higher species-resolving power with 40%-73.33% by tree-based method and 46.67%-73.33% by PWG-distance method, accordingly. Among them, the combined sequences C0 and C1 (in both tree-based and PWG-distance methods), C2 and C3 (in tree-based method), and C25 (in PWG-distance method) all showed the best resolution degree of 73.33%, indicating that combination of sequences could effectively improve species discrimination power. In addition, sequences psaJ-rpl33, rps16-trnQ, trnF-ndhJ, trnT-trnL, trnK-matK and atpF all exhibited relatively higher species-resolving degree, which could be used as specific molecular markers for the identification of medicinal Polygonatum species, and we propose the combination of psaJ-rpl33+rps16-trnQ+trnF-ndhJ+trnK-matK+atpF as the most ideal high-resolution molecular marker for discriminating the medicinal Polygonatum. This study will provide a basis for conservation and utilization of germplasm resources and accurate identification of medicinal Polygonatum, as well as standardizing the market for Polygonati Rhizoma.
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