Latest ArticlesThirteen compounds were isolated from the Lycii Cortex by macroporous resin column chromatography, gel column chromatography and semi-preparative high performance liquid chromatography. The structures of the isolated compounds were identified by ultraviolet spectroscopy, infrared spectroscopy, nuclear magnetic resonance spectroscopy and mass spectrometry as solavetivone A (1), solavetivone B (2), 9-hydroxy-3-methoxy-6H-pyrido [1, 2-a] pyrazin-6-one (3), 5, 5′-di(2-ethyl-hexyloxy)-5, 5′-bifuran (4), bis(2-ethylhexyl) phthalate (5), scopoletin (6), periplogenin (7), 3β, 5β-dihydroxy-14-en-card-20(22)-enolide (8), (7R, 8S)-4-hydroxy-3, 5′-dimethoxy-4′, 7-epoxy-8, 3′-neoligna-9, 9′-diol-4-O-β-D-glucopyranosyl-(1→4)-β-D-glucopy-ranoside (9), 2-carbomethoxy 3-prenyl-1, 4-naphtho hydroquinone-1, 4-di-O-β-glucoside (10), 4-hydroxy-3-methoxyphenyl-β-D-xylopyranosyl (1→6)-O-β-D-glucopyranoside (11), syringic acid (12), vanillic acid (13). Compounds 1 and 2 were new sesquiterpene glycosides with solavetivone skeleton. Compounds 4, 8-10 were isolated from Solanaceae for the first time. The bioactive screening results indicate that compounds 1 and 2 do not exhibit inhibitory effects on NO production; however, they demonstrate weak inhibitory activity against α-glucosidase.
The chemical components of the patchouli oil were isolated and purified by silica gel column chromatography, preparative thin layer chromatography and semi-preparative HPLC. Then, the structures of the obtained compounds were identified by HR-MS, IR, and NMR. The absolute configurations of the novel compounds were determined by single-crystal X-ray diffraction analysis and calculation of ECD. Finally, two novel spirocyclic sesquiterpenoids were obtained from patchouli oil and identified as spiroaxanol A (1) and spirojatamone A (2), respectively.
This study employs homogeneous time-resolved fluoroimmunoassay to quantitatively determine the concentration of cyclic adenosine monophosphate (cAMP) within LHCGR(-Ex10)-CRE-luc-HEK293 cells, utilizing a competitive immunoassay method. The research sets forth an in vitro biological activity assessment methodology for luteinizing hormone (LH). Key parameters of the methodology are optimized, and the relative accuracy, intermediate precision, linearity, and range are validated. The optimized experimental conditions are defined as follows: an initial concentration of 200 nmol·mL-1, a seven-fold gradient dilution, a cell density of 24 000 cells·well-1, and a duration of incubation of 30 min. The findings indicate that the method exhibits excellent linearity across a relative potency range of 64% to 156%, high relative accuracy, and satisfactory intermediate precision. The successful establishment and validation of a homogeneous time-resolved fluoroimmunoassay for the evaluation of LH biological activity is reported. This methodology is applicable for the assessment of biological activity and quality control of recombinant LH-like drugs, as well as for the differentiation of recombinant LH.
An integrated method based on UPLC-Q-Orbitrap-HRMS and ICP-MS was developed for the simultaneous characterization of chemical constituents and inorganic elements in brown sugar hand-crafted in the Ailao Mountain. After water extraction and ethanol precipitation, thirty metabolites were identified by UPLC-Q-Orbitrap-HRMS, including 10 amino acids and their derivatives, 8 sugars and derivatives, 4 organic acids, 3 aldehydes and 5 other organic compounds. ICP-MS quantified the elemental profiles of three independent batches, revealing high levels of the macro-elements K, Mg and Ca, along with nutritionally relevant amounts of the trace elements Fe, Zn, Cu, Se, Co, Mn and Cr. Fingerprinting, elemental correlation analysis and health-risk assessment were subsequently performed. Estimated daily exposure per kg body weight (Exp), hazard index (HI) and margin of exposure (MOE) indicated that all batches conformed to the heavy-metal limits set by the Chinese Pharmacopoeia (2025 edition), and the overall health risk from toxic elements is negligible. By integrating comprehensive chemical profiling with precise elemental quantification, the study establishes a dual-dimension quality evaluation system that provides robust data and technical support for constructing a quality profile of Ailao Mountain brown sugar and for elucidating the relationship between its chemical composition and nutritional functions.
Rheumatoid arthritis (RA) is a disease that seriously affects human health, and the existing treatments have the disadvantages of high side effects, drug resistance and poor effectiveness. In this study, we proposed a new anti-RA strategy based on the cross-linked hydrogel "acupuncture + swelling" dual stimulation of acupoints, and investigated the efficacy of brucine hydrogel microneedles targeting for RA in mice. All animal experimental procedures were approved by the Guizhou University of Traditional Chinese Medicine Laboratory Animal Ethics Committee (No: 20230179) and conducted in accordance with its guidelines. A mouse model of collagen-induced arthritis (CIA) was established, and the efficacy was investigated by using the swelling of the paw, spleen and thymus indices, histopathological sections of the ankle joints, serum levels of inflammatory factors and synovial tissue proteins, and it was found that the acupoint microneedling group and the acupoint + non-acupoint microneedling group could significantly decrease the swelling of the paw in the mouse model of CIA, reduce the swelling of the immune organs of the mice, reduce the levels of serum inflammatory factors, and improve the efficacy of CIA. Inflammatory factor content, improve the pathological state of synovial membrane and cartilage tissue of ankle joint and down-regulate the expression level of related inflammatory proteins in CIA mice, which has the effect of alleviating rheumatoid arthritis. The therapeutic strategy of brucine hydrogel microneedles based on "acupuncture + swelling" to stimulate the Zusanli (ST36) acupoint can significantly treat rheumatoid arthritis, which provides an important scientific basis for the subsequent development and utilisation of acupoint microneedles transdermal drug delivery system.
This study developed hyaluronic acid (HA)-modified, ginsenoside Rg3-loaded hollow mesoporous MnO2 nanoparticles (HMR@HA) and evaluated their characterization, in vitro release, and anti-triple-negative breast cancer efficacy. Hollow mesoporous MnO2 nanoparticles (HM) were synthesized by template method. HMR nanoparticles were prepared by loading ginsenoside Rg3, and then targeted HMR@HA system was constructed through HA modification. Laser particle size analysis, transmission electron microscopy (TEM), and Fourier transform infrared spectroscopy (FTIR) were used to characterize the samples. High-performance liquid chromatography (HPLC) quantified Rg3 loading capacity and assessed HMR@HA's in vitro release profile. We evaluated the uptake capacity of 4T1 cells for nanoparticles and the in vitro antitumor activity of nanoparticles. The experimental results indicate that the optimal preparation parameters are: the mass ratio of drug to carrier of 5∶1, the stirring time of 12 h, and the drug concentration of 10 mg·mL-1. The obtained HMR@HA exhibits the uniform hollow structure with a particle size of 216.3 ± 1.3 nm and the loading capacity is (42.42 ± 2.55)%. The release curve shows pH dependence, and the cumulative release gradually increases as the pH decreases. The results showed that HMR@HA was efficiently taken up by 4T1 cells and significantly inhibited the proliferation and migration of cancer cells. Active oxygen and mitochondrial membrane potential detection showed that HMR@HA can promote tumor cell apoptosis. HMR@HA has a high drug loading capacity and pH-sensitive drug release properties. Compared with ginsenoside Rg3, it significantly enhances antitumor activity and induces apoptosis, providing an effective treatment strategy for triple-negative breast cancer.
Lipid nanoparticles (LNP) are highly promising gene delivery platform due to their high safety, good stability, and excellent nucleic acid encapsulation efficiency. However, current clinical gene therapy primarily relies on invasive administration routes. The development of compliant, non-invasive delivery routes, such as oral administration, is crucial. Nevertheless, creating gastric acid-resistant oral gene delivery vectors faces a critical bottleneck that nucleic acid therapeutics are highly susceptible to degradation in the harsh acidic environment (pH 1.5-4.5) of the gastrointestinal tract. To address this, we constructed a cholesterol-enriched hybrid system (RLSC/OMVC) based on an amphiphilic cationic lipopeptide (RLS) and Escherichia coli outer membrane vesicles (OMV). This system demonstrates efficient gene delivery capability under both neutral and acidic conditions, along with excellent in vitro biocompatibility. The study characterized the physicochemical properties of different formulations (RLS, RLSC, OMV, and OMVC). In vitro cell transfection experiments showed that the gene delivery efficiency of RLSC/OMVC under acidic condition (pH 4.5) was significantly increased by nearly 3-fold compared with Lipofectamine 2000. Furthermore, transmission electron microscopy observation, particle size/zeta potential analysis, and gel electrophoresis experiments revealed the mechanism by which OMV and cholesterol synergistically protect plasmid DNA from acidic degradation in conjunction with lipid peptide. The developed RLSC/OMVC hybrid system boasts integrated advantages of exceptional acid resistance, high-efficiency gene delivery, and good biocompatibility. This work provides an innovative strategy for oral gene therapy.
Pregnane X receptor (PXR), a crucial member of the nuclear receptor superfamily, is predominantly expressed in the liver and intestine and serves as a key transcription factor regulating the expression of various drug-metabolizing enzymes and transporters. Beyond its classical role in xenobiotic detoxification, PXR also plays an important role in the metabolism of endogenous substances such as bile acids, lipids, and glucose. In recent years, extensive studies have demonstrated that PXR is closely associated with a variety of hepatic and intestinal diseases, including drug-induced liver injury, metabolic dysfunction-associated fatty liver disease, cholestasis, inflammatory bowel disease, and hepatointestinal malignancies. Multiple PXR agonists—including endogenous ligands, natural products, and synthetic small molecules—have shown significant potential in restoring metabolic homeostasis, regulating inflammation, and maintaining hepatic and intestinal functions. This review highlights the central role of PXR in metabolic regulation, systematically summarizes its mechanisms and recent advances in hepatic and intestinal diseases, and focuses on the development and clinical translation of PXR agonists, aiming to provide a theoretical basis for PXR-targeted therapeutic strategies against liver and intestinal disorders.
Farnesoid X receptor (FXR) is a member of the nuclear receptor superfamily and is highly expressed mainly in the liver and intestine. As a transcription factor regulating the expression of multiple target genes, FXR not only regulates bile acid, glycolipid, and microbial metabolism through a number of different metabolic pathways, but also plays an important role in inflammation, cell proliferation, differentiation, apoptosis, and cancer growth. FXR is now recognized as a key component in the regulation of various digestive diseases such as primary sclerosing cholangitis (PSC), primary biliary cholangitis (PBC), metabolic dysfunction-associated steatotic liver disease (MASLD) and inflammatory bowel disease (IBD). In recent years, significant progress has been made in the development of agonists and antagonists targeting FXR, but their clinical application still faces the challenge of balancing efficacy and safety. Based on the core physiological functions of FXR in regulating bile acid metabolism, glucose-lipid homeostasis and inflammatory response, this article systematically analyzes the mechanism of action and clinical translation of novel FXR agonists and antagonists, focusing on their therapeutic potential in digestive diseases such as PSC, PBC, MASLD and IBD, and the prospective development of drugs based on the precise regulation strategy of FXR.
Pregnane X receptor (PXR), an important member of the nuclear receptor superfamily, serves as a sensor for xenobiotics and regulates the expression of drug-metabolizing enzymes and transporters. Recent studies have revealed that PXR is not only involved in drug metabolism and detoxification but also plays a critical role in glucose metabolism, lipid metabolism, bile acid homeostasis, and inflammatory regulation. As a ligand-activated transcription factor, PXR regulates downstream target genes expression, thus defending the body from xenobiotic and endogenous toxin attacks. PXR is associated with the development of a number of metabolic diseases such as obesity, type 2 diabetes mellitus, metabolic dysfunction-associated fatty liver disease, cholestatic liver diseases, cardiovascular diseases, etc. However, the regulatory mechanism of PXR in the context of glucose, lipid, cholesterol, and bile acid metabolism are complex and vary depending on nutritional status, species, and tissues. Therefore, developing drugs that selectively regulate PXR and its downstream signaling pathways may represent a promising strategy for treating metabolic diseases in the future. We review the structural and functional characteristics of PXR in the article, its transcriptional regulatory mechanisms, and the research progress of PXR as a therapeutic target for metabolic diseases. We summarize the research progress of drugs targeting PXR for the treatment of metabolic diseases, aiming to provide insights for future drug development targeting the PXR receptor for metabolic diseases treatment.
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