Using separation methods such as silica gel, MCI, ODS, Sephadex LH-20 gel column chromatography, and high-performance liquid chromatography, two C21 steroid components were isolated and identified from the traditional medicinal plant Munronia unifoliolata Oliv. (commonly known as "Aituotuo"), which is used for treating rheumatic joint pain and traumatic injuries. The structures of these compounds were identified as 2α, 3α, 15β-trihydroxy-20(S)-benzoyl-pregnane (1) and 2α, 3α, 15β-trihydroxy-20(S)-tigloyl-pregnane (2) using comprehensive structural identification methods, including UV, IR, high-resolution mass spectrometry, and one-dimensional and two-dimensional nuclear magnetic resonance. Compounds 1 and 2 were reported for the first time as pregnane-type components from M. unifoliolata, with compound 1 being a new compound. The results of the bioactivity screening indicated that both compound 1 and compound 2 did not inhibit nitric oxide (NO) production and showed no activity in reversing multidrug resistance.

The rice fermentation products of the fungus Scedosporium aurantiacum GXIMD 02519 were isolated and purified by silica gel column chromatography and semi-preparative liquid chromatography, etc. Their structures were characterized by various spectroscopic methods, including HR-ESIMS and NMR, etc. The inhibitory activity of nuclear factor kappa-B (NF-κB) and osteoclast differentiation of these compounds were determined by approaches of NF-κB luciferase reporter gene and tartrate-resistant acidic phosphatase (TRAP) staining. A new azaphilone, isochromophilone M (1), along with nine known compounds, were isolated and identified from the fungus S. aurantiacum GXIMD 02519, which were identified as 6-((1E, 3E)-3, 5-dimethylhepta-1, 3-dien-1-yl)-2, 4-dihydroxy-3-methylbenzaldehyde (2), barbatinic acid (3), botryorhodine B (4), 2, 6-dihydroxy-3, 4-dimethylbenzoic acid methyl ester (5), 2, 4-dihydroxy-3, 6-dimethylbenzoic acid (6), atranol (7), 4-methoxyphenylacetic acid (8), 4-hydroxybenzaldehyde (9), and scopararane C (10). Compounds 3 and 10 showed inhibitions of lipopolysaccharide (LPS)-induced NF-κB activation in RAW264.7 cells. Moreover, compound 10 could further inhibit receptor activator of nuclear factor κB ligand (RANKL)-induced osteoclast differentiation in bone marrow macrophages without observed cytotoxicity. This is the first report of the diterpene compound (10) as a potential inhibitor of osteoclast differentiation.

Seventeen compounds were isolated from the ethyl acetate extract of the tubers of dry Alisma plantago-aquatica by silica gel, Sephadex LH-20 and high performance liquid chromatography. All of them were identified as the prototerpene triterpenoids by the analysis of mass spectrometry and nuclear magnetic resonance spectroscopy. Compounds 1 and 2 are the new compounds. Among of them, 16 compounds were screened for α-glucosidase inhibitory activity, however, none of them was active.

Gliomas represent highly malignant brain tumors with high recurrence rates, susceptible to drug resistance and difficult to treat, therefore finding and screening new therapeutic candidates is extremely significant. In this study, we firstly used UHPLC-Q/TOF-MS method to identify the chemical constituents of Scutellaria barbata extract, and a total of 38 constituents were identified. A microfluidic chip model containing six independent U251 cell units was constructed, each U251 cell unit consisted of three parallel channels, the middle channel was used for culturing matrigel-encapsulated U251 cells, and the channel of medium or drug-containing medium was on both sides, the U251 cells formed a multicellular sphere in the matrigel, and were able to mimic the microenvironment of tumor hypoxia to a certain extent. Based on the constructed glioma microfluidic chip model and the perfusion flow mode for the screening of active components of Scutellaria barbata which had antitumor activity, the perfusion samples of Scutellaria barbata were analyzed by using UHPLC-Q/TOF-MS, and the relative concentrations of potential active components were calculated by the internal standard method, and it was found that the constituents of the samples containing scutellarin, apigenin-7-O-β-D-glucuronide, luteolin, scutellarein, naringenin and apigenin were significantly decreased (P < 0.05), suggesting that these six compounds have potential anti-glioma activity. Using CCK-8 assay, scratch assay and apoptosis assay to validate the medicinal efficacy of the six potential active components obtained from the screening, it was observed that all the six potential active components could reduce the proliferation of U251 cells, decrease the migration rate of the cells, and kill the cells by apoptosis. The sensitization of temozolomide performed by the six potential active compounds was further investigated, which indicated that naringenin, apigenin and luteolin in combination with temozolomide individually increased the sensitivity of U251 cells to temozolomide as well as decreased the cell viability. These results will provide technical and scientific evidence for treating glioma and further solving the anti-drug resistance phenomenon of glioma treatment by Scutellaria barbata and its active components.

This study investigated the effects of acteoside (ACT) on serum metabolites in purinomycin aminonucleoside (PAN)-induced chronic glomerulonephritis (CGN) in young rats using non-targeted metabolomics and lipidomics, and initially explored its potential mechanism of efficacy. The experiment was approved by the Animal Welfare Ethics Committee of Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences (No. 2022B152). Firstly, ELISA kits were used to detect serum cytokines including IP-10, IL-6, IL-1β, and TNF-α in rats of each group to evaluate the efficacy of ACT. Non-targeted metabolomics and lipidomics techniques were used to determine metabolites and lipids in serum, and integrated analysis was conducted to reveal the mechanism. The results showed that compared with the model group, the levels of IP-10, IL-6, IL-1β, and TNF-α in the serum of the ACT groups were significantly reduced, indicating a significant pharmacological effect of ACT. Non-targeted metabolomics results revealed that 23 different metabolites were identified between the control and model groups, involving pathways such as biosynthesis of unsaturated fatty acids, biosynthesis and degradation of valine, leucine, and isoleucine, and linoleic acid metabolism. Between the ACT and model groups, 25 different metabolites were identified, involving pathways such as biosynthesis of unsaturated fatty acids, the TCA cycle, and linoleic acid metabolism. Lipidomics results showed that 68 significantly different lipids were identified between the control and model groups, involving pathways such as omega-3/omega-6 fatty acid synthesis, T-cell receptor and costimulatory signaling, and G-protein-coupled receptor activation of PKC. After ACT treatment, significant changes were observed in 67 differential lipids, with notable reversal in the aforementioned pathways. It also regulated PPARα modulation of lipid metabolism and related pathways such as α-linolenic acid and linoleic acid metabolism. Correlation analysis of differential metabolites and lipids indicated that metabolites such as homovanillic acid, palmitic acid, indoxyl sulfate, as well as triglycerides and phosphatidylcholines were critical. The commonly regulated pathways by non-targeted metabolomics and lipidomics were biosynthesis of unsaturated fatty acids and linoleic acid metabolism. In conclusion, ACT primarily treats CGN in young rats by regulating the biosynthesis of unsaturated fatty acids and linoleic acid metabolism pathways through differential lipids such as triglycerides and some phosphatidylcholines, and differential metabolites such as homovanillic acid, palmitic acid, and indoxyl sulfate. This study initially elucidated the intervention mechanism of ACT in the treatment of pediatric chronic glomerulonephritis from the perspective of serum metabolism, laying a solid foundation for the rational clinical application of ACT in children with CGN.

Rhubarb is a Chinese medicinal herb of multiple origins, there are differences in the purgative efficacy of three origins of rhubarb, and the active components of the purgative efficacy of rhubarb is not yet clear. The study reveals the differences in the purgative efficacy of three origins of rhubarb by method of pseudo-targeted metabolomics combined with pharmacological experiments (approval number: BUCM-4-2022080301-3026), and screens out the active components of the purgative efficacy of rhubarb. Analyzing the differences in the purgative efficacy of three origins of rhubarb through animal pharmacological experiments. Subsequently, potential active components of purgative efficacy were identified through literature review, and corresponding ion pairs were obtained by fragmentation pathways and software optimization, and the peak areas of each component were obtained by using dyMRM mode of QQQ-MS. Multivariate statistical analysis was used to analyze the potential active components of purgative efficacy in rhubarb with different origins, thereby achieving pseudo-targeted metabolomics analysis, and the active components can be screened with pharmacological experimental results. The pharmacological experimental results indicate that the purgative efficacy of Rheum tanguticum Maxim. ex Regel is significantly higher than that of Rheum palmatum L. and Rheum officinale Baill. The results of PCA showed that there were significant differences in the potential active components of purgative efficacy among three origins of rhubarb. 97 differential potential active components of purgative efficacy were screened through OPLS-DA combined with Kruskal Wallis test; combined with the results of metabolomics, 23 active components of purgative efficacy were screened, among which the compounds with clear chemical structures were sennoside A, sennoside B, rheinosides A, rheinosides C, rheinosides D, physcion-8-O-glucoside, rhein-8-O-glucoside, chrysophanol-1-O-glucoside. The above results suggest that the method of pseudo-targeted metabolomics combined with pharmacological experiments has been used to clarify the relationship of purgative efficacy between the three origins of rhubarb, reveal the distribution of potential active components of purgative efficacy in three origins of rhubarb, and screen out the active components of purgative efficacy. This not only provides a theoretical basis for the quality evaluation and precise clinical use of rhubarb, but also provides a new idea for traditional Chinese medicine to search for efficacy markers.

A new vardenafil analogue has been discovered in a sexual enhancement health beverage through the application of ultra-high performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UHPLC/Q-TOF MS) and high-performance liquid chromatography-diode array detection (HPLC-DAD). This analogue was then purified via preparative HPLC (Prep-HPLC), and its chemical structure was determined using NMR spectroscopy. Spectral data indicated that the vardenafil analogue possesses an n-propyloxy group in place of the ethoxy group on the aromatic ring, and a hydroxyethyl group in substitution for the ethyl group on the piperazine ring. The compound, termed "propoxyphenyl hydroxyvardenafil", has not been reported in China.

This study aimed to investigate the effects of colloidal silica nanoparticles Aerosil 200 (A200) on intestinal barrier and mucosal immunity in childhood mice. Three-week-old BALB/c mice were administered A200 (20, 50, 200 mg·kg^-1) via gavage for 7 days. Intestinal morphology, barrier function, immune cell phenotypes, and oral tolerance were systematically evaluated. Histopathological analysis of intestinal morphology revealed that no obvious pathological damage in the intestine. However, 200 mg·kg^-1 A200 increased ileal villus length, reduced crypt depth. Functional assessments of the intestinal barrier demonstrated that 200 mg·kg^-1 A200 upregulated ZO-1 in the ileum but downregulated it in the colon; The intestinal stem cell marker Lgr5 remained unchanged, while Mucin-2 increased and lysozyme decreased in the ileum. Analysis of immune cell phenotypes revealed that the 200 mg·kg^-1 group exhibited elevated proportions of Treg and Th2 cells in the mesenteric lymph nodes, while serum and intestinal levels of TNF-α and IL-6 remained unaffected. Oral tolerance assays revealed no alteration in OVA-specific IgG, IgG1, or IgG2a antibody levels. Animal welfare and the animal experimental protocols were strictly consistent with related ethics regulations of Peking University Health Science Center (Approval No.: BCJB0076). In conclusion, A200 is generally safe for childhood mice but may modulate epithelial barrier proteins and immune cell phenotypes at high doses, which may provide insights into its pediatric application.

To investigate the transformation of wettability of phosphoric acid-treated pollen after treatment with different reagents, to optimize the preparation of the wettability-transformed pollen sporopollenin carrier system to find the optimal alkali treatment conditions, and to characterize its structure and surface morphology, we first analyzed the wettability of the original pollen and the acid-dissolved pollen, measured the water contact angle of the acid-dissolved pollen treated with each reagent with the help of a contact angle tester, conducted a one-way test on the alkali treatment conditions that could transform the wettability of the pollen, explored the influence of the optimization of the conditions for the preparation of the hydrophilic pollen sporopollenin carriers by using a response surface methodology and the glycerol absorption time as the response value, and carried out a validation and verification test on the process parameters. The process parameters were verified and validation tests were conducted, and finally the sporopollenin was characterized by FTIR and SEM. The contact angle test showed that the water contact angle of pollen after acid digestion was 135.1°, which was changed to 16° after NaOH treatment, and the contact angle of glycerol was changed from 140.8° to 9.6°. The best alkali treatment process was obtained through the optimization of one-factor test and response surface method, and the final optimization conditions were obtained according to the actual experimental process: the volume of NaOH was 105 mL, i.e., 15 times the volume of pollen, and the concentration of NaOH was 1.5 mol·L^-1. The stirring time was 18 h, and the stirring temperature was 85 ℃. Under these conditions, three parallel experiments were carried out to verify the wettability of Codonopsis pollen and Lotus pollen respectively, in which the average value of Codonopsis pollen results was 58 s, and the average value of Lotus pollen results was 49 s, and the RSD was less than 5%. The wettability study revealed that pollen sporopollenin changed from hydrophobicity to hydrophilicity after NaOH treatment, and according to the results of response surface optimization, the prepared alkali-treated pollen sporopollenin showed a significantly shorter time for complete glycerol absorption and a better hydrophilicity with a water contact angle of close to 0°, which is a reproducible process and a stable and reliable preparative process, and theoretically, will be more conducive to the loading of hydrophilic drugs.

Acute myeloid leukemia (AML), characterized by rapid progression, therapeutic resistance, and high relapse rates, remains a critical threat to patient survival. The complex leukemic microenvironment often diminishes the efficacy of conventional monotherapies and single-target approaches. Drug delivery strategies based on microenvironment characteristics and multi-mechanism synergy are expected to have better therapeutic effects on AML. Therefore, we developed a biomimetic supramolecular nanoparticle (Fe-GA@CM) through homologous targeting strategy and metal-polyphenol coordination for co-delivery of gambogic acid (GA) and Fe³⁺. The particle size, zeta potential, and release performance of the system were characterized. Furthermore, the efficacy and mechanism of action of this system in treating AML was explored. The results showed that the particle size of the nano system was approximately 270 nm and positively charged. After being specifically taken up by AML cells, it is reduced by high concentrations of glutathione in the tumor microenvironment and released Fe²⁺ and GA in a responsive manner. The combination therapy for AML is achieved by inducing ferroptosis with Fe²⁺ and inhibiting glycolysis in AML cells with GA. In summary, the formulated Fe-GA@CM provides novel ideas for targeted therapy and combination therapy for AML.