Latest ArticlesEleven compounds were isolated from Eucommia ulmoides by silica gel, Sephadex LH-20, HW-40C column chromatography and semi-preparative HPLC. Their structures were identified by modern spectroscopic methods as neoeucommiate A (1), (7S, 8R)-dihydrodehydrodiconiferyl alcohol (2), urolignoside (3), ficusal (4), tiruneesiin (5), glochidioboside (6), forsythialansides B (7), ecdysanol B (8), (+)-syringaresinol-4-O-β-D-glucopyranoside (9), (+)-pinoresinol 4-O-[6ʹʹ-O-vanilloyl]-β-D-glucopyranoside (10), samsesquinoside (11). Compound 1 is a new compound, compounds 3-7, 10 and 11 were isolated from Eucommia ulmoides for the first time.
Astragalus polysaccharides are the most immunoregulatory active and abundant substances in Astragalus, with anti-tumor, anti-viral, and immune-promoting biological activities. They have been widely used in clinical practice. Previous studies have found that Astragalus polysaccharides are mainly composed of two different polysaccharides, APS-Ⅰ (> 2 000 kDa) and APS-Ⅱ (10 kDa), with APS-Ⅱ (10 kDa) being the most active component of Astragalus polysaccharides. We used α-1, 4-glucan endo-hydrolysis enzyme to degrade APS-Ⅱ into oligosaccharides, and screened the immune activity of oligosaccharides in vitro. We found that the overall immune activity of 2-9 oligosaccharides was low, while the immune activity of 10-14 oligosaccharides was strong, and the activity was better than that of untreated APS-Ⅱ. To investigate the key structural features of APS-Ⅱ oligosaccharides that play a role in immune activity, we used MALDI-TOF-MS biochemical mass spectrometry and high-resolution mass spectrometry instrument ESI-Q Exactive-MS to analyze the APS enzymatic oligosaccharides. By comparing, we found that 10-14 oligosaccharides contain 1→4 and 1→6 branched structures with coexisting linkages, suggesting that 1→4 and 1→6 linkages in branched structures are key structural features that play a role in the immune activity of APS-Ⅱ, laying a theoretical foundation for the structure-activity relationship of Astragalus polysaccharides and oligosaccharides.
Brother of regulator of imprinted sites (BORIS), also known as CCCTC binding factor-like (CTCFL), is a relatively newly discovered cancer-testis antigen. Drug development related to BORIS has been carried out in multiple directions, including small molecules, small RNA molecules, polypeptides, vaccines, and cellular therapies. Due to its unique ability to interfere with the higher-order spatial structure of the genome, BORIS may represent a new class of drug targets. Here we systematically review the molecular biology research results related to BORIS, including the diversity of its gene products, the multipartite interactions mediated by BORIS, the subsequent impact on signaling pathways, and current drug development strategies, in order to gain a better understanding of the molecular mechanisms of BORIS in both upstream and downstream regulation networks and to identify potential research directions for further breakthroughs.
Sturgeon cartilage has a wide range of applications as it is rich in biologically active substances such as chondroitin sulphate and protein. In this study, the safety evaluation of sturgeon cartilage peptide in NIH/3T3 and C2C12 cells was conducted, and the results showed that sturgeon cartilage peptide did not induce apoptosis and necrosis in NIH/3T3 and C2C12 cells compared to the blank control, which provides an in vitro experimental basis for the transdermal drug delivery of sturgeon cartilage peptide. Further evaluation of the scavenging activity of sturgeon cartilage peptides against the 2, 2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and 2, 2-diphenyl-1-picrylhydrazyl (DPPH) free radicals showed that sturgeon cartilage peptides have strong antioxidant activity. A stable sturgeon cartilage peptide ointment containing 7% sturgeon cartilage peptide was prepared and analysed for its transdermal absorption in mouse skin. This experiment was approved by the Animal Ethics Committee of the Institute of Materia Medica, Chinese Academy of Medical Sciences (approval number: 00007684). It was found that the 12-hour cumulative release of sturgeon cartilage peptide ointment reached 92%. In this study, we further analyzed the ability of sturgeon cartilage peptide ointment to inhibit ear swelling in mice after xylene-induced inflammation. The sturgeon cartilage peptide ointment showed significant anti-inflammatory activity compared to the matrix group and the control group. In conclusion, the present study clearly demonstrated that sturgeon cartilage peptide has good safety and antioxidant activity, and the prepared sturgeon cartilage peptide ointment provides an experimental basis for further application of sturgeon cartilage peptide as well as the study of transdermal drug delivery.
Eleven compounds were isolated and purified from the ethyl acetate part of 80% ethanol extract of Ferula feruloides root by a combination of normal-phase silica gel column chromatography, Sephadex LH-20 dextran gel column chromatography and semi-preparative liquid chromatography and then modern wave spectrometry methods (NMR, MS, UV, IR) were used to identify the structures of the compounds, which were identified as baigene D (1), baigene E (2), baigene F (3), β-kirialovin (4), α-kirialovin (5), falcarindiol (6), ammoresinol (7), dshamirone (8), 2, 3-dihydro-7-hydroxy-2S*, 3R*-dimethyl-3-[4-methyl-5-(4-methy1-2-furyl)-3(E)-pentenyl]-furo[3, 2-c]coumarin (9), 2, 3-dihydro-7-hydroxy-2S*, 3R*-dimethyl-2-[4, 8-dimethyl-3(E), 7-nonadi-enyl]-furo[3, 2-c]coumarin (10), and baigene C (11). Compounds 1-3 are new coumarin analogues, and compounds 4-6 are firstly isolated from F. feruloides. The anti-proliferative activity of compounds 5, 7-11 against human gastric cancer (MKN-45) cells was evaluated using MTT assay, which showed that compounds 7-11 exhibited strong inhibitory activity, and compound 5 exhibited weak inhibitory activity.
Four furan α-butenolactones were isolated from 50% acetone extract of tuber of Alisma orientale by silica gel column, chromatography gel column and high performance liquid chromatography techniques. Their structures were identified by modern wave spectroscopy techniques and electronic circular dichroism (ECD) and assigned as (5R)-5-hydroxy-3, 4-dimethylfuran-2(5H)-one (1), 5-hydroxy-3, 5-dimethylfuran-2(5H)-one (2), 5-hydroxy-4-(1-methylethyl)-2(5H)-furanone (3) and alismanoid A (4). Compound 1 was new compound and compounds 2–4 were first isolated from Alisma orientale. Compound 1-4 had potential antifibrotic activities.
In this study, we investigated the anti-inflammatory effect and mechanism of tilianin in lipopolysaccharide (LPS)-induced RAW264.7 cells. The cell viability was detected by cell counting kit-8 (CCK-8) assay. The content of tumor necrosis factor α (TNF-α) and interleukin-6 (IL-6) were detected by enzyme-linked immuno sorbent assay (ELISA) kits. The content of nitric oxide (NO) was assayed by Griess reagent method. The level of intracellular reactive oxygen species (ROS) was detected by 2', 7'-dichlorodihydrofluorescein diacetate (DCFH-DA) fluorescent probe. The protein levels of Toll like receptor 4 (TLR4), myeloid differentiation primary response gene 88 (Myd88), nuclear factors κB p65 (NF-κB p65), phosphorylated nuclear factor κB p65 (p-NF-κB p65), nuclear factor κB inhibitory protein α (ⅠκBα) and phosphorylation nuclear factor κB inhibitory protein α (p-ⅠκBα) were detected by Western blot. The mRNA and protein levels of NLRP3, pro-IL-1β, pro-IL-18 and pro-caspase-1 were detected by qRT-PCR and Western blot. Immunofluorescence staining was used to detect the nuclear translocation of NF-κB p65. The effect of tilianin on the TLR4/Myd88/NF-κB signaling pathway was further validated by using the TLR4 signaling inhibitor restatorvid (TAK242). The results showed that tilianin significantly reduced the levels of TNF-α, IL-6 and NO in the supernatant of RAW264.7 cells and decreased the content of intracellular ROS. Tilianin reduced the levels of TLR4, Myd88, p-NF-κB p65 and p-ⅠκBα protein and nuclear translocation of NF-κB p65. Tilianin could reduce the protein levels of NLRP3, pro-IL-1β, pro-IL-18 and pro-caspase-1. Tilianin significantly inhibited the mRNA levels of NLRP3 and pro-IL-1β. The above research results indicated that tilianin could significantly alleviate the LPS-induced inflammatory response in RAW264.7 cells and its mechanism might be related to downregulate the TLR4/Myd88/NF-κB signaling pathway to inhibit NLRP3 inflammasome.
In this study, the effective substance group and molecular mechanism of Rhei Radix et Rhizoma-Persicae Semen combination (RRR-PS) in activating blood circulation and dispelling blood stasis were investigated by integrating efficacy experiments, network pharmacology and HPLC. The rat model of blood stasis syndrome was established, and the blood rheology index and coagulation four comprehensive evaluation were carried out. The results showed that compared with the model group, the whole blood viscosity, erythrocyte sedimentation rate and erythrocyte aggregation index of the rats in the RRR-PS group were significantly callback (P < 0.01). Network pharmacology found that RRR-PS combination exerted the effect of activating blood circulation and dispelling blood stasis by acting on calmodulin-1 (CALM1), nitric oxide synthase-2 (NOS2), glucocorticoid receptor (NR3C1) and other targets, regulating platelet activation, peroxisome proliferator-activated receptor (PPAR), vascular endothelial growth factor A (VEGF) and other signaling pathways, and found key components: sennoside B, (+)-catechin, emodin, physcion, rhein, aloe-emodin, chrysophanol, gallic acid. HPLC was used to explore the dissolution rate of key components. The results showed that the contents of catechin, emodin, chrysophanol and physcion were significantly increased after RRR-PS combination (P < 0.01). In summary, RRR-PS has a significant effect on promoting blood circulation and removing blood stasis, and its mechanism of action is related to promoting angiogenesis, anti-coagulation, anti-thrombosis and anti-inflammation. The efficacy is related to the change of solvent system and the large dissolution of catechin, emodin, chrysophanol and physcion after the RRR-PS combination. The results of the study can further provide a reference for the follow-up study on the active substances and mechanism of the RRR-PS combination. Animal experiments have been approved by the Experimental Animal Committee of Shaanxi University of Traditional Chinese Medicine (No. SUCMDL20210309002).
Phellodendri Chinensis Cortex (PCC) featured with thick cortex and bright-yellow is considered to be of high quality according to traditional appearance traits evaluation mode. However, the correlation between appearance traits and internal quality of PCC has not been scientifically revealed. Here, based on the theory of "Quality Evaluation Through Morphological Identification", the correlation of both sides was studied systematically. Firstly, the thickness of PCC slices was measured by vernier calipers for classification, and the colour of PCC slice was estimated by naked eyes and automatic colorimeter and classified. Secondly, high performance liquid chromatography (HPLC) was used to establish fingerprint chromatogram containing 12 characteristic peaks, and the contents of moisture and ethanolic extractive were determined as well. The correlation among the appearance traits of PCC slice (including the thickness and the spatial values of colour of PCC slice powder: L*Lightness, a*Red-Green, b*Yellow-Blue) and peak areas of 12 characteristic peaks, contents of moisture and extractive were explored through multivariate statistical analysis tools, including Pearson's correlation analysis, principal component analysis (PCA), orthogonal partial least squares-discriminant analysis (PLS-DA) and analysis of variance (ANOVA). Association analysis results showed the morphological parameters (thickness and color) are significantly correlated with 2 kinds of principle chemical constituents (alkaloids and phenolic acids), among them, 5 major constituents including 2 isoquinoline alkaloids and 3 feruloylquinic acids were simultaneously quantitatively analyzed under the same chromatographic condition for establishing a correspondence between appearance traits and content of internal substances, and the sum of the contents of the five components was significantly higher in the thickness ≥ 4 mm (13.15% ± 2.25%) and bright yellow samples (12.14% ± 2.00%) than that in the thickness < 4 mm (10.89% ± 1.41%) and dark yellow samples (10.32% ± 2.41%). The research results confirm that thickness and colour, two main appearance parameters of PCC slice, can be used as the indicators for evaluating the quality PCC slice, which to some extent interprets the scientific connotation of traditional evaluation theory of "thick and yellow are better". At the same time, the results provided substantial data and foundation for the establishment of commodity grade standards of PCC slice.
Acanthopanax senticosus is one of the genuine regional herb in Northeast China. In this study, we identified the germplasm resources of commercial A. senticosus samples based on atpI and atpB_rbcL according to the previous chloroplast genome sequencing results, and determinated the content of syringin by HPLC to evaluated the quality of commercial samples. A total of 80 A. senticosus samples were collected from 47 cities in 24 provinces. DNA was extracted to amplify the products of atpI and atpB_rbcL by PCR. The results showed that 7 haplotypes (H2, H5, H8, H10, H12, H14, H23) were formed by the combined analysis of the two gene fragments. H2 from Yichun in Heilongjiang, Shangzhi in Harbin, Suihua in Heilongjiang, Fushun in Liaoning, Benxi in Liaoning, Changbai in Jilin and Jingyu in Jilin were the dominant genotype, representing 58.75% of the total samples. H14 and H23 were the unique haplotypes of the producing area. It is speculated that the commercial A. senticosus samples with haplotypes of H14 and H23 are from Raohe, Shuangyashan, Heilongjiang and Mingshui, Suihua, Heilongjiang, respectively. HPLC analysis indicated that the content of syringin in 73.96% of the samples met the Pharmacopoeia standards. There was a significant difference in the content of syringin among the samples, ranging from 0.003 7% to 0.524 5%, with a difference of 0.520 8%, indicating that the quality of the samples in the market of A. senticosus was uneven. However, there were no significant differences in the contents of syringin in the commercial A. senticosus among different haplotypes. The content of syringin in the haplotype H23 in the market sample is relatively high, so it may be a germplasm with better quality. This study researched the germplasm resources and medicinal materials quality of commercial A. senticosus samples and will help guide the commercial circulation, reasonable medication of A. senticosus, and the screening of excellent germplasm.