1. Mechanism of Shenqi Jiangtang Granules in treatment of diabetic microcirculation disorder based on multi-level interactive network pharmacology
Chinese Traditional and Herbal Drugs 2020;51(19):4861-4872
Objective: To explore the mechanism of Shenqi Jiangtang Granules (SJG) in the treatment of diabetic microcirculation disorder based on network pharmacology. Methods: The targets of diabetic kidney disease, diabetic retinopathy, diabetic peripheral neuropathy, diabetic foot disease and small cerebral vascular disease were searched through Genecards database to be integrated as the targets of diabetic microcirculation disorder disease. The targets of SJG' active components for treatment of diabetic microcirculation disorder were screened and predicted by utilizing PubChem Search and Swiss target prediction online tool. Cytoscape 3.3.0 software was adopted to construct an active component-diabetic microcirculation disorder target network. The protein-protein interaction (PPI) network was established by using STRING database. Gene ontology (GO) biological process and Kyoto Encyclopedia of Genes and Gnomes (KEGG) pathway enrichment analysis were performed using Clue GO. Results: A total of 85 active components of SJG and 10 targets (ACE, VEGFA, TNF, IL6, STAT3, ALB, PON1, PTPN22, PPARG and NOS3) related to diabetic microcirculation disorder were screened. Through GO and KEGG pathway enrichment analysis, it was found that the active components of SJG in the treatment of diabetic microcirculation disorder may participate in multiple signaling pathways, such as AGE-RAGE signaling pathway in diabetic complications, HIF-1 signaling pathway, insulin resistance, hypertrophic cardiomyopathy, inflammatory bowel disease, rheumatoid arthritis, etc. Conclusion: This study reflects the characteristics of multi-components, multi-targets and multi-pathways of SJG, which provides new ideas and clues for further research on the mechanism of SJG in the treatment of diabetic microcirculation disorder.
2. Chemical constituents of Picrasma quassioides
Chinese Traditional and Herbal Drugs 2020;51(19):4884-4890
Objective: To study the chemical constituents of Picrasma quassioidies. Methods: The isolation and purification were carried out by column chromatography on silica gel, ODS, Sephadex LH-20 and semi-preparative RP-HPLC. The structures were elucidated on the basis of physicochemical properties and spectroscopic analysis. Results: A total of 12 alkaloids and four quassinoids were isolated and identified from 80% ethanol aqueous extract of the stems of P. quassioides. They were named as 1-hydroxymethyl-4-methoxy-β-carboline (1), 1-methoxicabony-β-carboline (2), 1-methoxicabony-4-methoxy-β-carboline (3), 1-methoxicabony-4,8-dimethoxy-β-carboline (4), 1-ethyl-4-methoxy-β-carboline (5), 1-ethyl-4,8-dimethoxy-β-carboline (6), picrasidine I (7), canthin-6-one (8), 5-methoxyl-canthin-6-one (9), 4-methoxyl-5-hydroxyl-canthin-6-one (10), 4,5-dimethoxyl- canthin-6-one (11), quassidine B (12), quassin (13), nigakilactone B (14), nigakilactone E (15) and norquassin (16). Conclusion: Compound 1 is a new β-carboline alkaloid, named as kumujantine D, and compound 4 is isolated from P. quassioidies for the first time.
3. Two new α-pyronoids from endophytic fungus Aspergillus oryzae derived from Paris polyphylla var. yunnanensis
Chinese Traditional and Herbal Drugs 2020;51(19):4891-4895
Objective: To study the chemical composition and structure of the secondary metabolites of the endophytic fungus Aspergillus oryzae from Paris polyphylla var. yunnanensis. Methods: A. oryzae was fermented by liquid fermentation. After extraction, it was separated and purified by various chromatography methods. The structure of the compounds was identified according to the physical and chemical properties and spectral data. Results: Four compounds were isolated and their structures were identified as 4-hydroxy-6-[(2S,3S)-3-hydroxybutan-2-yl]-3-methyl-2H-pyran-2-one (1), (R)-4-hydroxy-6-(1-hydroxy-2- methylpropyl)-3- methyl-2H-pyran-2-one (2), flufuran (3) and flufuran methyl ester (4). Conclusion: Compounds 1 and 2 are new α-pyronoids named asper-α-pyranone A and asper-α-pyranone B.
4. A new steroid from leaves of Dysoxylum binectariferum
Chinese Traditional and Herbal Drugs 2020;51(19):4896-4901
Objective: To study the constituents of the leaves of Dysoxylum binectariferum. Methods: The chemical constituents were isolated by various column chromatographic methods, and their structures were identified on the basis of MS and NMR spectral analysis. Results: Five steroids were obtained and their structures were elucidated as stigmast-4(5)-en-3β,6β,22-triol (1), stigmast-5(6)-en-3β,21,22-triol (2), 2α,3β,4β-trihydroxypregnan-16-one (3), 2α,3β-dihydroxy-4β-acetoxypregnan-16-one (4) and 2α,3β-dihydroxypregnan-17(20)-en-16-one (5). Conclusion: Compound 1 is identified as a new compound and named dybinstigm A. Compounds 2-5 are obtained from D. binectariferum for the first time.
5. Chemical constituents of Schoenoplectus tabernaemontani
Chinese Traditional and Herbal Drugs 2020;51(19):4902-4906
Objective: To study the chemical constituents of the rhizomes of Schoenoplectus tabernaemontani. Methods: Compounds were isolated and purified by a combination of column chromatography including silica gel, polyamide and Sephadex LH-20. Their structures were elucidated by physiochemical properties and NMR analysis. Results: Twelve compounds were obtained from water extract of the rhizome of S. tabernaemontani and identified as 5,7,2',4'-tetrahydroxy-3, 5'-dimethoxyflavone (1), tricin (2), hesperetin (3), quercetin (4), luteolin (5), eriodictyol (6), apigenin (7), naringenin (8), chrysin (9), 5,7-dihydroxychromone (10), catechin (11) and tricin-7-O-β-D-glucoside (12), respectively. Conclusion: Compound 1 is a new flavone named schoenin. Compounds 2-5 and 7-12 are isolated from the Cyperaceae for the first time. Compound 6 is isolated from the genus Scirpus for the first time.
6. Chemical constituents of triterpenes from Centipeda minima and its anti-inflammatory activities
Chinese Traditional and Herbal Drugs 2020;51(19):4907-4915
Objective: To study triterpenes and their anti-inflammatory activity from the ethanol extract of Centipeda minima. Methods: The compounds were isolated and purified by silica gel, Sephadex LH-20, MCI, ODS and RP-HPLC gel column chromatography, and their structures were elucidated by NMR and MS spectroscopic techniques. The inhibitory activity of the compound on the release of inflammatory mediators NO from mouse macrophages (RAW264.7) induced by lipopolysaccharide (LPS) was determined by Griess method, and then the anti-inflammatory activity of the compounds was evaluated Results: A total of 17 compounds were isolated and identified as: 20-oxo-30-nortaraxastan-3β-yl acetate (1), 3β-acetoxytaraxaster-20-en-30-al (2), 3β-hydroxytaraxaster-20-en-30-al (3), taraxasterol (4), arnidiol (5), 3β,21β-dihydroxy-20(30)-en-taraxastane (6), faradiol (7), pseudotaraxasteryl acetate (8), taraxast-20-ene-3β,30-diol (9), 18α-olean-12-ene-3,11-dione (10), maniladiol (11), 3β- hydroxyolean-12-en-11-one (12), coflodiol (13), lupeol (14), 3β,16β-dihydroxylup-20(29)-ene (15), 16β-hydroxylupa-20(29)- en-3-one (16) and garcinielliptone Q (17). Compounds 2, 5-6, 8-10, 12-13, 15-17 displayed moderate inhibitory activity on theoverproduction of NO in LPS-activated RAW 264.7 mouse macrophage cell lines, IC50 values ranging from 11.9 to 27.1 μmol/L. Conclusion: Compound 1 is a new natural product, and its 1H-NMR and 13C-NMR data was first completely assigned on the basis of 1D and 2D NMR spectroscopic evidence. Compounds 2, 3, 6, 8-10, 12, 13, 15 and 16 are isolated from C. minima for the first time. This work provided theoretical basis for clinical application of C. minima
7. Structural characterization and anti-complement activity of polysaccharides from Glechomae Herba
Chinese Traditional and Herbal Drugs 2020;51(19):4916-4924
Objective: To isolate and purify the homogeneous polysaccharides from Glechomae Herba through the guidance of anti-complement activity, and study their structures. Methods: Crude polysaccharides from Glechomae Herba were extracted by water extraction and alcohol precipitation, then homogeneous polysaccharides were separated by DEAE-52 and Sephadex G-100 column chromatography. The structures of homogeneous polysaccharides were characterized by HPGPC, IR, GC, methylation and NMR, and their anti-complement activities were also determined. Results: Two homogeneous polysaccharides GLP-1 and GLP-2 were obtained with the molecular weight of 5 370 and 20 040. They were both heteropolysaccharides composed of arabinose and galactose with the ratio of 1:6.3 and 1:4.9, respectively. Conclusion: The structures of GLP-1 and GLP-2 further elucidate the pharmacodynamic basis of their anti-complement activities and provide basis for screening natural complement inhibitors.
8. Effect of particle design on pharmacokinetics of Shenling Baizhu Pulvis in rats
Chinese Traditional and Herbal Drugs 2020;51(19):4925-4933
Objective: Using LC-MS to explore the pharmacokinetic process in rats of Shenling Baizhu Pulvis (SBP), which was modified by particle design technology. Methods: Particle design powder of SBP was prepared by particle design technology. A scientific and feasible LC-MS analysis method was established to determine the blood concentration of index compounds such as ginsenoside Re (GI-Re), ginsenoside Rb1 (GI-Rb1), ginsenoside Rg1 (GI-Rg1), atractylenolide I (AT-I), atractylenolide II (AT-II) and pachymic acid (PA) in rats at different time points after administration. DAS 3.2.8 pharmacokinetic software was adopted to analyze the data, which related to blood concentration of index compounds, and the pharmacokinetics parameters were calculated by the non-compartmental model. Results: LC-MS analysis method was established, which has a good linear relationship and specificity for the index compounds in rats, and the RSD of precision, accuracy, extraction recovery and stability were all less than 5% or 10%. Compared with ordinary powder, the particle design powder displayed increased Cmax and AUC0-∞ after administration, and the AUC0-∞ of GI-Re, GI-Rb1, GI-Rg1, AT-I, AT-II and PA were increased to 1.52, 2.02, 1.22, 1.41, 1.13 and 1.43 times, respectively. Conclusion: The LC-MS analysis method meet the requirements of biological sample analysis in Pharmacopoeia of the People's Republic of China. After particle design and modification, the absorption speed of SBP in vivo become faster and the bioavailability is improved significantly.
9. Preparation of asiaticoside sodium alginate repair patch and its wound healing effect
Chinese Traditional and Herbal Drugs 2020;51(19):4934-4942
Objective: Asiaticoside-sodium alginate repair patch (As-SA RP) was prepared and its effect on skin wound healing was investigated. Methods: Based on the cross-linking characteristics of sodium alginate and Ca2+, As-SA RP was prepared using asiaticoside as a drug model through blending with sodium alginate. The compatibility of the blend films was investigated by scanning electron microscope and FTIR. The whole layer of skin on both sides of the back spine of New Zealand's big ear rabbit was used to establish the trauma model. The repair effect of the external application of As-SA RP on skin wounds was investigated by observing the healing status and determining the expression levels of collagen (hydroxyproline as an index) and pro-inflammatory (TNF-α, IL-1β and IL-6) factors in the injured skin tissue. Results: Asiaticoside had good compatibility with sodium alginate and can be successfully prepared As-SA RP. Compared with other groups, the red swelling, bleeding, infection, and exudate on injured skin were significantly reduced, and the wound healing rate was also relatively increased after As-SA RP treatment. Moreover, the less inflammatory cells infiltration, more new capillaries and intact wound skin structure relatively tight and orderly arrangement of collagen fibers were observed in the As-SA RP group. On the other hand, the biochemical analysis showed that As-SA RP could effectively inhibit the high expression of TNF-α, IL-1β, IL-6 in the injured skin tissue and significantly increase the contents of hydroxyproline and collagen fiber. Conclusion: As-SA RP could improve the skin absorption of asiaticoside and show the better effect of skin wound healing than the active component asiaticoside.
10. Mitochondrial targeting function of norcantharidin TPP-PEG-PCL nanomicelles promotes apoptosis of liver tumor cells
Chinese Traditional and Herbal Drugs 2020;51(19):4943-4953
Objective: To prepare norcantharidin TPP-PEG-PCL nanomicelles and study its release in vitro, intracellular transport and promoting effect on hepatoma cell apoptosis. Methods: Thin film hydration method was used to prepare norcantharidin TPP-PEG-PCL nanomicelles, and the particle size, electric potential and microscopic electron microscopy morphological analysis were measured. At the same time, the nanomicelles were evaluated for stability, in vitro release, pharmacokinetics and critical micelle concentration. Coumarin-6 was used as a fluorescent probe to evaluate the uptake of TPP-PEG-PCL nanomicelles in liver tumor cells, lysosomal escape and mitochondrial targeting function; Under the same dosage conditions, the effect of norcantharidin TPP-PEG-PCL nanomicelles on promoting apoptosis of liver tumor cells was evaluated. Results: The cantharidin TPP-PEG-PCL nanomicelles had a particle size of (16.8 ± 0.2) nm, a Zeta potential of (14.3 ± 0.2) mV, and transmission electron microscopy images showed that nanomicelles had a regular spherical shape. The fluorescence test results showed that TPP-PEG-PCL nanomicelles can promote the cellular uptake of drugs, escape lysosomal capture, and finally target aggregation at the mitochondrial site; Cell survival rate and Hoechst staining results showed that cantharidin TPP-PEG-PCL nanomicelles had a good effect on promoting apoptosis of liver tumor cells. Norcantharidin TPP-PEG-PCL nanomicelles can significantly reduce mitochondrial membrane potential, increase intracellular ROS levels, increase pro-apoptotic protein Bcl-2, and reduce resistance. The expression of apoptotic proteins Bax and these pro-apoptotic related experimental results are significantly better than those of norcantharidin PEG-PCL nanomicelles and norcantharidin, which have statistical significance. Conclusion: Norcantharidin TPP-PEG-PCL nanomicelles have good liver tumor cell mitochondrial targeting and promote tumor cell apoptosis, and it is a potentially effective drug delivery system for targeting tumor cell mitochondria.

Result Analysis
Print
Save
E-mail