Category: 6882-68-4

Li, Yanchu; Chen, Lu; Pu, Rong; Zhou, Lu; Zhou, Xufeng; Li, Xianyong published the artcile< Effects of a Matrine- and Sophoridine-Containing Herbal Compound Medicine (AH-05) on Liver Cancer>, Computed Properties of 6882-68-4, the main research area is liver cancer matrine sophoridine AH05.

Herbal medicine can present an alternative way of treating liver cancer. Here, we explored a matrine- and sophoridine-containing herbal compound medicine (AH-05) extracted from Adenophora capillaris, Sophora flavescens, Astragalus, and other plants. H22 and HepG2 cell models, as well as an H22 xenograft model, were established. Cell proliferation and apoptosis were measured in vitro, and tumor volume and weight were observed in vivo. The activation of AKT/mTOR and nuclear factor-κB (NF-κB) pathways in tumor cells and the polarization of CD4/CD8 T cells in the spleen were tested. To assess safety, hematol. toxicity and pathol. of the liver, kidney, spleen, and intestine were evaluated. AH-05 inhibited cell viability in a dose- and time-dependent manner. In vivo, tumor volume and weight were reduced, and the activation of NF-κB p50, NF-κB p65, AKT, p-AKT Ser473, and mTOR was suppressed. In addition, AH-05 promoted CD4+ T cell polarization in the spleen. With regard to safety, slight intestinal mucosa edema was observed, but no severe pathol. or hematol. toxicity was detected. AH-05 exhibited its therapeutic effects against liver cancer by regulating the AKT/mTOR and NF-κB signaling pathways, and the immune environment, by promoting CD4+ T cell polarization in the spleen. Thus, AH-05 represents a potential supplementary herbal compound medicine for liver cancer.

Natural Product Communications published new progress about Apoptosis. 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Computed Properties of 6882-68-4.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Ye, Xian-wen; Deng, Ya-ling; Zhang, Xia; Liu, Min-min; Liu, Ying; Xie, Ya-ting; Wan, Quan; Huang, Min; Zhang, Tao; Xi, Jia-he; Zhang, Jin-lian published the artcile< Study on the mechanism of treating COVID-19 with Shenqi Wan based on network pharmacology>, Application In Synthesis of 6882-68-4, the main research area is Shenqi Wan network pharmacol COVID treatment; Shenqi Wan; mechanism; molecular docking; network pharmacology; novel coronavirus pneumonia.

Through the method of network pharmacol., the active components and targets of Shenqi Wan (SQW) were excavated, the relationship with novel Coronavirus pneumonia (COVID-19) was discussed, and the possible mechanism of SQW in the treatment of COVID-19 was revealed from the aspects of multicomponents, multitargets, and multipathways. Firstly, the active components of SQW were screened from traditional Chinese medicine systems pharmacol. database and anal. platform and the 2020 edition of Chinese Pharmacopeia, and the related targets of the components were obtained. Then the disease targets related to COVID-19 were screened from GeneCards and Online Mendelian Inheritance in Man. Venny was used to map the relationship between component-target and disease-target, and String was used to analyze the interaction of common targets. The network was constructed and analyzed by Cytoscape, the function of Gene ontol. (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) genes was enriched by Metascape, and the mol. docking was verified by CB-Dock. Finally, 45 active components of SQW were obtained, and 72 potential targets were related to COVID-19, angiotensin-converting enzyme 2 (ACE2), interleukin (IL)-6, nitric oxide synthase (NOS3) and, C-reactive protein (CRP),may be the key targets. GO enrichment of 1715 projects, such as lipopolysaccharide stress response, active oxygen metabolism, pos. regulation of cell migration, and other GO enrichment. About 136 KEGG pathways, tumor necrosis factor signaling pathway, IL-17 signaling pathway, hypoxia-inducible factor 1-α signaling pathway were obtained. Mol. docking showed that kaempferol, quercetin, luteolin, astragaloside, calyx isoflavone glucoside, matrine, and other COVID-19-related targets such as ACE2, chymotrypsin-like protease (3CLpro), papain-like protease (PLpro), prostaglandin-endoperoxide synthase 2 (PTGS2) have good binding ability. According to the above results, it is suggested that SQW may play a role in the treatment of COVID-19 by directly or indirectly combining kaempferol, quercetin, and luteolin with ACE2, 3CLpro, PLpro, and PTGS2 to regulate multiple biol. functions and signaling pathways.

Drug Development and Industrial Pharmacy published new progress about Adipose tissue. 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Application In Synthesis of 6882-68-4.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Tang, Sheng; Wang, Can; Li, Ying-Hong; Niu, Tian-Yu; Zhang, Yuan-Hui; Pang, Yu-Dong; Wang, Yan-Xiang; Kong, Wei-Jia; Song, Dan-Qing published the artcile< Structure-activity relationship and hypoglycemic activity of tricyclic matrines with advantage of treating diabetic nephropathy>, Electric Literature of 6882-68-4, the main research area is diabetic nephropathy tricyclic matrinic hypoglycemic SAR pharmacodynamics glycolysis; Diabetic nephropathy; Hypoglycemic; Pharmacodynamics; Tricyclic matrinic; structure−activity relationship.

Forty-three tricyclic matrinic derivatives with a unique scaffold were prepared and evaluated for their stimulation effects on glucose consumption in HepG2 cells. The structure-activity relationship was systematically elucidated for the first time. Among them, compound 17a(I) exhibited the most promising potency, and dose-dependently increased glucose consumption in L6 myotubes. It significantly lowered blood glucose, glucosylated Hb and AGE level, and improved glucose tolerance and insulin resistance in KK-Ay mice as well. More importantly, 17a effectively ameliorated diabetic nephropathy (DN), as indicated by the improvement of renal function and pathol. changes, and decrease of urinary protein. Furthermore, 17a could induce glycolysis but suppressed aerobic oxidation of glucose, in a similar mechanism to Metform. Our results indicated that in addition to hyperglycemia, 17a may be developed to treat diabetic complication such as DN.

European Journal of Medicinal Chemistry published new progress about Advanced glycosylation end products Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Electric Literature of 6882-68-4.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Zhao, Zhongwei; Zhang, Dengke; Wu, Fazong; Tu, Jianfei; Song, Jingjing; Xu, Min; Ji, Jiansong published the artcile< Sophoridine suppresses lenvatinib-resistant hepatocellular carcinoma growth by inhibiting RAS/MEK/ERK axis via decreasing VEGFR2 expression>, Related Products of 6882-68-4, the main research area is hepatocellular carcinoma growth sophoridine lenvatinib RAS MEK ERK VEGFR2; VEGFR2; hepatocellular carcinoma; lenvatinib resistance; sophoridine.

This study aims to investigate the underlying mechanism of lenvatinib resistance and explore the potential drug to improve the treatment for lenvatinib-resistant (LR) HCC. Here, we developed two human LR HCC cell lines by culturing with long-term exposure to lenvatinib. Results showed that the vascular endothelial growth factor receptors (VEGFR)2 expression and its downstream RAS/MEK/ERK signalling were obviously up-regulated in LR HCC cells, whereas the expression of VEGFR1, VEGFR3, FGFR1-4 and PDGFRα/β showed no difference. Furthermore, ETS-1 was identified to be responsible for VEGFR2 mediated lenvatinib resistance. The cell models were further used to explore the potential strategies for restoration of sensitivity of lenvatinib. Sophoridine, an alkaloid extraction, inhibited the proliferation, colony formation, cell migration and increased apoptosis of LR HCC cells. In vivo and in vitro results showed Sophoridine could further sensitize the therapeutic of lenvatinib against LR HCC. Mechanism studies revealed that Sophoridine decreased ETS-1 expression to down-regulate VEGFR2 expression along with downstream RAS/MEK/ERK axis in LR HCC cells. Hence, our study revealed that up-regulated VEGFR2 expression could be a predicator of the resistance of lenvatinib treatment against HCC and provided a potential candidate to restore the sensitivity of lenvatinib for HCC treatment.

Journal of Cellular and Molecular Medicine published new progress about Angiogenesis. 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Related Products of 6882-68-4.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Zhang, Shilong; Liu, Yungen; Xing, Fangrong; Che, Chi-Ming published the artcile< Direct preparation of unprotected aminimides (R3N+-NH-) from natural aliphatic tertiary alkaloids (R3N) by [Mn(TDCPP)Cl]-catalysed N-amination reaction>, Synthetic Route of 6882-68-4, the main research area is unprotected aminimide preparation antitumor human; natural aliphatic tertiary alkaloid amination manganese complex catalyst; manganese complex preparation.

A panel of natural aliphatic tertiary alkaloids were directly converted to unprotected aminimides via [Mn(TDCPP)Cl]-catalyzed N-amination reaction using O-(2,4-dinitrophenyl)hydroxylamine as the nitrogen source in up to 98% yields under mild reaction conditions.

Chemical Communications (Cambridge, United Kingdom) published new progress about Alkaloids Role: PAC (Pharmacological Activity), PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Synthetic Route of 6882-68-4.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Li, Jian-Chun; Zhang, Zhi-Jun; Liu, Dan; Jiang, Ming-Yan; Li, Rong-Tao; Li, Hong-Mei published the artcile< Quinolizidine alkaloids from the roots of Sophora flavescens>, Electric Literature of 6882-68-4, the main research area is quinolizidine alkaloid isolation Sophora flavescens cancer inflammation; Sophora; Sophora flavescens Alt; anti-inflammation; cytotoxicity; quinolizidine alkaloids.

Seventeen quinolizidine alkaloids, including a new matrine-type one, sophcence A, were isolated from the roots of Sophora flavescens Alt. The structure of compound was elucidated by means of 1D and 2D NMR, as well as HR-ESI-MS spectroscopic data. The NMR data of (-)-Δ7-dehydrosophoramine () and oxy-N-methylcytisine () were reported for the first time. In addition, (+)-sophoranol () exhibited moderate inhibition on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 macrophages with IC50 value of 22.14 μM, while lupanine () was found to inhibit the growth of human glioma stem cells GSC-3# at 20 μg/mL.

Natural Product Research published new progress about Alkaloids Role: NPO (Natural Product Occurrence), PAC (Pharmacological Activity), PUR (Purification or Recovery), THU (Therapeutic Use), BIOL (Biological Study), OCCU (Occurrence), PREP (Preparation), USES (Uses). 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Electric Literature of 6882-68-4.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

ur Rashid, Haroon; Rasool, Shagufta; Ali, Yousaf; Khan, Kamin; Martines, Marco Antonio Utrera published the artcile< Anti-cancer potential of sophoridine and its derivatives: Recent progress and future perspectives>, Recommanded Product: (41S,7aR,13aR,13bR)-Dodecahydro-1H-dipyrido[2,1-f:3′,2′,1′-ij][1,6]naphthyridin-10(41H)-one, the main research area is review antitumor cancer sophoridine derivative; Alkaloid; Cancer; Phytochemical; Sophoridine; Topoisomerase I.

A review. Cancer is the second leading cause of mortality and has resulted in about 9.6 million deaths around the world in 2018. Cancer-caused deaths are expected to be 11.5 million by 2030 all over the world. Because of the fatal nature of cancer, substantial efforts are made all over the world to combat it. Phytoconstituents such as certain alkaloids, saponins, tannins, polyphenols, and terpenoids exhibit anticancer effects. Sophoridine is a tetracyclic quinolizidine alkaloid isolated from the stem and leaves of medicinal plants Sophora alopecuroides L., and Euchresta japonica Benth, and roots of Sophora alopecuroides Ait. Chinese Food and Drug Administration (CFDA) approved sophoridine as an antitumor agent in 2005. This review covers the antitumor activities of sophoridine and its derivatives The efficacy of sophoridine analogs is expressed with respect to their half-maximal inhibitory concentration (IC50 values). Structure-activity relationship (SAR) study for most of the sophoridine derivatives has been explained. Moreover, the current market of anticancer drugs and its expected growth are discussed. Prospects provide suggestions and clues for novel sophoridine-based anticancer agents with enhanced expected efficacy and min. toxicity.

Bioorganic Chemistry published new progress about Antitumor agents. 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Recommanded Product: (41S,7aR,13aR,13bR)-Dodecahydro-1H-dipyrido[2,1-f:3′,2′,1′-ij][1,6]naphthyridin-10(41H)-one.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Zhou, Wei; Wu, Jiarui; Zhang, Jingyuan; Liu, Xinkui; Guo, Siyu; Jia, ShanShan; Zhang, Xiaomeng; Zhu, Yingli; Wang, Miaomiao published the artcile< Integrated bioinformatics analysis to decipher molecular mechanism of compound Kushen injection for esophageal cancer by combining WGCNA with network pharmacology>, Reference of 6882-68-4, the main research area is esophageal cancer Kushen injection pharmacol bioinformatics.

Compound Kushen injection (CKI), a medicine in widespread clin. use in China, has proven therapeutic effects on cancer. However, few mol. mechanism analyses have been carried out. To address this problem, bioinformatics approaches combining weighted gene co-expression network anal. with network pharmacol. methods were undertaken to elucidate the underlying mol. mechanisms of CKI in the treatment of esophageal cancer (ESCA). First, the key gene modules related to the clin. traits of ESCA were analyzed by WCGNA. Based on the results, the hub genes related to CKI treatment for ESCA were explored through network pharmacol. Mol. docking simulation was performed to recognize the binding activity of hub genes with CKI compounds The results showed that the potential hub targets, including EGFR, ErbB2, CCND1 and IGF1R, are therapeutic targets of CKI for the treatment of ESCA. Moreover, these targets were significantly enriched in many pathways related to cancer and signalling pathways, such as the PI3K-Akt signalling pathway and ErbB signalling pathway. In conclusion, this research partially highlighted the mol. mechanism of CKI in the treatment of ESCA, offering great potential in the identification of the effective compounds in CKI and biomarkers for ESCA treatment.

Scientific Reports published new progress about Animal gene, c-erbB Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Reference of 6882-68-4.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Chen, Mengchun; Jiang, Qi; Zhang, Mingyao; Chen, Sailing; Lou, Junsheng; Chen, Yijie; Wang, Fang; Wang, Rongyue published the artcile< Establishment of quantitative methodology for sophoridine analysis and determination of its pharmacokinetics and bioavailability in rat>, Reference of 6882-68-4, the main research area is sophoridine detection blood circulation pharmacokinetics bioavailability rat; Sophoridine; UPLC–MS/MS; bioavailability; pharmacokinetics; rat plasma.

The aim of this study is to develop a rapid and sensitive UPLC-MS/MS approach to determine the sophoridine (SOP) level in rat plasma and the pharmacokinetics of the substance. Sophoridine is used as an anti-inflammatory, anti-virus, anti-microbial, and anti-tumor alkaloid. It is essential to explore specific detection methods for the quant. anal. of SOP in the blood circulation. The rat plasma samples were prepared by one-step protein precipitation with acetonitrile. Subsequently, the samples were separated by chromatog. using a UPLC BEH C18 reversed-phase with an initial mobile phase of methanol and 0.1% formic acid aqueous solution The gradient elution was performed at a fixed flow rate of 0.4 mL/min, and multiple reaction monitoring (MRM) mode with an electrospray pos. ionization source was employed to detect the transitions of m/z 249.1 → 84.2 for SOP and m/z 264.3 → 69.8 for dendrobine (IS). The entire process required 3.5 min for each sample. A linear correlation was established over the range of 2-2000 ng/mL (r2≥0.9954) for SOP in rat plasma with a lower limit of quantification (LLOQ) at 2 ng/mL. The range of accuracy was tested between 94.90% and 100.80%, and the relative standard deviations (RSDs) toward both intra- and inter-day precision were <10%. Thus, this method was successfully applied to a pharmacokinetic study, and the subsequent results demonstrated a low absolute bioavailability of 2.32%. The present study established a reliable method that quantified the SOP concentration in rat plasma after administering a dose of 2 mg/kg i.v. or 20 mg/kg orally. Drug Development and Industrial Pharmacy published new progress about Alkaloids Role: ANT (Analyte), BSU (Biological Study, Unclassified), THU (Therapeutic Use), ANST (Analytical Study), BIOL (Biological Study), USES (Uses). 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Reference of 6882-68-4.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Ren, Gang; Ding, Guotao; Zhang, Hongyan; Wang, Haipeng; Jin, Zengjun; Yang, Guoxing; Han, Yonghong; Zhang, Xia; Li, Guiying; Li, Weihao published the artcile< Antiviral activity of sophoridine against enterovirus 71 in vitro>, Reference of 6882-68-4, the main research area is sophoridine enterovirus antiviral activity; Antiviral activity; Cytopathic effect; Enterovirus 71; Sophoridine; Viral adsorption.

Enterovirus 71 (EV71) has a propensity to cause hand-foot-and-mouth disease (HFMD) epidemics associated with neurol. sequelae. Unfortunately, no drugs are currently available for the clin. treatment of EV71 infections. Sophoridine (SRI) is one of the most abundant alkaloids in Sophora flavescens Aiton (Leguminosae), which has been used to treat fever, throat inflammation, cancer, and other diseases. In this study, we found that SRI inhibits EV71 infection in Vero cells. To study the antiviral activity of SRI, Vero cells were divided into 3 treatment groups based on the timing of SRI dosing: prior to viral adsorption (Group A), during viral adsorption (Group B), and after viral adsorption (Group C). We further revealed the antiviral activity of SRI with the attachment assay and the penetration assay. For Group A, 50% viability of Vero cells was observed at a SRI concentration of 61.39μg/mL, whereas for Groups B, 50% viability was observed at SRI concentrations of 196.86μg/mL. Furthermore, 29.7% cell viability was observed even at a SRI concentration of 1000μg/mL in Groups C. The results show that SRI was highly effective against EV71 when Vero cells were pretreated with SRI for 2 h (Group A). Further researches indicate SRI was highly effective at inhibiting EV71 attachment when the SRI concentrations over 250μg/mL (P < 0.001). We have shown that Vero cell viability increases when SRI is administered prior to viral adsorption. This suggests that SRI has the considerable potential as an antiviral for EV71 disease prevention. Journal of Ethnopharmacology published new progress about Antiviral agents. 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Reference of 6882-68-4.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem