Category: 6882-68-4

Jia, Ya-qian; Yuan, Zi-wen; Zhang, Xiao-song; Dong, Jia-qi; Liu, Xue-nan; Peng, Xiao-ting; Yao, Wan-ling; Ji, Peng; Wei, Yan-ming; Hua, Yong-li published the artcile< Total alkaloids of Sophora alopecuroides L. ameliorated murine colitis by regulating bile acid metabolism and gut microbiota>, HPLC of Formula: 6882-68-4, the main research area is Sophora alkaloids ulcerative colitis bile acid metabolism; Bile acid metabolism; Gut microbiota; Total alkaloids of Sophora alopecuroides L.; Ulcerative colitis.

Sophora alopecuroides L. is one of the most commonly used plants in traditional medicine for the management conditions including inflammatory and gastrointestinal disease. However, the therapeutic mechanism of Sophora alopecuroides L.particularly in inflammatory bowel disease (IBD) remains unclear. To evaluate the treatment effects of total alkaloids of Sophora alopecuroides L. in ulcerative colitis (UC) mice model and explore the therapeutic mechanism of KDZ on UC based on bile acid metabolism and gut microbiota. Colitis were induced in BALB/c mice by administering 3.5% dextran sulfate sodium (DSS) in drinking water for 7 days. The mice were then given KDZ (300, 150 and 75 mg/kg) and the pos. drug sulfasalazine (SASP, 450 mg/kg) via oral administration for 7 days. The levels of 23 bile acids in the liver, bile, serum, cecum content and colon were determined through ultra-performance liquid chromatog./tandem mass spectrometry (UPLC-MS/MS). The cecum microbiota was characterized through high-throughput Illumina MiSeq sequencing. KDZ treatment significantly decreased the disease activity index (DAI) scores and ameliorated colonic injury in DSS-treated mice. The expression of IL-1β and TGF-β1 were suppressed, yet, IL-10 was up-regulated by KDZ and SASP treatment compared with those in the model group. Meanwhile, the serum contents of total bile acid and total cholesterol in the DSS group increased significantly compared with those in the control group, but reversed by SASP and KDZ. The relative abundance of Firmicutes increased after KDZ was administration, whereas the abundance of Bacteroidetes decreased. αMCA, βMCA, ωMCA and CA in the SASP and KDZ groups did not differ from those in the control group, whereas these parameters significantly increased in the DSS group. KDZ had a protective effect on DSS-induced colitis by mitigating colonic injury, preventing gut microbiota dysbiosis and regulating bile acid metabolism

Journal of Ethnopharmacology published new progress about Adlercreutzia. 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, HPLC of Formula: 6882-68-4.

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

Zhang, Wan-Ying; Chen, Ying; Zhang, Miao-Miao; Zhang, Guo-Wei published the artcile< Molecular mechanism prediction analysis of compound Kushen injection in the treatment of COVID-19 based on network pharmacology and molecular docking>, Application In Synthesis of 6882-68-4, the main research area is COVID 19 compound Kushen injection.

As 1 of the 8 effective traditional Chinese medicines for the treatment of atypical pneumonia, compound Kushen injection (CKI) played an important role in combating pneumonia caused by severe acute respiratory syndrome coronavirus 2 virus in China in 2003. CKI is known to inhibit inflammation, and its main chem. components, namely matrine and oxymatrine, can promote Th cells to recognize and eliminate viruses. In this study, network pharmacol. and mol. docking were used to explore the mechanisms of CKI for treating coronavirus disease 2019. The Traditional Chinese Medicine Systems Pharmacol. Database and Anal. Platform and other related literature were used to screen CKI’s active ingredients in the blood. Traditional Chinese Medicine Systems Pharmacol. Database and Anal. Platform, Swiss Target Prediction and STITCH were used to search for potential targets of the active ingredients. The ingredient-target network was constructed using the Cytoscape software. The STRING online database was used to construct a target protein-protein interaction network that can be visualized and analyzed using the Cytoscape software to obtain key targets. Sophocarpine, sophoridine, matrine, (+)-allomatrine, AIDS211310, and sophranol were the 6 active ingredients. After docking the active ingredients with severe acute respiratory syndrome coronavirus 2 3CL hydrolase and angiotensin-converting enzyme 2 (ACE2), they displayed suitable affinity, which could block viral replication and its binding to ACE2. The key targets mainly involved inflammatory factors, such as interleukin-6 (IL-6) and tumor necrosis factor (TNF). Gene Ontol. enrichment anal. mainly indicated the IL-6 cytokine-mediated signaling pathway and cytokine-mediated signaling pathway. The Kyoto Encyclopedia of Genes and Genome pathway enrichment anal. mainly indicated steroid hormone biosynthesis and the TNF signaling pathway. The alkaloids in CKI can block viral replication and its binding to severe acute respiratory syndrome coronavirus 2 and ACE2 receptors. They regulate the IL-6-mediated signaling pathway, TNF signaling pathway, and steroid hormone biosynthesis, thereby initiating therapeutic responses against COVID-19.

Traditional Medicine Research published new progress about COVID-19. 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

Jia, Xu; Zhang, Hanghang; Jiang, Xiangfu; Lu, Yaling; Liu, Wenjie; Yu, Jianna published the artcile< Profiling and quantitation of alkaloids in different parts of Sophora alopecuroides L. extracts by high-performance liquid chromatography with electrospray ionisation ion mobility spectrometry detection>, Application of C15H24N2O, the main research area is Sophora alopecuroides extract alkaloid HPLC electrospray ionization MS; HPLC-IMS; alkaloids; ion mobility spectrometry.

Ambient pressure electrospray ionisation ion mobility spectrometry coupled to high-performance liquid chromatog. (HPLC) was used to detect alkaloids from different parts of Sophora alopecuroides L. extracts Multiplexing ion mobility spectrometry (IMS) was used to improve the signal-to-noise ratio while maintaining high resolving power for the detecting of eluents from HPLC separation The alkaloids profile and distribution are demonstrated by retention time-drift time two-dimensional spaces, and the contents of five major alkaloids including sophoridine, sophocarpine, cytisine, aloperine, and matrine were determined in the leaf, skin, stem, seed kernel, and seed husk using the HPLC-IMS method. This method offers extra separation ability to isomers such as matrine and sophocarpine, which can be difficult to distinguish by mass spectrometry. The reduced mobilities for cytisine, sophoridine, sophocarpine, matrine, and aloperine are 0.828, 0.718, 0.731, 0.725, and 0.769 cm2/V/s, resp. The limits of detection are 0.553, 0.488, 0.479, 0.484, and 0.513 ug/mL. This method adds extra separation ability to HPLC to resolve co-eluted peaks and provides another qual. parameter besides HPLC retention time.

Phytochemical Analysis published new progress about Alkaloids Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Application of C15H24N2O.

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

Hu, Chunhui; Gan, Xuehui; Jia, Qiangqiang; Gao, Pan; Du, Tao; Zhang, Fabin published the artcile< Optimization of supercritical-CO2 extraction and pharmacokinetics in SD rats of alkaloids form Sophora moorcroftiana seed>, Category: naphthyridine, the main research area is Sophora alkaloid carbon dioxide extraction pharmacokinetics optimization.

The total alkaloids extracted from the seeds of Sophora moorcroftiana (TAs-SM) have the potential to treat alveolar echinococcosis, a disease included by the WHO in a list of 17 key neglected diseases world-wide. The aims of the current study were first to develop a supercritical fluid extraction (SFE) method for optimizing TAs-SM extraction, and second, to develop an optimized method for evaluating TAs-SM pharmacokinetics in vivo. The Box-Behnken response surface method was used to optimize the extraction process, and ultra-high liquid chromatog. coupled with high resolution electrospray mass spectrometry (UPLC-HR-ESI-MS) was used to determine the pharmacokinetics of TAs-SM in SD rats. The results indicated the following optimal SFE extraction conditions: pressure = 31 MPa, temperature = 70 °C, time = 162.18 min. With these parameters, total alkaloids could be extracted from each gram of S. moorcroftiana, with the total content being 68.88 μg. The linear range of UPLC-HR-ESI-MS is 0.78-200.00 ng/mL, R2 > 0.99, and the sample recovery is 99-113%. The precision, accuracy, selectivity and stability of the method meet the requirements of US FDA guidelines. To our knowledge this study is the first to establish an SFE method for extracting TAs-SM and the first to employ UPLC-HR-ESI-MS for measuring TAs-SM in rats. These findings provide important contributions for using TAs-SM in further drug development and clin. applications.

Scientific Reports published new progress about Alkalinization. 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Category: naphthyridine.

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

Li, Wenxuan; Deng, Lijuan; Lei, Yuhe; Liu, Junshan published the artcile< Network-pharmacology and molecular docking-based investigation of mechanism of Sophora flavescens on cancer and inflammation>, Category: naphthyridine, the main research area is Sophora network pharmacol mol docking.

Objective: In order to explore the systematical regulatory mechanism of Kushen (Sophora flavescens, SF) on inflammation and cancer, we analyzed inter-mol. interactions between herbal ingredients of SF and human inflammation and cancer through network-pharmacol. and mol. docking-based approaches. Methods: Firstly, ingredients and potential targets were obtained from Traditional Chinese Medicine Systems Pharmacol. Database and Anal. Platform, GeneCards database, Therapeutic Targets Database and Online Mendelian Inheritance in Man database. Then, protein-protein interaction network and medicine-ingredient-target-disease network were established and analyzed via STRING and Cytoscape. Surflex-dock was performed by SybylX-2.0. Finally, functional enrichment and pathway enrichment were achieved by Gene Ontol. database and Kyoto Encyclopedia of Genes and Genomes database. Results: The results showed that 113 components of SF and 53 potential targets were related in the study. Conclusions: The study predicted the mechanism of SF on cancer and inflammation. According to the results, we suggest that the ingredients of SF effect on DNA bingding and transcription in nuclear receptors-like JUN, MYC, RELA, NCOA, PPARG. the receptors trigger several pathways including NF-κB pathway, the Bcl-2/Bax pathway and others. Eventually, it regulats inflammatory factors and cell proliferation, senescence and apoptosis.

TMR Modern Herbal Medicine published new progress about Aging, animal. 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Category: naphthyridine.

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

Hou, Zhifei; Sun, Guoxiang; Guo, Yong; Yang, Fangliang; Gong, Dandan published the artcile< Capillary electrophoresis fingerprints combined with Linear Quantitative Profiling Method to monitor the quality consistency and predict the antioxidant activity of Alkaloids of Sophora flavescens>, Safety of (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 Sophora antioxidant alkaloid determination capillary electrophoresis; Alkaloids of Sophora flavescens; Capillary electrophoresis fingerprints; Fingerprint-efficacy relationship; Quality consistency; The total antioxidant capacity.

Alkaloids of Sophora flavescens (ASF) has various pharmacol. effects, and it is widely used in clin. practice. The aim of this research was to develop an environmentally friendly methodol. that enables not only identification but also the quality consistency assessment of Alkaloids of Sophora flavescens. A background electrolyte composed of 50 mmol/L sodium tetraborate solution, 500 mmol/L boric acid and 1.2 mmol/L citric acid was used to conduct the fingerprint anal. coupled with quant. determination of three components. Linear quant. profiling method was used for comprehensive quality discrimination of the test samples from both qual. and quant. perspectives, and the 27 batches of samples were well differentiated. In addition, the fingerprint-efficacy relationship between chem. components and antioxidant activity in vitro was established using partial least squares regression model, which provided important medicinal efficacy information for quality control.

Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences published new progress about Alkaloids Role: ANT (Analyte), THU (Therapeutic Use), ANST (Analytical Study), BIOL (Biological Study), USES (Uses). 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Safety of (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

Zhuang, Haiwen; Dai, Xudong; Zhang, Xiaoyu; Mao, Zhongqi; Huang, Haijin published the artcile< Sophoridine suppresses macrophage-mediated immunosuppression through TLR4/IRF3 pathway and subsequently upregulates CD8+ T cytotoxic function against gastric cancer>, Synthetic Route of 6882-68-4, the main research area is gastric cancer sophoridine immunosuppression TLR4 IRF3 CD8; CD8(+) T cells; Gastric cancer; Sophoridine; TLR4/IRF3 pathway; Tumor-associated macrophages.

Gastric cancer is one of the most common and deadly neoplasms with limited effective treatments. The emergence of the immunotherapy has brought great expectations for cancer patients. Sophoridine is extracted from the seeds of sophora alopecuroides and has various pharmacol. actions including anti-tumor, anti-inflammatory, anti- arrhythmia and anti-virus. However, the effect of Sophoridine on gastric cancer microenvironment immunity and its underling mechanism remains poorly known. This study was aimed to investigate the effect of Sophoridine on the polarization status of gastric tumor-associated macrophages (TAMs) and its underlying mechanism. We isolated primary bone marrow-derived macrophages (BMDMs) and primary CD8+ T cells to perform coculture assay. Sophoridine educated TAMs polarize to M1-TAMs and suppressed M2-TAMs polarization through TLR4/IRF3 axis. Sophoridine-treated TAMs exhibited stronger pro-inflammatory function through upregulation the expression of INOS, IFN-β and IL-12α, and downregulation the expression of Arg-1, CD206 and IL-10. Sophoridine -primed TAMs increased the proliferation and cytotoxic function of CD8+ T by upregulating the expression of Granzyme-B, TNF-α and Perforin, and downregulated the expression of CD8+ T cells function exhaustion markers PD-1, Tim-3 and Lag-3. Furthermore, Sophoridine inhibited the migration ability of macrophage by decrease the CCR2 expression. Thus, Sophoridine acted on macrophages and CD8+ T cells to reshape gastric cancer immune microenvironment. Our studies provided preclin. basis for clin. application of Sophoridine.

Biomedicine & Pharmacotherapy published new progress about CC chemokine receptor CCR2 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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

Shang, Hai; Li, Lingyu; Ma, Liyan; Tian, Yu; Jia, Hongmei; Zhang, Tao; Yu, Meng; Zou, Zhongmei published the artcile< Design and synthesis of molecular hybrids of sophora alkaloids and cinnamic acids as potential antitumor agents>, Category: naphthyridine, the main research area is sophora alkaloid cinnamic acid hybrid preparation SAR antitumor apoptosis; antitumor; apoptosis; cinnamic acid; hybrid; sophora alkaloid.

Twenty-five sophora alkaloids-cinnamic acid hybrids, including matrine-cinnamic acid hybrids I (R1 = H, Cl; R2 = H, OMe, Cl, Br; R3 = H, CF3, NO2, etc.; R4 = H, OMe; -R2R3- = -OCH2O-), sophoridine-cinnamic acid hybrids II (R1 = H, Cl; R2 = H, Cl, Br; R3 = H, OMe, NO2, etc.; R4 = H; -R2R3- = -OCH2O-), and sophocarpine-cinnamic acid hybrids III (R1 = H, Cl; R2 = R4 = H; R3 = H, OMe), were designed, synthesized, and evaluated in vitro against three human tumor cell lines (HeLa, HepG2 and A549) with cisplatin as a pos. control. Some matrine-cinnamic acid and sophoridine-cinnamic acid compounds exhibited potent effect against all three cancer cell lines, such as compounds I (R1 = Cl; R2 = R3 = R4 = H), I (R1= R4 = H; R2 = R3 = Cl), I (R1 = R2 =R4= H; R3 = CF3) and I (R1 = R2 = R4 = H; R3 = Cl). The structure-activity relationship study of the synthesized compounds was also performed. Preliminary mechanistic studies indicated that compounds I (R1= R4 = H; R2 = R3 = Cl) and I (R1 = R2 = R4 = H; R3 = Cl) could induce apoptosis in HepG2 cell line. Further, compounds I (R1= R4 = H; R2 = R3 = Cl) and I (R1 = R2 = R4 = H; R3 = Cl) altered mitochondrial membrane potential and produced ROS leading to cell apoptosis of HepG2 cells. Overall, findings suggested that these compounds may provide promising lead compounds for further development as antitumor agents by structural modification.

Molecules published new progress about Alkaloids Role: PAC (Pharmacological Activity), 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, Category: naphthyridine.

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

Zhao, Wu-li; Xing, Yan; Ye, Cheng; Qiu, Yu-han; Li, Yi; Liu, Xiu-jun; Wang, Meng-yan; Bi, Chong-wen; Song, Dan-qing; Shao, Rong-guang published the artcile< The novel sophoridine derivate IMB-HDC induced lessened phosphorylation of STAT5a at 694 and 780 and promoted DNA breakage and cell apoptosis via blocking STAT5a nuclear translocation>, 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 cancer cell apoptosis sophoridine derivate STAT5a DNA breakage; DNA breakage; STAT5a; anticancer; nuclear location; shuttle.

Sophoridine is a quinolizidine natural product and the exploration of its derivatives has been carried out, and the potent anticancer compound IMB-HDC was acquired. Although previous studies have revealed that some sophoridine derivatives could induce DNA breakage, the underlying mechanisms of inhibition of DNA damage repair (ATR inactivation) and the apoptosis independent of p53, have not been elucidated. Our research reveals a novel DNA response mechanism different from general DNA-damaging agents, and that sophoridine derivate inhibits the phosphorylation of Tyr694 and Ser780 of STAT5a to induce the lessened shuttle from the cytoplasm to the nucleus, and leads to the decreased nuclear STAT5a and subsequently inhibits the expression of STAT5a target gene RAD51 that contributes to the checkpoint activation, thus inhibiting ATR activation. Meanwhile, IMB-HDC that induced the diminished expression of STAT5a target gene contributes to proliferation and leads to apoptosis. More importantly, we give the first evidence that promoting the effect of Tyr694 phosphorylation on nuclear location and subsequent STAT5a target gene transcription depends on Ser780 increased or unchanged phosphorylation and was not correlated with Ser726 phosphorylation.

Acta Pharmacologica Sinica published new progress about Animal gene, Bcl-2 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 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

Vinoth, M.; Natarajan, B.; Sundaram, C. Shanmuga published the artcile< Characterization and evaluation ethyl acetate extract of melochia corchorifolia leaf-anticancer antibiological and molecular docking studies on breast cancer estrogen receptor>, 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 Melochia leaf extract anticancer antibiol breast cancer estrogen receptor.

The present work focused on Phytochem. screening, characterization, anticancer activity and antibiol. activity of Et acetate extract of Melochia corchorifolia leaves followed by mol. docking studies have been carried out. The plant leaves have been collected, weighed, and extracted with the soxhlet apparatus by using Et acetate solvent and then extracted are subjected to phytochem. screening. Antibiol. activity of plant leaves Et acetate extract has been tested against six bacterial and two fungal strains using agar well diffusion methodol. The characterization of phytoconstituents compounds has been carried out using various spectroscopy method such as GC-MS (Gas chromatog. Mass spectroscopy), UV-visible and Fourier-transform IR. Auto dock tool (4.2.0) is used for mol. docking studies. The phytochem. anal. of Melochia corchorifolia Et acetate leaves, reveals the existence of carbohydrates, glycosides, triterpenes flavonoids and alkaloids. Antimicrobial activity is effective against gram-pos. bacterial strains namely Staphylococcus aureus (17 mm), Bacillus subtilis (16 mm), the gram-neg. bacterial strains namely Salmonella typhi (15 mm) and E. coli (14 mm). Moreover, the extract is also found to be effective against Aspergillus Niger (18 mm) fungal species. The GC-MS and FT-IR anal. show bioactive compounds and their functional groups. UV-VIS anal. results reveal that the presence of phytoconstituents derivatives in the range between 206-350 nm. The cytotoxicity activity for the MCF-7 cell line shows that the drug efficacy IC50 value is 148.836 (μg/mL). Further, the predicted bioactive compounds are docked with the cancer estrogen protein receptor (PDB ID: 3s7s) with ligand martidin-15 one shows the highest binding affinity. The study reveals the potential of Melochia corchorifolia leaves Et acetate extract showed antibiol. and anticancer activity.

Indian Journal of Chemical Technology published new progress about Affinity (Binding). 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