Category: 6882-68-4

Wei, Guangfei; Chen, Yongzhong; Guo, Xiaotong; Wei, Jianhe; Dong, Linlin; Chen, Shilin published the artcile< Biosyntheses characterization of alkaloids and flavonoids in Sophora flavescens by combining metabolome and transcriptome>, Application of C15H24N2O, the main research area is Sophora flavescens alkaloid flavonoid metabolome transcriptome biosynthesis.

Sophora flavescens are widely used for their pharmacol. effects. As its main pharmacol. components, alkaloids and flavonoids are distributed in the root tissues wherein mol. mechanisms remain elusive. In this study, metabolite profiles are analyzed using metabolomes to obtain biomarkers detected in different root tissues. These biomarkers include alkaloids, phenylpropanoids, and flavonoids. The high-performance liquid chromatog. anal. results indicate the differences in principal component contents. Oxymatrine, sophoridine, and matrine contents are the highest in the phloem, whereas trifolirhizin, maackiain, and kushenol I contents are the highest in the xylem. The transcript expression profiles also show tissue specificity in the roots. A total of 52 and 39 transcripts involved in alkaloid and flavonoid syntheses are found, resp. Among them, the expression levels of LYSA1, LYSA2, AO2, AO6, PMT1, PMT17, PMT34, and PMT35 transcripts are highly and pos. correlated with alkaloids contents. The expression levels of 4CL1, 4CL3, 4CL12, CHI5, CHI7, and CHI9 transcripts are markedly and pos. correlated with flavonoids contents. Moreover, the quant. profiles of alkaloids and flavonoids are provided, and the pivotal genes regulating their distribution in S. flavescens are determined These results contribute to the existing data for the genetic improvement and target breeding of S. flavescens.

Scientific Reports 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

Lei, Lijing; Zhao, Yu; Shi, Kai; Liu, Ying; Hu, Yunxia; Shao, Hua published the artcile< Phytotoxic activity of alkaloids in desert plant Sophora alopecuroides>, 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 phytotoxic activity oxymatrine Sophora desert plant; Sophora alopecuroides L.; abscisic acid (ABA); alkaloids; allelopathy; antioxidant defense system; cytokinin (CTK); indole-3-acetic acid (IAA); malondialdehyde (MDA).

Sophora alopecuroides is known to produce relatively large amounts of alkaloids; however, their ecol. consequences remain unclear. In this study, we evaluated the allelopathic potential of the main alkaloids, including aloperine, matrine, oxymatrine, oxysophocarpine, sophocarpine, sophoridine, as well as their mixture both in distilled H2O and in the soil matrix. Our results revealed that all the alkaloids possessed inhibitory activity on four receiver species, i.e., Amaranthus retroflexus, Medicago sativa, Lolium perenne and Setaria viridis. The strength of the phytotoxicity of the alkaloids was in the following order: sophocarpine > aloperine > mixture > sophoridine > matrine > oxysophocarpine > oxymatrine (in Petri dish assays), and matrine > mixture > sophocarpine > oxymatrine > oxysophocarpine > sophoridine > aloperine (in pot experiments). In addition, the mixture of the alkaloids was found to significantly increase the IAA content, MDA content and POD activity of M. sativa seedlings, whereas CTK content, ABA content, SOD activity and CAT activity of M. sativa seedlings decreased markedly. Our results suggest S. alopecuroides might produce allelopathic alkaloids to improve its competitiveness and thus facilitate the establishment of its dominance; the potential value of these alkaloids as environmentally friendly herbicides is also discussed.

Toxins published new progress about Alfalfa. 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

Li, Jian-Chun; Dai, Wei-Feng; Liu, Dan; Zhang, Zhi-Jun; Jiang, Ming-Yan; Rao, Kai-Rui; Li, Rong-Tao; Li, Hong-Mei published the artcile< Quinolizidine alkaloids from Sophora alopecuroides with anti-inflammatory and anti-tumor properties>, 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 Sophora Quinolizidine alkaloid anti inflammatory antitumor; Anti-inflammatory; Anti-tumor; Leguminosae; Quinolizidine alkaloids; Sophora alopecuroides.

Forty-three quinolizidine alkaloids (1-43), including twelve new matrine-type ones, sophalodes A-L (1-7, 17, 19 and 28-30), were isolated from the seeds of Sophora alopecuroides. Structurally, compounds 1-4 were the first examples of C-11 oxidized matrine-type alkaloids from Sophora plants. The structures and absolute configurations of new compounds were elucidated by extensive spectroscopic techniques, X-ray diffraction anal., and quantum chem. calculation In addition, the NMR data and absolute configuration of compound 18 was reported for the first time. All the isolates were evaluated for their inhibition on nitric oxide production induced by lipopolysaccharide in RAW 264.7 macrophages, among them, compounds 29, 38 and 42 exhibited the most significant activity with IC50 values of 29.19, 25.86 and 33.30μM, resp. Further research about new compound 29 showed that it also suppressed the protein levels of iNOS and COX-2, which revealed its anti-inflammatory potential. Moreover, addnl. research showed that compound 16 exhibited marginal cytotoxicity against HeLa cell lines, with an IC50 value of 24.27μM.

Bioorganic Chemistry published new progress about Anti-HIV 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

Gao, Yuan; Hai, Lina; Kang, Yuan; Qin, Wenjie; Liu, Fang; Cai, Runlan; Yang, Xiuwei; Qi, Yun published the artcile< Compound kushen injection induces immediate hypersensitivity reaction through promoting the production of platelet-activating factor via de novo pathway>, Computed Properties of 6882-68-4, the main research area is Sophora Smilacis root extract platelet activating factor hypersensitivity; compound kushen injection; de novo pathway of platelet-activating factor; matrine; non-immunologic immediate hypersensitivity reaction; platelet-activating factor.

Compound Kushen Injection (CKI) is a bis-herbal formulation extracted from Kushen (Radix Sophorae Flavescentis) and Baituling (Rhizoma Heterosmilacis Yunnanensis). Clin., it is used as the adjuvant treatment of cancer. However, with the increased application, the cases of immediate hypersensitivity reactions (IHRs) also gradually rise. In this study, we investigated the underlying mechanism(s) and active constituent(s) for CKI-induced IHRs in exptl. models. The obtained results showed that CKI did not elevate serum total IgE (tIgE) and mouse mast cell protease 1 (MMCP1) after consecutive immunization for 5 wk, but could induce Evans blue extravasation (local) and cause obvious hypothermia (systemic) after a single injection. Further study showed that alkaloids in Kushen, especially matrine, were responsible for CKI-induced IHRs. Mechanism study showed that various platelet-activating factor (PAF) receptor antagonists could significantly counter CKI-induced IHRs locally or systemically. In cell system, CKI was able to promote PAF production in a non-cell-selective manner. In cell lysate, the effect of CKI on PAF production became stronger and could be abolished by blocking de novo pathway. In conclusion, our study identifies, for the first time, that CKI is a PAF inducer. It causes non-immunol. IHRs, rather than IgE-dependent IHRs, by promoting PAF production through de novo pathway. Alkaloids in Kushen, especially matrine, are the prime culprits for IHRs. Our findings may provide a potential approach for preventing and treating CKI-induced IHRs.

Frontiers in Pharmacology 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, Computed Properties of 6882-68-4.

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

Dai, Lin-Lin; Li, Dong-Dong; Zhao, Xiu-Mei; Zhi, Shuang; Shen, Hong-Sheng; Yang, Zi-Bo published the artcile< Synthesis and Antitumor Effect of Sophoridine Derivatives Bearing an Acyclic Aryloxy Phosphoramidate Mustard Functionality>, HPLC of Formula: 6882-68-4, the main research area is sophoridine aryloxy phosphoramidate mustard synthesis antitumor.

To elevate the potency of sophoridine, phosphoramidate mustard motif was incorporated to D-ring opened sophoridine scaffold. A series of acyclic aryloxy phosphoramidate mustard functionalized sophoridine derivatives were synthesized and screened for cytostatic activity in a range of different tumor cell lines (S180, H22, K562, MCF-7, SMMC-7721, and LoVo). All these compounds were shown to be more sensitive to S180 and H22 cells with IC50 values ranging from 2.10 to 7.21 μM. In addition, all targeted derivatives distinctly are more cytotoxic to cancer cells than normal cell L929. Compounds I (R = 3-ClC6H4, 4-BrC6H4, 1-naphthyl, 2-naphthyl) displayed moderate tumor suppression without apparent organ toxicity in vivo against mice bearing H22 liver tumors. Their potential binding modes with DNA topoisomerase I complex have also been investigated.

Journal of Heterocyclic Chemistry published new progress about Antitumor agents. 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

Lin, Bei-Bei; Liu, Xiang; Wu, San-Qiao; Zheng, Hong-Xing; Huo, Ke-Ke; Qi, Shan-Shan; Chen, Chen published the artcile< Phytochemicals content, antioxidant and antibacterial activities of Sophora viciifolia>, Name: (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 phytochem antioxidant antibacterial Sophora extract; Sophora viciifolia; UPLC; antimicrobial activity; antioxidants; extract; phytochemistry.

The objective of this study is to compare the efficacy of ethanol extracts from different parts of Sophora viciifolia. The content of polyphenols, flavonoids, alkaloids, and antioxidant capacity, antimicrobial activity were investigated, and individual polyphenols and alkaloids were analyzed and quantified by ultra-high performance liquid chromatog. (UPLC). The microdilution method was used to determine the antimicrobial activity of extracts from S. viciifolia on six strains. The results for extracts from the different parts (flowers, leaves, and fruit) were compared in varying concentrations to determine whether one extract source is superior to another. Testing verified that extracts from the different parts of S. viciifolia did vary, as expected. For example, extract from the leaves had the best antimicrobial activity against pathogenic Candida albicans, but all extracts had good antimicrobial activity against the six tested strains. These results reveal that the active substances in S. viciifolia are abundant and have good antioxidant and antimicrobial activities, which can provide theor. support for the subsequent development and utilization of S. viciifolia extracts

Chemistry & Biodiversity 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, Name: (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

Wang, Rui; Liu, Hongwei; Shao, Yingying; Wang, Kailong; Yin, Shuangshuang; Qiu, Yuling; Wu, Honghua; Liu, Erwei; Wang, Tao; Gao, Xiumei; Yu, Haiyang published the artcile< Sophoridine inhibits human colorectal cancer progression via targeting MAPKAPK2>, Reference of 6882-68-4, the main research area is sophoridine MAPKAPK colorectal cancer progression human.

Radian Sophorae flavescentis is a traditional Chinese medicine commonly used to treat cancer in China. However, its active components and underlying mechanism remain ambiguous. In this study, we have screened the pharmacokinetic parameters of the main chem. constituents of Radian Sophorae flavescentis by Traditional Chinese Medicine Systems Pharmacol. (TCMSP) Database and Anal. Platform and have found that Sophoridine is one of the best antitumor active ingredients. We have found that MAPKAPK2 is a potential target for Sophoridine by the PharmMapper and KEGG databXase anal. Moreover, we have found that Sophoridine selectively inactivates phospho-MAPKAPK2 (Thr222) and directly binds into the ATP site of MAPKAPK2 by mol. docking. Furthermore, we have found out a direct binding between MAPKAPK2 and Sophoridine by cellular thermal shift assay and drug affinity responsive targets stability assay. The inhibition effects are further confirmed by Western blot: Sophoridine significantly decreases phospho-MAPKAPK2 (Thr222) in a time-dependent manner, but there is no obvious change in its total expression in colorectal cancer cells. Clin. studies have shown that a higher level of MAPKAPK2 is associated with a poorer percent survival rate (prognosis). Furthermore, a higher level of MAPKAPK2 is pos. associated with the enrichment of downregulation of apoptosis and autophagy by gene set enrichment anal., as well as upregulation of proliferation and cell-cycle arrest. Taken together, our results suggest that the MAPKAPK2 plays a key role in Sophoridine-inhibited growth and invasion in colorectal cancers.

Molecular Cancer Research published new progress about Animal gene 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

Aung, T. N.; Nourmohammadi, S.; Qu, Z.; Harata-Lee, Y.; Cui, J.; Shen, H. Y.; Yool, A. J.; Pukala, T.; Du, Hong; Kortschak, R. D.; Wei, W.; Adelson, D. L. published the artcile< Fractional Deletion of Compound Kushen Injection Indicates Cytokine Signaling Pathways are Critical for its Perturbation of the Cell Cycle>, Product Details of C15H24N2O, the main research area is breast cancer cell cytokine signaling anticancer Kushen injection.

We used computational and exptl. biol. approaches to identify candidate mechanisms of action of aTraditional Chinese Medicine, Compound Kushen Injection (CKI), in a breast cancer cell line (MDA-MB-231). Because CKI is a complex mixture of plant secondary metabolites, we used a high-performance liquid chromatog. (HPLC) fractionation and reconstitution approach to define chem. fractions required for CKI to induce apoptosis. The initial fractionation separated major from minor compounds, and it showed that major compounds accounted for little of the activity of CKI. Furthermore, removal of no single major compound altered the effect of CKI on cell viability and apoptosis. However, simultaneous removal of two major compounds identified oxymatrine and oxysophocarpine as critical with respect to CKI activity. Transcriptome anal. was used to correlate compound removal with gene expression and phenotype data. Many compounds in CKI are required to trigger apoptosis but significant modulation of its activity is conferred by a small number of compounds In conclusion, CKI may be typical of many plant based extracts that contain many compounds in that no single compound is responsible for all of the bioactivity of the mixture and that many compounds interact in a complex fashion to influence a network containing many targets.

Scientific Reports published new progress about Adenocarcinoma. 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Product Details of C15H24N2O.

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

Shalaby, Khaled; Mostafa, Ehab M.; Musa, Arafa; Moustafa, Abd El Ghany A.; Ibrahim, Mohamed F.; Alruwaili, Nabil K.; Zafar, Ameeduzzafar; Elmowafy, Mohammed published the artcile< Enhanced full-thickness wound healing via Sophora gibbosa extract delivery based on a chitosan/gelatin dressing incorporating microemulsion>, SDS of cas: 6882-68-4, the main research area is Sophora gibbosa extract chitosan gelatin wound healing dressing microemulsion; Sophora gibbosa; chitosan/gelatin; dressing; microemulsion; wound healing.

There are many synthetic drugs in literature have been utilized in healing of the wounds although the natural product specially antioxidants can offer similar if not better biol. activity in that regard. Genus Sophora is well known to contain flavonoids and phenolic compounds which have antioxidant and inflammatory effects. So, the aim of the current study was to develop and evaluate chitosan/gelatin based Sophora gibbosa extract-loaded microemulsion as wound dressing. Sophora gibbosa extract (SGE) contained 16 major compounds which have reasonable antioxidant activity. The developed microemulsion showed that Tween 80 produced significant (p < 0.05) lower particle size than Pluronic F127 at the same SGE concentration whereas high concentration of extract results in large particle size. Thermodn. stability studies showed that using higher concentration of the extract produced less stable formulations. The selected formulation was impregnated in the dressing base (chitosan/gelatin; 2:1 weight/weight ratio) which exhibited more water absorption. In vivo evaluation revealed that the dressing displayed superior wound repair compared to the control in terms histol. examination and determination of alpha smooth muscle actin (α-SMA) and proliferating cell nuclear antigen (PCNA). Thus, SGE-loaded microemulsion-impregnated gelatin/chitosan could be a potential candidate for the wound healing. Drug Development and Industrial Pharmacy published new progress about Absorption. 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, SDS of cas: 6882-68-4.

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

Liang, Jinping; Liu, Juntong; Tang, Yezhen; Peng, Qian; Zhang, Ling; Ma, Xiaoxia; Xu, Nan; Wei, Jun; Han, Huaiqin published the artcile< Sophoridine inhibits endotoxin-induced acute lung injury by enhancing autophagy of macrophage and reducing inflammation>, Formula: C15H24N2O, the main research area is sophoridine macrophage autophagy inflammation acute lung injury; acute lung injury; autophagy; inflammation; sophoridine.

Acute lung injury (ALI) is characterized by uncontrolled inflammation, which can lead to respiratory distress syndrome and cause patient death. In this study, we sought to determine the role of sophoridine, a compound purified from sophora, in ALI. A mouse model of ALI was established by treating mice with LPS through nonexposed tracheal instillation. After LPS-induced mice were treated with sophoridine, LPS-induced alveolar wall thickening, alveolar interstitial inflammatory exudation and thickening, and the degree of pulmonary edema were found to be inhibited. Macrophages play an important role in inflammation, and in vitro experiments have demonstrated that sophoridine reduces the LPS-induced expression of inflammatory factors by macrophages, suggesting that sophoridine may inhibit lung inflammation in LPS-treated mice through reduces the secretion of inflammatory factors. Further, treatment with sophoridine up-regulated autophagy in macrophage cells in vitro and mouse lung tissues in vivo. LPS can bind to TLRs and activate the MyD88/NF-κB pathways, leading to increased inflammation in the pathogenesis of ALI. Our findings revealed that sophoridine down-regulated the expression of TLR4/MyD88/NF-κB and mTOR mRNA and protein in mouse pulmonary tissue. Collectively, these findings indicate that sophoridine may inhibit LPS-induced ALI by enhancing autophagy of macrophages and reducing inflammation.

Journal of Leukocyte Biology published new progress about Acute pulmonary injury. 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Formula: C15H24N2O.

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