Tag: M.W=200-250

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

Wang, Qi; Li, Ying; Li, Kun-Wei; Zhou, Chang-Zheng published the artcile< Sophoridine: A review of its pharmacology, pharmacokinetics and toxicity>, 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 Review sophoridine pharmacol pharmacokinetics toxicity; Pharmacokinetics; Pharmacology; Sophoridine; Toxicology.

A review. Sophoridine is a bioactive alkaloid found in many Chinese herbs, such as Sophora alopecuroides l, Euchresta japonica Benth and Sophora moocrorftinan. Sophoridine hydrochloride injection has been approved as an anticancer drug in China. This aims to provide a comprehensive summary on the pharmacol., mol. mechanism, pharmacokinetic and toxicity studies of sophoridine. PubMed, Web of Science and China National Knowledge Infrastructure were used for a systematic search with the keywords including “”sophoridine””, “”pharmacol.””, “”pharmacokinetics””, and “”toxicity””. Emerging evidence suggests that sophoridine exhibits a broad spectrum of pharmacol. activities including antitumor, anti-inflammatory, antiviral, myocardialprotective and hepatoprotective activities. These pharmacol. properties lay foundation for using the plants containing sophoridine for the treatment of numerous diseases, such as cancer, colitis, injury of lungs, ischemia myocardial,etc. The mechanisms involved in the pharmacol. actions of sophoridine are regulation of NF-κB, TLR4/IRF3, JNK/ERK, Akt/mTOR signaling pathways, down-regulating the expression of HMG3B, bcl-2, MMP-2, MMP-9, TNF-α, IL-1β IL-6 and other cytokines or kinases. However, an increasing number of published reports indicated that sophoridine has serious adverse effects. The primary toxic effects are neurotoxicity and acute toxicity, which are of wide concern in worldwide. Moreover, sophoridine is reported to distribute in kidney, liver, uterus, lung and other organs. It undergoes glucuronidation and excreted in urine. Future studies should elucidate the detailed in vivo metabolism studies on sophoridine. The effect of substituent functional groups on sophoridine on metabolism, the enzymes involved in the metabolism and the chem. of metabolites also should be studied. Either structural modification of sophoridine or its combined with other drugs may play a pivotal role to enhance its pharmacol. activities and reduce its toxicity.

Phytomedicine 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, 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

Tang, Qing; Luo, Ding; Lin, Ding-Chai; Wang, Wen-Zhi; Li, Can-Jie; Zhuo, Xue-Fang; Wu, Zhong-Nan; Zhang, Yu-Bo; Wang, Guo-Cai; Li, Yao-Lan published the artcile< Five matrine-type alkaloids from Sophora tonkinensis>, 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 root 1213 dehydrosophoridine isosophocarpine sophoridine; 12,13-dehydrosophoridine; 13β-hydroxymatrine; Anti-inflammatory activity; Matrine-type alkaloid; Sophora tonkinensis.

Five matrine-type alkaloids (1-5) including two new compounds (1 and 3) and a new natural product (2) were isolated from the roots of Sophora tonkinesis. Their structures were identified by extensive spectroscopic anal. (UV, IR, HRESIMS and NMR). The absolute configurations of 2 and 3 were determined by X-ray diffraction. Compounds 1-5 were evaluated their activity against inflammatory cytokines TNF-α and IL-6 levels on LPS-induced RAW 264.7 macrophages, and compound 1 showed the most significant activity, potent than that of matrine, the representative ingredient from Sophora plants. Graphic abstract: [graphic not available: see fulltext]

Journal of Natural Medicines 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, 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

Zhu, Lingling; Huang, Shanshan; Li, Junhe; Chen, Jun; Yao, Yangyang; Li, Li; Guo, Hui; Xiang, Xiaojun; Deng, Jun; Xiong, Jianping published the artcile< Sophoridine inhibits lung cancer cell growth and enhances cisplatin sensitivity through activation of the p53 and Hippo signaling pathways>, 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 lung cancer sophoridine cisplatin sensitizer p53 Hippo signaling pathways; Cisplatin sensitivity; Hippo; Lung cancer; Sophoridine; p53.

Sophoridine, a quinolizidine alkaloid extracted from the Chinese herb Sophora alopecuroides L., has been reported to exert antitumor effects against multiple human cancers. However, few studies have evaluated its tumor-suppressing effects and associated mechanism with respect to lung cancer, in addition to its potential to be used for clin. lung cancer treatment. Different types of lung cancer cells were used to investigate the antitumor effects of sophoridine using cell viability, colony formation, and cell invasion, and migration assays. To determine the signaling pathways involved, western blot anal., quant. real-time polymerase chain reaction, an in vivo ubiquitination assay, and immunohistochem. were used in cellular assays and with a s.c. xenograft model in BALB/c mice. Sophoridine significantly suppressed the proliferation of and colony formation by lung cancer cells in vitro. Transwell assays demonstrated that sophoridine also inhibited invasion and migration in lung cancer cells. In addition, sophoridine enhanced the effects of cisplatin on lung cancer cells. A mechanistic study revealed that sophoridine significantly activated the Hippo and p53 signaling pathways, and mouse xenograft experiments further confirmed in vitro findings in lung cancer cells. Taken together, these results suggest that sophoridine can inhibit lung cancer progression and enhance the effects of the anticancer drug cisplatin against lung cancer cells. The mechanism of action of sophoridine might involve the Hippo and p53 signaling pathways.

Gene published new progress about Antitumor agents. 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

Gurung, Arun Bahadur; Ali, Mohammad Ajmal; Lee, Joongku; Abul Farah, Mohammad; Al-Anazi, Khalid Mashay published the artcile< Unravelling lead antiviral phytochemicals for the inhibition of SARS-CoV-2 Mpro enzyme through in silico approach>, Related Products of 6882-68-4, the main research area is COVID 19 coronavirus protease inhibition phytochem; Antiviral properties; Binding affinity; COVID-19; Medicinal plants; Molecular docking; Phytochemicals; SARS-CoV-2; SARS-CoV-2 M(pro).

A new SARS coronavirus (SARS-CoV-2) belonging to the genus Betacoronavirus has caused a pandemic known as COVID-19. Among coronaviruses, the main protease (Mpro) is an essential drug target which, along with papain-like proteases catalyzes the processing of polyproteins translated from viral RNA and recognizes specific cleavage sites. There are no human proteases with similar cleavage specificity and therefore, inhibitors are highly likely to be nontoxic. Therefore, targeting the SARS-CoV-2 Mpro enzyme with small mols. can block viral replication. The present study is aimed at the identification of promising lead mols. for SARS-CoV-2 Mpro enzyme through virtual screening of antiviral compounds from plants. The binding affinity of selected small drug-like mols. to SARS-CoV-2 Mpro, SARS-CoV Mpro, and MERS-CoV Mpro were studied using mol. docking. Bonducellpin D was identified as the best lead mol. which shows higher binding affinity (-9.28 kcal/mol) as compared to the control (-8.24 kcal/mol). The mol. binding was stabilized through 4 hydrogen bonds with Glu166 and Thr190 as well as hydrophobic interactions via 8 residues. The SARS-CoV-2 Mpro shows identities of 96.08% and 50.65% to that of SARS-CoV Mpro and MERS-CoV Mpro resp. at the sequence level. At the structural level, the root mean square deviation (RMSD) between SARS-CoV-2 Mpro and SARS-CoV Mpro was found to be 0.517 Å and 0.817 Å between SARS-CoV-2 Mpro and MERS-CoV Mpro. Bonducellpin D exhibited broad-spectrum inhibition potential against SARS-CoV Mpro and MERS-CoV Mpro and therefore is a promising drug candidate, which needs further validations through in vitro and in vivo studies.

Life Sciences published new progress about Antiviral agents. 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

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>, Reference of 6882-68-4, 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, Reference of 6882-68-4.

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>, Computed Properties of 6882-68-4, 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, Computed Properties of 6882-68-4.

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

Wang, Qi; Li, Ying; Li, Kun-Wei; Zhou, Chang-Zheng published the artcile< Sophoridine: A review of its pharmacology, pharmacokinetics and toxicity>, Synthetic Route of 6882-68-4, the main research area is Review sophoridine pharmacol pharmacokinetics toxicity; Pharmacokinetics; Pharmacology; Sophoridine; Toxicology.

A review. Sophoridine is a bioactive alkaloid found in many Chinese herbs, such as Sophora alopecuroides l, Euchresta japonica Benth and Sophora moocrorftinan. Sophoridine hydrochloride injection has been approved as an anticancer drug in China. This aims to provide a comprehensive summary on the pharmacol., mol. mechanism, pharmacokinetic and toxicity studies of sophoridine. PubMed, Web of Science and China National Knowledge Infrastructure were used for a systematic search with the keywords including “”sophoridine””, “”pharmacol.””, “”pharmacokinetics””, and “”toxicity””. Emerging evidence suggests that sophoridine exhibits a broad spectrum of pharmacol. activities including antitumor, anti-inflammatory, antiviral, myocardialprotective and hepatoprotective activities. These pharmacol. properties lay foundation for using the plants containing sophoridine for the treatment of numerous diseases, such as cancer, colitis, injury of lungs, ischemia myocardial,etc. The mechanisms involved in the pharmacol. actions of sophoridine are regulation of NF-κB, TLR4/IRF3, JNK/ERK, Akt/mTOR signaling pathways, down-regulating the expression of HMG3B, bcl-2, MMP-2, MMP-9, TNF-α, IL-1β IL-6 and other cytokines or kinases. However, an increasing number of published reports indicated that sophoridine has serious adverse effects. The primary toxic effects are neurotoxicity and acute toxicity, which are of wide concern in worldwide. Moreover, sophoridine is reported to distribute in kidney, liver, uterus, lung and other organs. It undergoes glucuronidation and excreted in urine. Future studies should elucidate the detailed in vivo metabolism studies on sophoridine. The effect of substituent functional groups on sophoridine on metabolism, the enzymes involved in the metabolism and the chem. of metabolites also should be studied. Either structural modification of sophoridine or its combined with other drugs may play a pivotal role to enhance its pharmacol. activities and reduce its toxicity.

Phytomedicine 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, Synthetic Route of 6882-68-4.

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

Tang, Qing; Luo, Ding; Lin, Ding-Chai; Wang, Wen-Zhi; Li, Can-Jie; Zhuo, Xue-Fang; Wu, Zhong-Nan; Zhang, Yu-Bo; Wang, Guo-Cai; Li, Yao-Lan published the artcile< Five matrine-type alkaloids from Sophora tonkinensis>, HPLC of Formula: 6882-68-4, the main research area is Sophora root 1213 dehydrosophoridine isosophocarpine sophoridine; 12,13-dehydrosophoridine; 13β-hydroxymatrine; Anti-inflammatory activity; Matrine-type alkaloid; Sophora tonkinensis.

Five matrine-type alkaloids (1-5) including two new compounds (1 and 3) and a new natural product (2) were isolated from the roots of Sophora tonkinesis. Their structures were identified by extensive spectroscopic anal. (UV, IR, HRESIMS and NMR). The absolute configurations of 2 and 3 were determined by X-ray diffraction. Compounds 1-5 were evaluated their activity against inflammatory cytokines TNF-α and IL-6 levels on LPS-induced RAW 264.7 macrophages, and compound 1 showed the most significant activity, potent than that of matrine, the representative ingredient from Sophora plants. Graphic abstract: [graphic not available: see fulltext]

Journal of Natural Medicines 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, HPLC of Formula: 6882-68-4.

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

Zhu, Lingling; Huang, Shanshan; Li, Junhe; Chen, Jun; Yao, Yangyang; Li, Li; Guo, Hui; Xiang, Xiaojun; Deng, Jun; Xiong, Jianping published the artcile< Sophoridine inhibits lung cancer cell growth and enhances cisplatin sensitivity through activation of the p53 and Hippo signaling pathways>, Related Products of 6882-68-4, the main research area is lung cancer sophoridine cisplatin sensitizer p53 Hippo signaling pathways; Cisplatin sensitivity; Hippo; Lung cancer; Sophoridine; p53.

Sophoridine, a quinolizidine alkaloid extracted from the Chinese herb Sophora alopecuroides L., has been reported to exert antitumor effects against multiple human cancers. However, few studies have evaluated its tumor-suppressing effects and associated mechanism with respect to lung cancer, in addition to its potential to be used for clin. lung cancer treatment. Different types of lung cancer cells were used to investigate the antitumor effects of sophoridine using cell viability, colony formation, and cell invasion, and migration assays. To determine the signaling pathways involved, western blot anal., quant. real-time polymerase chain reaction, an in vivo ubiquitination assay, and immunohistochem. were used in cellular assays and with a s.c. xenograft model in BALB/c mice. Sophoridine significantly suppressed the proliferation of and colony formation by lung cancer cells in vitro. Transwell assays demonstrated that sophoridine also inhibited invasion and migration in lung cancer cells. In addition, sophoridine enhanced the effects of cisplatin on lung cancer cells. A mechanistic study revealed that sophoridine significantly activated the Hippo and p53 signaling pathways, and mouse xenograft experiments further confirmed in vitro findings in lung cancer cells. Taken together, these results suggest that sophoridine can inhibit lung cancer progression and enhance the effects of the anticancer drug cisplatin against lung cancer cells. The mechanism of action of sophoridine might involve the Hippo and p53 signaling pathways.

Gene published new progress about Antitumor agents. 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