Category: 152121-47-6

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 152121-47-6, Name is SB-203580, molecular formula is C21H16FN3OS. In an article, author is Kushida, Hirotaka,once mentioned of 152121-47-6, Product Details of 152121-47-6.

Ethnopharmacological relevance: Geissoschizine methyl ether (GM), an indole alkaloid from Uncaria hook, is an active ingredient in the traditional Japanese Kampo medicine yokukansan, which is used to treat neurosis, insomnia, irritability, and night crying in children. Aim of the study: Recent our pharmacokinetic studies suggested that there may be gender differences in the plasma concentrations of GM in rats, but not in humans. However, the details of this difference remain unverified. The purpose of this study was to clarify the reasons for the gender differences in rats. Materials and methods: GM plasma pharmacokinetics was compared in male and female rats orally administered yokukansan (4 g/kg). To confirm the involvement of cytochrome P450 (CYP) in GM liver metabolism, GM was incubated with male and female rat liver 59 fraction in the absence or presence of 1-aminobenzotriazole (a nonspecific CYP inhibitor). CYP isoforms involved in GM metabolism were estimated using recombinant rat CYP isoforms and anti-rat CYP antibodies. Results: The maximum GM plasma concentrations were significantly higher in female than in male rats. When GM was incubated with rat liver 59 fractions, GM reduction was more striking in male 59 (69.3%) than that in female 59 (10.0%) and was completely blocked with nonspecific CYP inhibitor 1-aminobenzotriazole. Screening experiments using recombinant rat cytochmme P450 (CYP) isoforms showed that CYP1A1, CYP2C6, CYP2C11, CYP2D1, and CYP3A2 were involved in GM metabolism. Of these CYP isoforms, the use of anti-rat CYP antibodies indicated that male-dependent CYP2C11 and CYP3A2 were predominantly involved in the liver micro-somal GM metabolism with gender differences. Conclusions: These results suggest that the cause of gender differences in plasma GM pharmacokinetics in rats is most likely because of male-dependent CYP2C11 and CYP3A2, and provide also useful information to further evaluate the pharmacological and toxicological effects in future. This study is the first to demonstrate that the gender differences in plasma GM pharmacokinetics in rats are caused by the gender-dependent metabolism of GM.

Interested yet? Keep reading other articles of 152121-47-6, you can contact me at any time and look forward to more communication. Product Details of 152121-47-6.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Hadi, Fazal, once mentioned the application of 152121-47-6, Name is SB-203580, molecular formula is C21H16FN3OS, molecular weight is 377.4347, MDL number is MFCD00922198, category is indole-building-block. Now introduce a scientific discovery about this category, Category: indole-building-block.

Phytoremediation has emerged as promising technology for reclamation of metal-polluted sites. The present study was conducted with an aim to assess the hyperaccumulation potential of Ricinus communis for cadmium, with the application of exogenous substances, [nitrogen (N), phosphorus (P) and potassium (K)] and phytohormones [Gibberellic acid (GA(3)) and Indole acetic acid (IAA)]. These were applied to increase plant biomass, improve phytoextraction of Cd and its accumulation in aerial parts, with generation of endogenous proline and phenols in R. communis, grown in soil contaminated with 100 mg Cd/Kg. Plant hormones were used only as foliar spray while growth regulators were applied to soil and also used as foliar spray. T4 (Cd+NPK (AS)) significantly increased root length, T12 (GA3+ NPK (FS)) highly increased stem length and leaf length as compared to control C1 (plant only Cd). FBM was highly increased by N alone or in combination with P, K, and GA(3) foliar sprayed in R. communis. Conclusively, it was found that NPK (foliar) in combination with GA(3) followed by N and IAA, significantly increased biomass, Cd concentration and accumulation in all the treated plants of R. communis. Cadmium bio-concentration values for R. communis were higher than unity (1) i.e. +/- 2.54. Highest significant concentration of phenolic and proline in R. communis were recorded in combination treatments of GA(3) and NPK foliar spray while in other plants in NPK addition into soil treatment. Thus, R. communis has the natural potential as hyperaccumulator and further study is required for its industrial implementation in polluted soil.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

In an article, author is Wei, Yu-Fang, once mentioned the application of 152121-47-6, Quality Control of SB-203580, Name is SB-203580, molecular formula is C21H16FN3OS, molecular weight is 377.4347, MDL number is MFCD00922198, category is indole-building-block. Now introduce a scientific discovery about this category.

This article reported a hemicyanine dye fluorescent probe (1), based on benzo[e]indole and aromatic azonia skeleton, for simultaneous detection of viscosity fluctuation in mitochondria and lysosomes. Probe 1 exhibited near infrared emission and high sensitivity towards viscosity of the medium. As the viscosity increases, the rotation of C-C single bond between the benzo[e]indole and the nitrogen heterocycle could be suppressed, and the entire molecular scaffold was coplanar and emitted strong fluorescence due to more delocalized electron distribution. The fluorescence intensity of probe 1 was enhanced 16.2 times at 650 nm as the viscosity increased from 0.89 cP to 865 cP. Correspondingly, the fluorescence quantum yield of probe 1 increased from 4.2% to 49.6%. The change of lg (I-650nm) had a good linear relationship with lgri (viscosity values: 0.89 cP to 8.6 cP), which meant the viscosity of dilute solution could be detected quantitatively. In cell experiments, probe 1 with low concentration (500 nM) had stronger fluorescence intensity in cancer cells than in normal cells. Besides, probe 1 could monitor the viscosity changes of mitochondria and lysosomes caused by the addition of ionophores (monensin, nystatin and dexamethasone) or in the process of autophagy. The results provide a simple and effective method for the early diagnosis of related diseases.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Application of 152121-47-6, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, 152121-47-6, Name is SB-203580, SMILES is CS(=O)C1=CC=C(C=C1)C1=NC(=C(N1)C1=CC=NC=C1)C1=CC=C(F)C=C1, belongs to indole-building-block compound. In a article, author is Yang, Jin, introduce new discover of the category.

A series of well-defined (NHC)Pd(N-heterocyclic carboxylate)(OAc) complexes (N-heterocyclic carboxylate = pyridine-2-carboxylate, quinoline-2-carboxylate andisoquinoline-1-carboxylate) were synthesized and fully characterized by NMR spectra, HR-MS and X-ray single crystal diffraction. The obtained complexes were then used for direct C2-arylation of free (NH)-indoles with arylsulfonyl hydrazides. With low catalyst loading, all complexes exhibited high catalytic activities for the arylation reactions.

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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 152121-47-6, Name is SB-203580, molecular formula is C21H16FN3OS. In an article, author is Kushida, Hirotaka,once mentioned of 152121-47-6, Recommanded Product: 152121-47-6.

Gender differences in plasma pharmacokinetics and hepatic metabolism of geissoschizine methyl ether from Uncaria hook in rats

Ethnopharmacological relevance: Geissoschizine methyl ether (GM), an indole alkaloid from Uncaria hook, is an active ingredient in the traditional Japanese Kampo medicine yokukansan, which is used to treat neurosis, insomnia, irritability, and night crying in children. Aim of the study: Recent our pharmacokinetic studies suggested that there may be gender differences in the plasma concentrations of GM in rats, but not in humans. However, the details of this difference remain unverified. The purpose of this study was to clarify the reasons for the gender differences in rats. Materials and methods: GM plasma pharmacokinetics was compared in male and female rats orally administered yokukansan (4 g/kg). To confirm the involvement of cytochrome P450 (CYP) in GM liver metabolism, GM was incubated with male and female rat liver 59 fraction in the absence or presence of 1-aminobenzotriazole (a nonspecific CYP inhibitor). CYP isoforms involved in GM metabolism were estimated using recombinant rat CYP isoforms and anti-rat CYP antibodies. Results: The maximum GM plasma concentrations were significantly higher in female than in male rats. When GM was incubated with rat liver 59 fractions, GM reduction was more striking in male 59 (69.3%) than that in female 59 (10.0%) and was completely blocked with nonspecific CYP inhibitor 1-aminobenzotriazole. Screening experiments using recombinant rat cytochmme P450 (CYP) isoforms showed that CYP1A1, CYP2C6, CYP2C11, CYP2D1, and CYP3A2 were involved in GM metabolism. Of these CYP isoforms, the use of anti-rat CYP antibodies indicated that male-dependent CYP2C11 and CYP3A2 were predominantly involved in the liver micro-somal GM metabolism with gender differences. Conclusions: These results suggest that the cause of gender differences in plasma GM pharmacokinetics in rats is most likely because of male-dependent CYP2C11 and CYP3A2, and provide also useful information to further evaluate the pharmacological and toxicological effects in future. This study is the first to demonstrate that the gender differences in plasma GM pharmacokinetics in rats are caused by the gender-dependent metabolism of GM.

Interested yet? Keep reading other articles of 152121-47-6, you can contact me at any time and look forward to more communication. Recommanded Product: 152121-47-6.

Reference:
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles