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项与 Kotobuki Seika Co., Ltd. 相关的药物

KT-2962

靶点

TBXA2R

作用机制

TBXA2R拮抗剂

在研机构-

原研机构

Kotobuki Pharmaceutical Co. Ltd.

在研适应症-

非在研适应症

哮喘 [+2]

最高研发阶段终止

首次获批国家/地区-

首次获批日期-

KT-362

靶点

calcium channel

作用机制

calcium channel抑制剂

在研机构-

原研机构

Kotobuki Pharmaceutical Co. Ltd.

在研适应症-

非在研适应症

心律失常 [+3]

最高研发阶段终止

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首次获批日期-

KT-734

靶点

Phosphoric diester hydrolases

作用机制

磷酸二酯水解酶抑制剂

在研机构-

原研机构

Kotobuki Seika Co., Ltd.

在研适应症-

非在研适应症

高血压

最高研发阶段终止

首次获批国家/地区-

首次获批日期-

100 项与 Kotobuki Seika Co., Ltd. 相关的临床结果

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0 项与 Kotobuki Seika Co., Ltd. 相关的专利（医药）

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13

项与 Kotobuki Seika Co., Ltd. 相关的文献（医药）

2024-01-01·Food Science and Technology Research

Efficient and safe extraction of an antioxidant, 3,5,4’-trihydroxy-6,7-methylenedioxyflavone-3-<i>O</i>-glycoside, from indigo leaves using alkaline hydrolysis of modifying ester moieties

作者: Ishida, Miki ; Murota, Kaeko ; Jisaka, Mitsuo ; Kimura, Hideto ; Ishihara, Tomoe ; Hirabayashi, Yu

Indigo plant (Persicaria tinctoria (Aiton) Spach) has been utilized as a dye material with antioxidant activity.To increase polyphenol yield, alk. water was used for the extraction of indigo leaves.Total polyphenol content and hydrophilic oxygen radical absorbance capacity value of the alk. water extract were higher than those of the pure water extract, whereas its β-carotene bleaching inhibitory activity and 1,1-diphenyl-2-picrylhydrazyl radical scavenging activity were lower.The predominant compound in the alk. water extract was 3,5,4′-trihydroxy-6,7-methylenedioxyflavone (TMF)-3-O-β-D-glucopyranoside.β-Carotene bleaching inhibitory activity of TMF was higher than those of TMF-O-glycosides.TMF-3-O-βD-glucopyranoside was hydrolyzed by β-glucosidase from rat small intestine most effectively among the TMF-O-glycosides.Our results showed that alk. water extraction of indigo leaves is a useful method to increase the recovery of polyphenols, in which TMF-3-O-β-D-glucopyranoside is the predominant compound, which can be easily hydrolyzed in the small intestine to TMF with high antioxidant activity against lipid peroxidation

2021-01-01·Journal of Pharmaceutical and Biomedical Analysis3区 · 医学

Anti-inflammatory and bioavailability studies on dietary 3,5,4’-trihydroxy-6,7-methylenedioxyflavone-O-glycosides and their aglycone from indigo leaves in a murine model of inflammatory bowel disease

3区 · 医学

Article

作者: Yu Hirabayashi ; Mitsuo Jisaka ; Tomoe Ishihara ; Shota Tokuyama-Nakai ; Hideto Kimura ; Kazushige Yokota

Persicaria tinctoria (Aiton) Spach, also called Polygonum tinctorium Lour., (family Polygonaceae) for indigo plant has been traditionally useful as a medicinal or edible plant with a variety of biological activities. Of these, much attention has been paid to their anti-inflammatory activities. We have recently demonstrated that indigo leaves contain high levels of flavonol O-glycosides with 3,5,4'-trihydroxy-6,7-methylenedioxyflavone (TMF) as an aglycone. In this study, we attempted to evaluate anti-inflammatory activities of TMF-O-glycosides and free TMF prepared from indigo leaves after extraction with hot water. Free TMF was found to appreciably down-regulate the gene expression of pro-inflammatory cytokines including interleukin (IL)-1β, IL-6, inducible nitric oxide, and tumor necrosis factor-α in cultured macrophage cells stimulated with lipopolysaccharide while up-regulating the expression of anti-inflammatory IL-10. However, no study has been conducted regarding in vivo anti-inflammatory activities of TMF-O-glycosides and free TMF until now. Here, we assessed in vivo anti-inflammatory effects of these dietary compounds on ulcerative colitis in a murine model of inflammatory bowel disease by the induction with dextran sulfate sodium (DSS). Histological evaluation revealed that both TMF-O-glycosides and free TMF effectively protected against DSS-induced ulcerative colitis. The analysis of digested products by liquid chromatography and mass spectrometry led us to detect free TMF as a predominant metabolite in the feces of mice fed with TMF-O-glycosides. Moreover, free TMF was later detected as glucuronyl conjugates of TMF in the liver of mice fed with both fractions. These results indicate the effective digestion of TMF-O-glycosides and the subsequent absorption of free TMF in the gut of mice for exerting anti-inflammatory effects. Taken together, our findings suggest that dietary TMF-O-glycosides could be promising natural sources for the utilization as herbal medicine and nutraceuticals to expect in vivo anti-inflammatory activities.

2019-03-01·Heliyon

Constituents of flavonol O-glycosides and antioxidant activities of extracts from seeds, sprouts, and aerial parts of Polygonum tinctorium Lour.

Article

作者: Ishihara, Tomoe ; Jisaka, Mitsuo ; Yokota, Kazushige ; Tokuyama-Nakai, Shota ; Hirabayashi, Yu ; Kimura, Hideto

Polygonum tinctorium Lour. (family Polygonaceae), known as indigo plant, has been useful as a medicinal or edible plant abundant in polyphenolic compounds. We have recently shown that flavonol O-glycosides with 3,5,4'-trihydroxy-6,7-methylenedioxyflavone (TMF) are predominant flavonoids in indigo leaves. However, no study has been performed regarding changes in the levels of flavonoid species during the germination and growth of indigo plant. Here, we attempted to determine the individual constituents of flavonol O-glycosides and the changes in their contents of the seeds, sprouts, and aerial parts. These results revealed that only the seeds predominantly contained flavonol O-(acetyl)-rhamnosides with quercetin or kaempferol as an aglycone. During the development of the sprouts and aerial parts, flavonol O-glycosides with TMF as an aglycone became mainly detectable and accounted for 79.4% and 74.9% of total flavonol O-glycosides from the extracts of aerial parts harvested in 2016 and 2017, respectively. Of the plant organs tested, the aerial parts exhibited the highest antioxidant activities concomitant with greatly increased levels of total polyphenols. Thus, we were able to conduct the identification and quantification of flavonol O-glycosides from the seeds, sprouts, and aerial parts of indigo plant and to evaluate antioxidant activities of their extracts. Taken together, our findings clearly provide the evidence that the aerial parts of indigo plant are a rich source of flavonol O-glycosides with TMF and exhibit much higher antioxidant activities, indicating the usefulness for the application to food and nutraceutical purposes.

100 项与 Kotobuki Seika Co., Ltd. 相关的药物交易

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100 项与 Kotobuki Seika Co., Ltd. 相关的转化医学

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当前项目

药物(靶点)	适应症	全球最高研发状态

KT-6207 ( PPARα )	2型糖尿病更多	终止
KT-362 ( calcium channel )	心律失常更多	终止
KT-3866 ( Angiotensin II receptor )	高血压更多	终止
KT-2962 ( TBXA2R )	偏头痛更多	终止
KT-734 ( Phosphoric diester hydrolases )	高血压更多	终止