Therapeutic Potential of Danyankang Capsule in High-Fat Diet-Induced Cholelithiasis and Its Impact on Liver FXR Signaling and Gut Microbiota
In conclusion, the present study demonstrates that Danyankang exerts potent therapeutic efficacy against high-fat diet-induced cholelithiasis. This beneficial outcome is potentially linked to the inhibition of the TLR4/pNF-κB and SHP/CYP7A1/CYP8B1 signaling pathways, as well as the enhancement of intestinal flora species abundance.PMID:38522942 | DOI:10.1248/bpb.b24-00052 (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - March 24, 2024 Category: Drugs & Pharmacology Authors: Lin Zhou Chu-Ling Zhang Kun Jiang Hong-Yu Cheng Wen-Wen Xiong Ji-Xiao Zhu Source Type: research

Therapeutic Potential of Danyankang Capsule in High-Fat Diet-Induced Cholelithiasis and Its Impact on Liver FXR Signaling and Gut Microbiota
In conclusion, the present study demonstrates that Danyankang exerts potent therapeutic efficacy against high-fat diet-induced cholelithiasis. This beneficial outcome is potentially linked to the inhibition of the TLR4/pNF-κB and SHP/CYP7A1/CYP8B1 signaling pathways, as well as the enhancement of intestinal flora species abundance.PMID:38522942 | DOI:10.1248/bpb.b24-00052 (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - March 24, 2024 Category: Drugs & Pharmacology Authors: Lin Zhou Chu-Ling Zhang Kun Jiang Hong-Yu Cheng Wen-Wen Xiong Ji-Xiao Zhu Source Type: research

Spasmolytic Effect of Flopropione Does Not Involve Catechol-O- methyltransferase (COMT) Inhibition
Biol Pharm Bull. 2024;47(3):660-668. doi: 10.1248/bpb.b23-00808.ABSTRACTFlopropione (Flo) has been used for gallstone and urolithiasis as a spasmolytic agent almost exclusively in Japan. According to the package insert, its main mechanism is catechol-O-methyltransferase (COMT) inhibition and anti-serotonergic effect. This is obviously contrary to pharmacological common sense, but it is described that way in pharmacology textbooks and occurs in questions in the National Examination for Pharmacists in Japan. As this is a serious problem in education, we re-examined the action of Flo. The guinea pig ureter was hardly contract...
Source: Biological and Pharmaceutical Bulletin - March 20, 2024 Category: Drugs & Pharmacology Authors: Yoko Amagase Mari Hoshiyama Shiho Hasegawa Miwa Kanbara Yumiko Mizukawa Tetsuro Urushidani Source Type: research

Oxidized-LDL Induces Metabolic Dysfunction in Retinal Pigment Epithelial Cells
In this study, we focused on oxidized low-density lipoprotein (ox-LDL), a major constituent of drusen that accumulates in the retina of patients with AMD, and investigated whether it could be a causative factor for metabolic alterations in retinal pigment epithelial (RPE) cells. We found that prolonged exposure to ox-LDL induced changes in fatty acid β-oxidation (FAO), OXPHOS, and glycolytic activity and increased the mitochondrial reactive oxygen species production in RPE cells. Notably, the effects on metabolic alterations varied with the concentration and duration of ox-LDL treatment. In addition, we addressed the limi...
Source: Biological and Pharmaceutical Bulletin - March 20, 2024 Category: Drugs & Pharmacology Authors: Manami Tomomatsu Naoto Imamura Hoshimi Izumi Masatsugu Watanabe Masataka Ikeda Tomomi Ide Shohei Uchinomiya Akio Ojida Mirinthorn Jutanom Kazushi Morimoto Ken-Ichi Yamada Source Type: research

Platelets Affect the Activity of Amino Acid Transporter SNAT4 in HuH-7 Human Hepatoma Cells
In this study, we examined the effects of platelets on the activity of amino acid transporter system A, which is known to be changed by various factors, and we clarified the mechanism by which platelets affect system A activity. Among system A subtypes, we found that sodium-coupled neutral amino acid transporter (SNAT) 4 played a central role in the transport activity of system A in HuH-7 human hepatoma cells. Interestingly, platelets showed a biphasic effect on system A activity: activated platelet supernatants (APS) including the granule contents released from platelets downregulated system A activity at lower concentrat...
Source: Biological and Pharmaceutical Bulletin - March 20, 2024 Category: Drugs & Pharmacology Authors: Hitoshi Kashiwagi Yuki Sato Shunsuke Nashimoto Shungo Imai Yoh Takekuma Mitsuru Sugawara Source Type: research

Osteoblastgenic and Osteogenic Effects of KY-273 with CDK8/19 Inhibitory Activity in Bone Marrow Mesenchymal Stem Cells and Female Rats
In conclusion, KY-273 has cortical-bone-selective osteogenic effects by osteoblastogenesis via CDK8/19 inhibition in ovaries-intact and ovariectomized rats, and is an orally active drug candidate for bone diseases such as osteoporosis in monotherapy and combination therapy.PMID:38508765 | DOI:10.1248/bpb.b23-00834 (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - March 20, 2024 Category: Drugs & Pharmacology Authors: Megumi Yamamoto Yui Shibata Yuma Ito Masaki Fukui Hikaru Kioka Yoshimichi Shoji Tatsuya Kitao Hiroaki Shirahase Eiichi Hinoi Source Type: research

Spasmolytic Effect of Flopropione Does Not Involve Catechol-O- methyltransferase (COMT) Inhibition
Biol Pharm Bull. 2024;47(3):660-668. doi: 10.1248/bpb.b23-00808.ABSTRACTFlopropione (Flo) has been used for gallstone and urolithiasis as a spasmolytic agent almost exclusively in Japan. According to the package insert, its main mechanism is catechol-O-methyltransferase (COMT) inhibition and anti-serotonergic effect. This is obviously contrary to pharmacological common sense, but it is described that way in pharmacology textbooks and occurs in questions in the National Examination for Pharmacists in Japan. As this is a serious problem in education, we re-examined the action of Flo. The guinea pig ureter was hardly contract...
Source: Biological and Pharmaceutical Bulletin - March 20, 2024 Category: Drugs & Pharmacology Authors: Yoko Amagase Mari Hoshiyama Shiho Hasegawa Miwa Kanbara Yumiko Mizukawa Tetsuro Urushidani Source Type: research

Oxidized-LDL Induces Metabolic Dysfunction in Retinal Pigment Epithelial Cells
In this study, we focused on oxidized low-density lipoprotein (ox-LDL), a major constituent of drusen that accumulates in the retina of patients with AMD, and investigated whether it could be a causative factor for metabolic alterations in retinal pigment epithelial (RPE) cells. We found that prolonged exposure to ox-LDL induced changes in fatty acid β-oxidation (FAO), OXPHOS, and glycolytic activity and increased the mitochondrial reactive oxygen species production in RPE cells. Notably, the effects on metabolic alterations varied with the concentration and duration of ox-LDL treatment. In addition, we addressed the limi...
Source: Biological and Pharmaceutical Bulletin - March 20, 2024 Category: Drugs & Pharmacology Authors: Manami Tomomatsu Naoto Imamura Hoshimi Izumi Masatsugu Watanabe Masataka Ikeda Tomomi Ide Shohei Uchinomiya Akio Ojida Mirinthorn Jutanom Kazushi Morimoto Ken-Ichi Yamada Source Type: research

Platelets Affect the Activity of Amino Acid Transporter SNAT4 in HuH-7 Human Hepatoma Cells
In this study, we examined the effects of platelets on the activity of amino acid transporter system A, which is known to be changed by various factors, and we clarified the mechanism by which platelets affect system A activity. Among system A subtypes, we found that sodium-coupled neutral amino acid transporter (SNAT) 4 played a central role in the transport activity of system A in HuH-7 human hepatoma cells. Interestingly, platelets showed a biphasic effect on system A activity: activated platelet supernatants (APS) including the granule contents released from platelets downregulated system A activity at lower concentrat...
Source: Biological and Pharmaceutical Bulletin - March 20, 2024 Category: Drugs & Pharmacology Authors: Hitoshi Kashiwagi Yuki Sato Shunsuke Nashimoto Shungo Imai Yoh Takekuma Mitsuru Sugawara Source Type: research

Osteoblastgenic and Osteogenic Effects of KY-273 with CDK8/19 Inhibitory Activity in Bone Marrow Mesenchymal Stem Cells and Female Rats
In conclusion, KY-273 has cortical-bone-selective osteogenic effects by osteoblastogenesis via CDK8/19 inhibition in ovaries-intact and ovariectomized rats, and is an orally active drug candidate for bone diseases such as osteoporosis in monotherapy and combination therapy.PMID:38508765 | DOI:10.1248/bpb.b23-00834 (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - March 20, 2024 Category: Drugs & Pharmacology Authors: Megumi Yamamoto Yui Shibata Yuma Ito Masaki Fukui Hikaru Kioka Yoshimichi Shoji Tatsuya Kitao Hiroaki Shirahase Eiichi Hinoi Source Type: research

Spasmolytic Effect of Flopropione Does Not Involve Catechol-O- methyltransferase (COMT) Inhibition
Biol Pharm Bull. 2024;47(3):660-668. doi: 10.1248/bpb.b23-00808.ABSTRACTFlopropione (Flo) has been used for gallstone and urolithiasis as a spasmolytic agent almost exclusively in Japan. According to the package insert, its main mechanism is catechol-O-methyltransferase (COMT) inhibition and anti-serotonergic effect. This is obviously contrary to pharmacological common sense, but it is described that way in pharmacology textbooks and occurs in questions in the National Examination for Pharmacists in Japan. As this is a serious problem in education, we re-examined the action of Flo. The guinea pig ureter was hardly contract...
Source: Biological and Pharmaceutical Bulletin - March 20, 2024 Category: Drugs & Pharmacology Authors: Yoko Amagase Mari Hoshiyama Shiho Hasegawa Miwa Kanbara Yumiko Mizukawa Tetsuro Urushidani Source Type: research

Oxidized-LDL Induces Metabolic Dysfunction in Retinal Pigment Epithelial Cells
In this study, we focused on oxidized low-density lipoprotein (ox-LDL), a major constituent of drusen that accumulates in the retina of patients with AMD, and investigated whether it could be a causative factor for metabolic alterations in retinal pigment epithelial (RPE) cells. We found that prolonged exposure to ox-LDL induced changes in fatty acid β-oxidation (FAO), OXPHOS, and glycolytic activity and increased the mitochondrial reactive oxygen species production in RPE cells. Notably, the effects on metabolic alterations varied with the concentration and duration of ox-LDL treatment. In addition, we addressed the limi...
Source: Biological and Pharmaceutical Bulletin - March 20, 2024 Category: Drugs & Pharmacology Authors: Manami Tomomatsu Naoto Imamura Hoshimi Izumi Masatsugu Watanabe Masataka Ikeda Tomomi Ide Shohei Uchinomiya Akio Ojida Mirinthorn Jutanom Kazushi Morimoto Ken-Ichi Yamada Source Type: research

Platelets Affect the Activity of Amino Acid Transporter SNAT4 in HuH-7 Human Hepatoma Cells
In this study, we examined the effects of platelets on the activity of amino acid transporter system A, which is known to be changed by various factors, and we clarified the mechanism by which platelets affect system A activity. Among system A subtypes, we found that sodium-coupled neutral amino acid transporter (SNAT) 4 played a central role in the transport activity of system A in HuH-7 human hepatoma cells. Interestingly, platelets showed a biphasic effect on system A activity: activated platelet supernatants (APS) including the granule contents released from platelets downregulated system A activity at lower concentrat...
Source: Biological and Pharmaceutical Bulletin - March 20, 2024 Category: Drugs & Pharmacology Authors: Hitoshi Kashiwagi Yuki Sato Shunsuke Nashimoto Shungo Imai Yoh Takekuma Mitsuru Sugawara Source Type: research

Osteoblastgenic and Osteogenic Effects of KY-273 with CDK8/19 Inhibitory Activity in Bone Marrow Mesenchymal Stem Cells and Female Rats
In conclusion, KY-273 has cortical-bone-selective osteogenic effects by osteoblastogenesis via CDK8/19 inhibition in ovaries-intact and ovariectomized rats, and is an orally active drug candidate for bone diseases such as osteoporosis in monotherapy and combination therapy.PMID:38508765 | DOI:10.1248/bpb.b23-00834 (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - March 20, 2024 Category: Drugs & Pharmacology Authors: Megumi Yamamoto Yui Shibata Yuma Ito Masaki Fukui Hikaru Kioka Yoshimichi Shoji Tatsuya Kitao Hiroaki Shirahase Eiichi Hinoi Source Type: research

Ketogenic Diet Alleviates Mechanical Allodynia in the Models of Inflammatory and Neuropathic Pain in Male Mice
Biol Pharm Bull. 2024;47(3):629-634. doi: 10.1248/bpb.b23-00732.ABSTRACTInflammation is involved in the induction of chronic inflammatory and neuropathic pain. Moreover, the ketogenic diet, a high-fat, low-carbohydrate, and adequate protein diet, has an anti-inflammatory effect. Thus, we hypothesized that a ketogenic diet has a therapeutic effect on both types of chronic pain. In the present study, we investigated the effect of a ketogenic diet on mechanical allodynia, a chronic pain symptom, in formalin-induced chronic inflammatory pain and nerve injury-induced neuropathic pain models using adult male mice. Formalin injec...
Source: Biological and Pharmaceutical Bulletin - March 18, 2024 Category: Drugs & Pharmacology Authors: Kei Eto Masanori Ogata Yoshitaka Toyooka Toru Hayashi Hitoshi Ishibashi Source Type: research