Quercetin antagonized advanced glycated end products induced apoptosis and functional inhibition of fibroblasts from the prolapsed uterosacral ligament
In conclusion, quercetin antagonized AGEs-induced apoptosis and functional inhibition of fibroblasts from the prolapsed uterosacral ligament. And inhibiting AGEs-induced down-regulation of miR-4429/PTEN/PI3K/Akt pathway was the mechanism underlying the antagonistic effect of quercetin on AGEs-induced apoptosis.PMID:38044121 | DOI:10.5582/ddt.2023.01047 (Source: Drug Discoveries and Therapeutics)
Source: Drug Discoveries and Therapeutics - December 3, 2023 Category: Drugs & Pharmacology Authors: Yizhen Sima Junwei Li Leimei Xu Chengzhen Xiao Lisha Li Ling Wang Yisong Chen Source Type: research

Evaluation of < sup > D < /sup > -amino acid oxidase activity in rat kidney using a < sup > D < /sup > -kynurenine derivative, 6-methylthio- < sup > D < /sup > -kynurenine: An in vivo microdialysis study
Drug Discov Ther. 2023 Dec 3. doi: 10.5582/ddt.2023.01083. Online ahead of print.ABSTRACTD-Amino acid oxidase (DAO), a D-amino acid metabolizing enzyme, is reportedly associated with the psychiatric disease schizophrenia, suggesting a role for DAO inhibitors in its treatment. We have previously reported that DAO catalyzes the conversion of nonfluorescent 6-methylthio-D-kynurenine (MeS-D-KYN) to fluorescent 5-methylthiokynurenic acid (MeS-KYNA) in vitro. The present study aimed to determine the potential of MeS-D-KYN in evaluating DAO activity in vivo using renal microdialysis technique in rats. Male Sprague-Dawley rats wer...
Source: Drug Discoveries and Therapeutics - December 3, 2023 Category: Drugs & Pharmacology Authors: Takeshi Fukushima Ayano Kansaku Maho Umino Tatsuya Sakamoto Mayu Onozato Source Type: research

Generic selection criteria for safety and patient benefit [ Ⅻ]: Comparing the physicochemical and pharmaceutical properties of brand-name and generic tulobuterol tape
Drug Discov Ther. 2023 Dec 3. doi: 10.5582/ddt.2023.01076. Online ahead of print.ABSTRACTPhysicochemical properties (drug release, peel strength, adhesion, and stiffness) of Hokunalin® Tape (Hokunalin) and 13 generic transdermal bronchodilator patches containing tulobuterol were characterized and evaluated for comparison. Drug-release studies evaluating sustained release behavior demonstrated better performance by the drug Hokunalin, than the generics MED, YP, Sawai, and Teikoku. Hokunalin yield a 16.2% release 1 hour after initiation, 30.1% at 3 hours, 50.0% at 8 hours. In comparison, the generics MED, YP, Sawai, and Tei...
Source: Drug Discoveries and Therapeutics - December 3, 2023 Category: Drugs & Pharmacology Authors: Ken-Ichi Shimokawa Kayo Yotsukura Mitsuru Nozawa Yuko Wada Fumiyoshi Ishii Source Type: research

Development of a simple high-performance liquid chromatography-ultraviolet detection method for olaparib in patients with ovarian cancer
Drug Discov Ther. 2023 Dec 3. doi: 10.5582/ddt.2023.01074. Online ahead of print.ABSTRACTOlaparib is a small-molecule inhibitor of poly(ADP)-ribose polymerase (PARP) used as maintenance therapy for recurrent ovarian cancer and newly diagnosed advanced ovarian cancer after initial chemotherapy. An exposure-toxicity correlation has been reported between the probability of anemia, a common adverse event associated with olaparib, and the steady-state minimum plasma concentration (Cmin) as well as the predicted maximum plasma concentration (Cmax). On the other hand, olaparib exhibits high interpatient variability with regard to...
Source: Drug Discoveries and Therapeutics - December 3, 2023 Category: Drugs & Pharmacology Authors: Takeo Yasu Ryosuke Nishijima Risa Ikuta Mikio Shirota Haruko Iwase Source Type: research

Quercetin antagonized advanced glycated end products induced apoptosis and functional inhibition of fibroblasts from the prolapsed uterosacral ligament
In conclusion, quercetin antagonized AGEs-induced apoptosis and functional inhibition of fibroblasts from the prolapsed uterosacral ligament. And inhibiting AGEs-induced down-regulation of miR-4429/PTEN/PI3K/Akt pathway was the mechanism underlying the antagonistic effect of quercetin on AGEs-induced apoptosis.PMID:38044121 | DOI:10.5582/ddt.2023.01047 (Source: Drug Discoveries and Therapeutics)
Source: Drug Discoveries and Therapeutics - December 3, 2023 Category: Drugs & Pharmacology Authors: Yizhen Sima Junwei Li Leimei Xu Chengzhen Xiao Lisha Li Ling Wang Yisong Chen Source Type: research

Evaluation of < sup > D < /sup > -amino acid oxidase activity in rat kidney using a < sup > D < /sup > -kynurenine derivative, 6-methylthio- < sup > D < /sup > -kynurenine: An in vivo microdialysis study
Drug Discov Ther. 2023 Dec 3. doi: 10.5582/ddt.2023.01083. Online ahead of print.ABSTRACTD-Amino acid oxidase (DAO), a D-amino acid metabolizing enzyme, is reportedly associated with the psychiatric disease schizophrenia, suggesting a role for DAO inhibitors in its treatment. We have previously reported that DAO catalyzes the conversion of nonfluorescent 6-methylthio-D-kynurenine (MeS-D-KYN) to fluorescent 5-methylthiokynurenic acid (MeS-KYNA) in vitro. The present study aimed to determine the potential of MeS-D-KYN in evaluating DAO activity in vivo using renal microdialysis technique in rats. Male Sprague-Dawley rats wer...
Source: Drug Discoveries and Therapeutics - December 3, 2023 Category: Drugs & Pharmacology Authors: Takeshi Fukushima Ayano Kansaku Maho Umino Tatsuya Sakamoto Mayu Onozato Source Type: research

Generic selection criteria for safety and patient benefit [ Ⅻ]: Comparing the physicochemical and pharmaceutical properties of brand-name and generic tulobuterol tape
Drug Discov Ther. 2023 Dec 3. doi: 10.5582/ddt.2023.01076. Online ahead of print.ABSTRACTPhysicochemical properties (drug release, peel strength, adhesion, and stiffness) of Hokunalin® Tape (Hokunalin) and 13 generic transdermal bronchodilator patches containing tulobuterol were characterized and evaluated for comparison. Drug-release studies evaluating sustained release behavior demonstrated better performance by the drug Hokunalin, than the generics MED, YP, Sawai, and Teikoku. Hokunalin yield a 16.2% release 1 hour after initiation, 30.1% at 3 hours, 50.0% at 8 hours. In comparison, the generics MED, YP, Sawai, and Tei...
Source: Drug Discoveries and Therapeutics - December 3, 2023 Category: Drugs & Pharmacology Authors: Ken-Ichi Shimokawa Kayo Yotsukura Mitsuru Nozawa Yuko Wada Fumiyoshi Ishii Source Type: research

Development of a simple high-performance liquid chromatography-ultraviolet detection method for olaparib in patients with ovarian cancer
Drug Discov Ther. 2023 Dec 3. doi: 10.5582/ddt.2023.01074. Online ahead of print.ABSTRACTOlaparib is a small-molecule inhibitor of poly(ADP)-ribose polymerase (PARP) used as maintenance therapy for recurrent ovarian cancer and newly diagnosed advanced ovarian cancer after initial chemotherapy. An exposure-toxicity correlation has been reported between the probability of anemia, a common adverse event associated with olaparib, and the steady-state minimum plasma concentration (Cmin) as well as the predicted maximum plasma concentration (Cmax). On the other hand, olaparib exhibits high interpatient variability with regard to...
Source: Drug Discoveries and Therapeutics - December 3, 2023 Category: Drugs & Pharmacology Authors: Takeo Yasu Ryosuke Nishijima Risa Ikuta Mikio Shirota Haruko Iwase Source Type: research

Quercetin antagonized advanced glycated end products induced apoptosis and functional inhibition of fibroblasts from the prolapsed uterosacral ligament
In conclusion, quercetin antagonized AGEs-induced apoptosis and functional inhibition of fibroblasts from the prolapsed uterosacral ligament. And inhibiting AGEs-induced down-regulation of miR-4429/PTEN/PI3K/Akt pathway was the mechanism underlying the antagonistic effect of quercetin on AGEs-induced apoptosis.PMID:38044121 | DOI:10.5582/ddt.2023.01047 (Source: Drug Discoveries and Therapeutics)
Source: Drug Discoveries and Therapeutics - December 3, 2023 Category: Drugs & Pharmacology Authors: Yizhen Sima Junwei Li Leimei Xu Chengzhen Xiao Lisha Li Ling Wang Yisong Chen Source Type: research

Evaluation of < sup > D < /sup > -amino acid oxidase activity in rat kidney using a < sup > D < /sup > -kynurenine derivative, 6-methylthio- < sup > D < /sup > -kynurenine: An in vivo microdialysis study
Drug Discov Ther. 2023 Dec 3. doi: 10.5582/ddt.2023.01083. Online ahead of print.ABSTRACTD-Amino acid oxidase (DAO), a D-amino acid metabolizing enzyme, is reportedly associated with the psychiatric disease schizophrenia, suggesting a role for DAO inhibitors in its treatment. We have previously reported that DAO catalyzes the conversion of nonfluorescent 6-methylthio-D-kynurenine (MeS-D-KYN) to fluorescent 5-methylthiokynurenic acid (MeS-KYNA) in vitro. The present study aimed to determine the potential of MeS-D-KYN in evaluating DAO activity in vivo using renal microdialysis technique in rats. Male Sprague-Dawley rats wer...
Source: Drug Discoveries and Therapeutics - December 3, 2023 Category: Drugs & Pharmacology Authors: Takeshi Fukushima Ayano Kansaku Maho Umino Tatsuya Sakamoto Mayu Onozato Source Type: research

Generic selection criteria for safety and patient benefit [ Ⅻ]: Comparing the physicochemical and pharmaceutical properties of brand-name and generic tulobuterol tape
Drug Discov Ther. 2023 Dec 3. doi: 10.5582/ddt.2023.01076. Online ahead of print.ABSTRACTPhysicochemical properties (drug release, peel strength, adhesion, and stiffness) of Hokunalin® Tape (Hokunalin) and 13 generic transdermal bronchodilator patches containing tulobuterol were characterized and evaluated for comparison. Drug-release studies evaluating sustained release behavior demonstrated better performance by the drug Hokunalin, than the generics MED, YP, Sawai, and Teikoku. Hokunalin yield a 16.2% release 1 hour after initiation, 30.1% at 3 hours, 50.0% at 8 hours. In comparison, the generics MED, YP, Sawai, and Tei...
Source: Drug Discoveries and Therapeutics - December 3, 2023 Category: Drugs & Pharmacology Authors: Ken-Ichi Shimokawa Kayo Yotsukura Mitsuru Nozawa Yuko Wada Fumiyoshi Ishii Source Type: research

Development of a simple high-performance liquid chromatography-ultraviolet detection method for olaparib in patients with ovarian cancer
Drug Discov Ther. 2023 Dec 3. doi: 10.5582/ddt.2023.01074. Online ahead of print.ABSTRACTOlaparib is a small-molecule inhibitor of poly(ADP)-ribose polymerase (PARP) used as maintenance therapy for recurrent ovarian cancer and newly diagnosed advanced ovarian cancer after initial chemotherapy. An exposure-toxicity correlation has been reported between the probability of anemia, a common adverse event associated with olaparib, and the steady-state minimum plasma concentration (Cmin) as well as the predicted maximum plasma concentration (Cmax). On the other hand, olaparib exhibits high interpatient variability with regard to...
Source: Drug Discoveries and Therapeutics - December 3, 2023 Category: Drugs & Pharmacology Authors: Takeo Yasu Ryosuke Nishijima Risa Ikuta Mikio Shirota Haruko Iwase Source Type: research

Quercetin antagonized advanced glycated end products induced apoptosis and functional inhibition of fibroblasts from the prolapsed uterosacral ligament
In conclusion, quercetin antagonized AGEs-induced apoptosis and functional inhibition of fibroblasts from the prolapsed uterosacral ligament. And inhibiting AGEs-induced down-regulation of miR-4429/PTEN/PI3K/Akt pathway was the mechanism underlying the antagonistic effect of quercetin on AGEs-induced apoptosis.PMID:38044121 | DOI:10.5582/ddt.2023.01047 (Source: Drug Discoveries and Therapeutics)
Source: Drug Discoveries and Therapeutics - December 3, 2023 Category: Drugs & Pharmacology Authors: Yizhen Sima Junwei Li Leimei Xu Chengzhen Xiao Lisha Li Ling Wang Yisong Chen Source Type: research

Evaluation of < sup > D < /sup > -amino acid oxidase activity in rat kidney using a < sup > D < /sup > -kynurenine derivative, 6-methylthio- < sup > D < /sup > -kynurenine: An in vivo microdialysis study
Drug Discov Ther. 2023 Dec 3. doi: 10.5582/ddt.2023.01083. Online ahead of print.ABSTRACTD-Amino acid oxidase (DAO), a D-amino acid metabolizing enzyme, is reportedly associated with the psychiatric disease schizophrenia, suggesting a role for DAO inhibitors in its treatment. We have previously reported that DAO catalyzes the conversion of nonfluorescent 6-methylthio-D-kynurenine (MeS-D-KYN) to fluorescent 5-methylthiokynurenic acid (MeS-KYNA) in vitro. The present study aimed to determine the potential of MeS-D-KYN in evaluating DAO activity in vivo using renal microdialysis technique in rats. Male Sprague-Dawley rats wer...
Source: Drug Discoveries and Therapeutics - December 3, 2023 Category: Drugs & Pharmacology Authors: Takeshi Fukushima Ayano Kansaku Maho Umino Tatsuya Sakamoto Mayu Onozato Source Type: research

Generic selection criteria for safety and patient benefit [ Ⅻ]: Comparing the physicochemical and pharmaceutical properties of brand-name and generic tulobuterol tape
Drug Discov Ther. 2023 Dec 3. doi: 10.5582/ddt.2023.01076. Online ahead of print.ABSTRACTPhysicochemical properties (drug release, peel strength, adhesion, and stiffness) of Hokunalin® Tape (Hokunalin) and 13 generic transdermal bronchodilator patches containing tulobuterol were characterized and evaluated for comparison. Drug-release studies evaluating sustained release behavior demonstrated better performance by the drug Hokunalin, than the generics MED, YP, Sawai, and Teikoku. Hokunalin yield a 16.2% release 1 hour after initiation, 30.1% at 3 hours, 50.0% at 8 hours. In comparison, the generics MED, YP, Sawai, and Tei...
Source: Drug Discoveries and Therapeutics - December 3, 2023 Category: Drugs & Pharmacology Authors: Ken-Ichi Shimokawa Kayo Yotsukura Mitsuru Nozawa Yuko Wada Fumiyoshi Ishii Source Type: research