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Possible Involvement of Protein Binding Inhibition in Changes in Dexmedetomidine Concentration in Extracorporeal Circuits during Midazolam Use
In this study, we investigated whether displacement of dexmedetomidine by midazolam from the binding site of major plasma proteins, human serum albumin (HSA) and α1-acid glycoprotein (AAG), would increase levels of free dexmedetomidine that could be adsorbed to the circuit. Equilibrium dialysis experiments indicated that dexmedetomidine binds to a single site on both HSA and AAG with four times greater affinity than midazolam. Midazolam-mediated inhibition of the binding of dexmedetomidine to HSA and AAG was also examined. The binding of dexmedetomidine to these proteins decreased in the presence of midazolam. Competitive...
Source: Biological and Pharmaceutical Bulletin - February 7, 2024 Category: Drugs & Pharmacology Authors: Keishi Yamasaki Masahiro Tokuno Kenji Tsukigawa Yuka Nagatsuka Koji Nishi Masaki Otagiri Yuhki Sato Source Type: research

Generation of Dopamine Transporter (DAT)-mCherry Knock-in Rats by CRISPR-Cas9 Genome Editing
Biol Pharm Bull. 2024;47(2):394-398. doi: 10.1248/bpb.b23-00598.ABSTRACTMidbrain dopaminergic neurons respond to rewards and have a crucial role in positive motivation and pleasure. Electrical stimulation of dopaminergic neurons and/or their axonal fibers and arborization has been often used to motivate animals to perform cognitive tasks. Still, the electrical stimulation is incompatible with electrophysiological recordings. In this light, optical stimulation following artificial expression of channelrhodopsin-2 (ChR2) in the cell membrane has been also used, but the expression level of ChR2 varies among researchers. Thus,...
Source: Biological and Pharmaceutical Bulletin - February 7, 2024 Category: Drugs & Pharmacology Authors: Nobuyoshi Matsumoto Miyuki Miyano Takaya Abe Tetsuhiko Kashima Eriko Kato-Ishikura Ken-Ichi Inoue Jiayan Liu Hiroshi Kiyonari Haruki Takeuchi Yuji Ikegaya Source Type: research

Scraping Assay as a Novel Strategy to Evaluate Axonal Regeneration Using Human-Induced Pluripotent Stem Cell-Derived Neurons
Biol Pharm Bull. 2024;47(2):366-372. doi: 10.1248/bpb.b23-00675.ABSTRACTNeuronal regrowth after traumatic injury is strongly inhibited in the central nervous system (CNS) of adult mammals. Cell-intrinsic and extrinsic factors limit the regulation of axonal growth and regrowth of fibers is minimal despite nearly all neurons surviving. Developing medical drugs to promote neurological recovery is crucial since neuronal injuries have few palliative cares and no pharmacological interventions. Herein, we developed a novel in vitro axonal regeneration assay system to screen the chemical reagents using human-induced pluripotent st...
Source: Biological and Pharmaceutical Bulletin - February 7, 2024 Category: Drugs & Pharmacology Authors: Tomu Oonishi Kaneyasu Nishimura Kazuyuki Takata Masahiro Fujimuro Yuichi Sekine Source Type: research

Efficacy of Glycicumarin and Isoliquiritigenin in Suppressing Colonic Peristalsis in Both an Animal Model and a Clinical Trial
We examined the relationship between SKT and intestinal peristalsis in an animal model and a prospective study. In the animal model, SKT and its components were administered from the serosal side of the colon and colonic peristalsis was evaluated using intraluminal pressure and spatiotemporal mapping before and after the administration of SKT and its components. In this clinical trial, we used abdominal ultrasonography (US) to obtain long-axis images of the sigmoid colon of 11 patients. The frequency of intestinal peristalsis was measured using US in five patients with SKT and six patients without medication after the inge...
Source: Biological and Pharmaceutical Bulletin - February 7, 2024 Category: Drugs & Pharmacology Authors: Reo Kobayashi Ken Inoue Satoshi Sugino Ryohei Hirose Toshifumi Doi Akihito Harusato Osamu Dohi Naohisa Yoshida Kazuhiko Uchiyama Takeshi Ishikawa Tomohisa Takagi Hideyuki Konishi Yasuko Hirai Katsura Mizushima Yuji Naito Yoshito Itoh Source Type: research

Association between the Prognostic Nutritional Index and the Occurrence of Immune-Related Adverse Events
In conclusion, pretreatment PNI may be associated with the risk of developing irAEs in patients with advanced recurrent solid tumors. When the PNI is ≥44.2, patient management is important for avoiding serious AEs because while the treatment may be effective, the occurrence of irAEs is a concern.PMID:38311396 | DOI:10.1248/bpb.b23-00760 (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - February 4, 2024 Category: Drugs & Pharmacology Authors: Tatsuya Furuno Rintaro Sogawa Takanori Hashimoto Shunsuke Matsuo Wakako Shirahama Tomoko Kamura Kazuhisa Hosoya Yoko Senjyu Yoshio Yamashita Takuya Inoue Moriyasu Yamauchi Hiroo Katsuya Mitsuru Noguchi Naoko Sueoka-Aragane Chisato Shimanoe Source Type: research

Role of the Cytosolic Domain of the a3 Subunit of V-ATPase in the Interaction with Rab7 and Secretory Lysosome Trafficking in Osteoclasts
Biol Pharm Bull. 2024;47(1):339-344. doi: 10.1248/bpb.b23-00833.ABSTRACTWe previously reported that the a3 subunit of proton-pumping vacuolar-type ATPase (V-ATPase) interacts with Rab7 and its guanine nucleotide exchange factor, Mon1a-Ccz1, and recruits them to secretory lysosomes in osteoclasts, which is essential for anterograde trafficking of secretory lysosomes. The a3 subunit interacts with Mon1a-Ccz1 through its cytosolic N-terminal domain. Here, we examined the roles of this domain in the interaction with Rab7 and trafficking of secretory lysosomes. Immunoprecipitation experiments showed that a3 interacted with Rab7...
Source: Biological and Pharmaceutical Bulletin - January 31, 2024 Category: Drugs & Pharmacology Authors: Mayumi Nakanishi-Matsui Naomi Matsumoto Ge-Hong Sun-Wada Yoh Wada Source Type: research

A Morpholine Derivative N-(4-Morpholinomethylene)ethanesulfonamide Induces Ferroptosis in Tumor Cells by Targeting NRF2
Biol Pharm Bull. 2024 Feb 14;47(2):417-426. doi: 10.1248/bpb.b23-00544. Epub 2024 Jan 30.ABSTRACTSmall molecule drugs containing morpholine-based moieties have become crucial candidates in the tumor targeted therapy strategies, but the specific molecular mechanisms of these drugs causing tumor cell death require further investigation. The morpholine derivative N-(4-morpholinomethylene)ethanesulfonamide (MESA) was used to stimulate prostate and ovarian cancer cells and we focused on the ferroptosis effects, including the target molecule and signal pathways mediated by MESA. The results showed that MESA could induce ferropto...
Source: Biological and Pharmaceutical Bulletin - January 31, 2024 Category: Drugs & Pharmacology Authors: Bingchun Sun Ligang Zhang Binhua Wu Xiping Luo Source Type: research

A Novel Strategy for the Discovery of Drug Targets: Integrating Clinical Evidence with Molecular Studies
Biol Pharm Bull. 2024;47(2):345-349. doi: 10.1248/bpb.b23-00831.ABSTRACTThe mechanisms of several drugs remain unclear, limiting our understanding of how they exert their effects. Receptor affinities have not been comprehensively measured during drug development, and the safety investigations in humans are limited. Therefore, numerous unknown adverse and beneficial effects of drugs in humans persist. In this review, I highlight our achievements in identifying the unexpected beneficial effects of drugs through the analysis of real-world clinical data, which can contribute to drug repositioning and target finding. (1) Throug...
Source: Biological and Pharmaceutical Bulletin - January 31, 2024 Category: Drugs & Pharmacology Authors: Shuji Kaneko Source Type: research

Drug Discovery Research for Traumatic Brain Injury Focused on Functional Molecules in Astrocytes
Biol Pharm Bull. 2024;47(2):350-360. doi: 10.1248/bpb.b23-00731.ABSTRACTTraumatic brain injury (TBI) is severe damage to the head caused by traffic accidents, falls, and sports. Because TBI-induced disruption of the blood-brain barrier (BBB) causes brain edema and neuroinflammation, which are major causes of death or serious disabilities, protection and recovery of BBB function may be beneficial therapeutic strategies for TBI. Astrocytes are key components of BBB integrity, and astrocyte-derived bioactive factors promote and suppress BBB disruption in TBI. Therefore, the regulation of astrocyte function is essential for BB...
Source: Biological and Pharmaceutical Bulletin - January 31, 2024 Category: Drugs & Pharmacology Authors: Shotaro Michinaga Source Type: research

Inhibitory Actions of Antidepressants, Hypnotics, and Anxiolytics on Recombinant Human Acetylcholinesterase Activity
Biol Pharm Bull. 2024;47(1):328-333. doi: 10.1248/bpb.b23-00719.ABSTRACTAlzheimer's disease (AD) is accompanied by behavioral and psychological symptoms of dementia (BPSD), which is often alleviated by treatment with psychotropic drugs, such as antidepressants, hypnotics, and anxiolytics. If these drugs also inhibit acetylcholinesterase (AChE) activity, they may contribute to the suppression of AD progression by increasing brain acetylcholine concentrations. We tested the potential inhibitory effects of 31 antidepressants, 21 hypnotics, and 12 anxiolytics on recombinant human AChE (rhAChE) activity. At a concentration of 1...
Source: Biological and Pharmaceutical Bulletin - January 31, 2024 Category: Drugs & Pharmacology Authors: Keisuke Obara Haruka Mori Suzune Ihara Kento Yoshioka Yoshio Tanaka Source Type: research

The Mechanism of 5-Fluorouracil-Induced Hyperpigmentation in HRM-2 Hairless Mice: Focus on the Increase of Blood Vessels
In conclusion, this study indicates that 5-FU causes hyperpigmentation by melanin accumulation in a characteristic manner, including an increase in blood vessels.PMID:38281766 | DOI:10.1248/bpb.b23-00584 (Source: Biological and Pharmaceutical Bulletin)
Source: Biological and Pharmaceutical Bulletin - January 28, 2024 Category: Drugs & Pharmacology Authors: Atsuo Fujito Shota Tanaka Keiichi Hiramoto Ning Ma Kazuya Ooi Source Type: research

Proteomic Analysis of Staphylococcus aureus Treated with ShangKeHuangShui
This study's primary objective was to delve into the antibacterial properties, potential antibacterial compounds within SKHS, and their associated molecular targets. In vitro SKHS antibacterial assays demonstrated that the minimum inhibitory concentration (MIC) was 8.625 mg/mL and the minimum bactericide concentration (MBC) was 17.25 mg/mL. Proteomic analysis based on tandem mass tag (TMT) showed significant changes in the expression level of 246 proteins in SKHS treated group compared to control group, with 79 proteins upregulated and 167 proteins downregulated (>1.5-fold, p < 0.05). Subsequently, thirteen target pr...
Source: Biological and Pharmaceutical Bulletin - January 28, 2024 Category: Drugs & Pharmacology Authors: Lichu Liu Na Zhao Kuangyang Yang Honghong Liao Xiaofang Liu Ying Wu Yan Wang Xiao Peng Yuanyan Wu Source Type: research

Hydroxytyrosol Alleviates Methotrexate-Induced Pulmonary Fibrosis in Rats: Involvement of TGF- β1, Tissue Factor, and VEGF
Biol Pharm Bull. 2024;47(1):303-310. doi: 10.1248/bpb.b23-00477.ABSTRACTMethotrexate (MTX) is an indispensable drug used for the treatment of many autoimmune and cancerous diseases. However, its clinical use is associated with serious side effects, such as lung fibrosis. The main objective of this study is to test the hypothesis that hydroxytyrosol (HT) can mitigate MTX-induced lung fibrosis in rats while synergizing MTX anticancer effects. Pulmonary fibrosis was induced in the rats using MTX (14 mg/kg/week, per os (p.o.)). The rats were treated with or without HT (10, 20, and 40 mg/kg/d p.o.) or dexamethasone (DEX; 0.5 mg...
Source: Biological and Pharmaceutical Bulletin - January 28, 2024 Category: Drugs & Pharmacology Authors: Mohamed F Manie Hala M Fawzy El-Sayed M El-Sayed Source Type: research

Wild-Type DCTN1 Suppresses the Aggregation of DCTN1 Mutants Associated with Perry Disease
In this study, we comprehensively investigated the intracellular distribution of the p150glued mutants in HEK293T cells. We further assessed the effect of co-overexpression of the wild-type p150glued protein with mutants on the formation of mutant aggregates. Notably, overexpression of p150glued mutants identified in healthy controls, which is also associated with amyotrophic lateral sclerosis, showed a thread-like cytoplasmic distribution, similar to the wild-type p150glued. In contrast, p150glued mutants in Perry disease and motor neuron disease caused aggregation. In addition, the co-overexpression of the wild-type prot...
Source: Biological and Pharmaceutical Bulletin - January 24, 2024 Category: Drugs & Pharmacology Authors: Yuto Fukui Hisashi Shirakawa Shuji Kaneko Kazuki Nagayasu Source Type: research

Development of Hollow Gold Nanoparticles for Photothermal Therapy and Their Cytotoxic Effect on a Glioma Cell Line When Combined with Copper Diethyldithiocarbamate
Biol Pharm Bull. 2024;47(1):272-278. doi: 10.1248/bpb.b23-00789.ABSTRACTGold-based nanoparticles hold promise as functional nanomedicines, including in combination with a photothermal effect for cancer therapy in conjunction with chemotherapy. Here, we synthesized hollow gold nanoparticles (HGNPs) exhibiting efficient light absorption in the near-IR (NIR) region. Several synthesis conditions were explored and provided monodisperse HGNPs approximately 95-135 nm in diameter with a light absorbance range of approximately 600-720 nm. The HGNPs were hollow and the surface had protruding structures when prepared using high conce...
Source: Biological and Pharmaceutical Bulletin - January 24, 2024 Category: Drugs & Pharmacology Authors: Jin Liu Tatsuaki Tagami Koki Ogawa Tetsuya Ozeki Source Type: research