[Translation] A single-center, open-label, single-arm study evaluating the drug-drug interactions of fluvoxamine and rifampicin on succinylcholine tablets in healthy adult Chinese volunteers

主要目的：（1）评价琥珀八氢氨吖啶片单独使用和与氟伏沙明合用时在中国成年健康受试者中的药代动力学特征；（2）评价琥珀八氢氨吖啶片单独使用和与利福平合用时在中国成年健康受试者中的药代动力学特征。次要目的：（1）评价琥珀八氢氨吖啶片单独使用和与氟伏沙明合用时在中国成年健康受试者中的安全性和耐受性特征；（2）评价琥珀八氢氨吖啶片单独使用和与利福平合用时在中国成年健康受试者中的安全性和耐受性特征。

[Translation]

Primary objectives: (1) To evaluate the pharmacokinetic characteristics of succinic acid tablets when used alone and in combination with fluvoxamine in healthy adult Chinese subjects; (2) To evaluate the pharmacokinetic characteristics of succinic acid tablets when used alone and in combination with rifampicin in healthy adult Chinese subjects. Secondary objectives: (1) To evaluate the safety and tolerability characteristics of succinic acid tablets when used alone and in combination with fluvoxamine in healthy adult Chinese subjects; (2) To evaluate the safety and tolerability characteristics of succinic acid tablets when used alone and in combination with rifampicin in healthy adult Chinese subjects.

Start Date26 Sep 2022

Sponsor / Collaborator

Changchun Huayang High-Tech Co., Ltd.

[+1]

CTR20202210

/ CompletedPhase 1

[14C]琥珀八氢氨吖啶在中国成年男性健康志愿者体内吸收、代谢和排泄临床试验——[14C]琥珀八氢氨吖啶人体物质平衡与生物转化研究临床试验

[Translation] Clinical trial on the absorption, metabolism and excretion of [14C] succinic octahydroaminoacridine in healthy adult male volunteers in China——Clinical trial on the material balance and biotransformation of [14C] succinic octahydroaminoacridine in humans

主要目的：评价中国男性健康志愿者单次口服[14C]琥珀八氢氨吖啶的物质平衡及生物转化途径。次要目的：评价琥珀八氢氨吖啶在人体内的药代动力学整体特征及安全性。

[Translation]

Primary objective: To evaluate the material balance and biotransformation pathway of [14C] succinic acid octahydrogenacridine after a single oral administration in healthy Chinese male volunteers. Secondary objective: To evaluate the overall pharmacokinetic characteristics and safety of succinic acid octahydrogenacridine in humans.

Start Date23 Nov 2020

Sponsor / Collaborator

Changchun Huayang High-Tech Co., Ltd.

[+1]

100 Clinical Results associated with BChE x AChE

100 Translational Medicine associated with BChE x AChE

0 Patents (Medical) associated with BChE x AChE

4,122

Literatures (Medical) associated with BChE x AChE

01 Apr 2025·Talanta

A new near-infrared fluorescence probe for highly selective and sensitive detection and imaging of Butyrylcholinesterase in Alzheimer's disease mice

Article

Author: Zhang, Jian ; He, Xiaowei ; Tang, Xiaojie ; Li, Zhao ; Qi, Honglan

Butylcholinesterase (BChE) is a key enzyme in living system, closely related to liver and neurological diseases. It is very challenge to develop near-infrared (NIR) fluorescence probe methods for highly selective and sensitive detection of BChE in vivo. Based on the differences in active sites and spatial pockets between acetylcholinesterase (AChE) and BChE, a new NIR BChE-responsive fluorescence probe Probe-BChE (λ_ex/λ_em = 600 nm/676 nm) was designed and synthesized by introducing dimethyl carbamate group as recognizing moiety to a NIR fluorophore hemicyanine skeleton. It was found that Probe-BChE specifically binds with BChE, rather than AChE, since BChE has a big cavity and strong intermolecular forces with Probe-BChE, which was supported by the molecular docking scores. The fluorescence method for the determination of BChE was developed with a detection limit of 0.14 U/mL BChE and high selectivity as well as short reaction time (∼3 s). The fluorescence imaging method using Probe-BChE efficiently image the levels of endogenous BChE in brains and main organs (heart, liver, spleen, lung and kidney) of Alzheimer's disease (AD) mice. The results reveal that the levels of endogenous BChE in old AD mice is higher than that in young AD mice, and endogenous BChE is enriched in the liver of AD mice. This work demonstrates that Probe-BChE is a promising fluorescence probe for imaging of endogenous BChE in AD mice. The design of NIR fluorescence probes for endogenous BChE in this work will promote to design NIR fluorescence probes for endogenous cholinesterase.

01 Mar 2025·Food Chemistry

Carob (Ceratonia siliqua) leaves: A comprehensive analysis of bioactive profile and health-promoting potential of an untapped resource

Article

Author: Tardugno, Roberta ; Fiore, Donatella ; Serio, Simona ; Piccinelli, Anna Lisa ; Corbo, Filomena ; Santoro, Valentina ; Proto, Maria Chiara ; Clodoveo, Maria Lisa ; Celano, Rita ; Rastrelli, Luca

Carob is a resilient plant with ecological and nutritional significance. A comprehensive study of Ceratonia siliqua leaves (CSL) was conducted to explore its chemical composition and health-promoting potential, aiming at improving the carob-crop sustainability through valorization of this untapped co-product. UHPLC-DAD-HRMS/MS quali-quantitative profiling of CSL revealed high levels of n-galloylated glucoses (129-196 mg g^-1) and flavonol-glycosides (36-42 mg g^-1), with siliquapyranone (39-56 mg g^-1), 1,2,3,6-tetragalloylglusose (47-69 mg g^-1) and myricitrin (27-33 mg g^-1) as main markers. Highest bioactive content and antioxidant capacity (5.0 and 3.1 TEAC) was obtained during pods harvesting. Besides significant antioxidant potential, CSL exhibited strong-high inhibitory activity against α-glucosidase, acetylcholinesterase and butyrylcholinesterase (IC₅₀, 0.51, 13.5 and 58.0 μg mL^-1, respectively). 1,2,3,6-tetragalloylglusose and siliquapyranone are the main contributors to antioxidant and α-glucosidase inhibitory capacities. Excellent ability of extract and 1,2,3,6-tetragalloylglusose (IC₅₀, 0.05 μM) in selectively inhibiting α-glucosidase, make them promising candidates to manage hyperglycemia with fewer side effects.

11 Feb 2025·Journal of Biomolecular Structure and Dynamics

New 1,2,3-triazoles and their oxime derivatives: AChE/BChE enzyme inhibitory and DNA binding properties

Article

Author: Kose, Aysegul ; Kose, Muhammet ; Gungor, Ozge ; Veziroglu, Yunus Emre ; Gungor, Seyit Ali

1,2,3-Triazole compounds (1a-3a) and their oxime derivatives (1b-3b) were synthesized. The structures of these synthesized compounds were characterized using common spectroscopic methods. Crystal structures of the compounds 3, 2b and 3b were determined by single crystal X-ray diffraction studies. The acetylcholinesteras (AChE) and butyrylcholinesterase (BChE) cholinesterase inhibitor (ChEI) and DNA/calf serum albumin (BSA) binding properties of the compounds were examined. DNA binding studies have shown that compounds interact with DNA through 1,2,3-triazole and oxime groups. When the binding constant K_b values were compared, it was revealed that compound 3b (K_b = 4.6 × 10⁵ M^-1) with oxime in its structure binds more strongly than the others. In addition, in vitro BSA binding studies showed that compounds 1b and 3b exhibited higher binding affinity. These results confirm that the quenching is due to the formation of a compound resulting from the static quenching mechanism, rather than being initiated by a dynamic mechanism. Likewise, when the enzyme activity of the compounds was examined, the compounds exhibited high inhibitory activity against AChE. The highest activity was observed for compounds 2b and 3b (8.6 ± 0.05 and 4.8 ± 0.052 µM). It was observed that the compounds were not selective with respect to BChE. Communicated by Ramaswamy H. Sarma.

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