Article
Biochemistry & Molecular Biology
Julia Lisa-Molina, Pedro Gomez-Murillo, Irene Arellano-Martin, Carles Jimenez, Maria L. Rodriguez-Escobar, Luciana R. Tallini, Francesc Viladomat, Laura Torras-Claveria, Jaume Bastida
Summary: Amaryllidaceae alkaloids, found in Narcissus species, have medicinal properties and potential for treating cholinergic disorders like Alzheimer's disease. The production of galanthamine, an Amaryllidaceae alkaloid used in AD treatment, is insufficient to meet the demand. This study aims to improve galanthamine production and explore new drugs for AD treatment. Additionally, the alkaloid content and AChE inhibitory activity of less-studied autumn-flowering Narcissus species were evaluated.
Article
Agriculture, Multidisciplinary
Nancy D. Asen, Chibuike C. Udenigwe, Rotimi E. Aluko
Summary: The aim of this study was to determine the structural requirements for peptides that inhibit acetylcholinesterase and butyrylcholinesterase activities. A dataset of 19 oligopeptides identified through mass spectrometry was used to analyze the structure-function relationship. The study found that the most active peptides had specific amino acid combinations at specific positions.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Dentistry, Oral Surgery & Medicine
Mu-Yeol Cho, Eun-Song Lee, Hoi-In Jung, Baek-Il Kim
Summary: The study successfully solubilized Curcuma xanthorrhiza oil using nanoemulsification and demonstrated that the nanoemulsion form had superior anti-biofilm effects compared to the emulsion form.
JOURNAL OF DENTISTRY
(2023)
Article
Biochemistry & Molecular Biology
Joanna Grzelczyk, Ilona Galazka-Czarnecka, Joanna Oracz
Summary: This study evaluated the nutrient composition, including fat, total phenolic compounds, vitamins, and antioxidant properties, of four species of freeze-dried edible insects (Alphitobius diaperinus Panzer, Gryllus campestris, Tenebrio molitor, Chorthippus biguttulus) and their potential inhibitory effect on acetylcholinesterase (AChE). The study also aimed to obtain olive oil enriched with edible insects, which showed high affinity to AChE and increased levels of vitamin C and B vitamins.
Article
Biochemistry & Molecular Biology
Leticia B. Silva, Pablo A. Nogara, Paula T. Halmenschelager, Jessica C. Alvim, Fernanda D'A. Silva, Sarah C. Feitosa, Joao B. T. Rocha, Marcos A. P. Martins, Nilo Zanatta, Helio G. Bonacorso
Summary: Five new spirochromeno-quinolines were synthesized using a sequential one-pot two-step cyclocondensation reaction with cyclopentane, cyclohexane, and cycloheptane. The molecule with a spirocyclopentane derivative showed the highest AChE and BChE inhibitory activity. Non-halogenated compounds were found to be better inhibitors of AChE and BChE compared to halogenated molecules. Their inhibitory potency was weaker than that of tacrine, possibly due to the size of the spirocarbocyclic moieties hindering the interaction with cholinesterases. These findings may contribute to the development of new anticholinesterase drugs.
BIOORGANIC CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Ashwani Arya, Rubal Chahal, Rekha Rao, Md. Habibur Rahman, Deepak Kaushik, Muhammad Furqan Akhtar, Ammara Saleem, Shaden M. A. Khalifa, Hesham R. El-Seedi, Mohamed Kamel, Ghadeer M. Albadrani, Mohamed M. Abdel-Daim, Vineet Mittal
Summary: Alzheimer's disease is a gradually growing irreversible illness of the brain that affects a large population worldwide, with potential treatment options involving inhibitors of acetylcholine (ACh) to improve cholinergic transmission.
Article
Chemistry, Medicinal
Xin Wang, Tao Zhang, Xiaochen Chen, Yating Xu, Zhipeng Li, Yuanfan Yang, Xiping Du, Zedong Jiang, Hui Ni
Summary: All-trans astaxanthin, derived mainly from marine organisms, showed a strong inhibitory effect on acetylcholinesterase and oxidative stress. It acted as a reversible competitive inhibitor with a half inhibitory concentration (IC50 value) of 8.64 mu mol/L. Additionally, all-trans astaxanthin reduced oxidative stress by decreasing malondialdehyde content and increasing the activity of superoxide dismutase and catalase. It also induced changes in the secondary structure of acetylcholinesterase to reduce its activity. Molecular-docking analysis revealed that all-trans astaxanthin prevented substrate binding to acetylcholinesterase by occupying the active pocket space.
Article
Plant Sciences
Adelina Simamora, Kris Herawan Timotius, Mukerrem Betul Yerer, Heri Setiawan, Abdul Mun'im
Summary: Xanthorrhizol (XTZ), a bisabolene sesquiterpenoid, has anticancer activities and multiple pharmacological effects. Studies have shown that XTZ has preventive and therapeutic effects against various types of cancer, and it inhibits the growth and metastasis of cancer cells by regulating multiple signaling pathways.
Article
Chemistry, Applied
Zekeriya Biyiklioglu, Huseyin BaS, Huseyin Sahin
Summary: In this study, axially pyridine groups substituted silicon (IV) phthalocyanines and their water soluble derivatives showed various degrees of acetylcholinesterase inhibition activity, indicating their potential as effective agents against Alzheimer's disease.
APPLIED ORGANOMETALLIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Nguyen Manh Cuong, Pham Ngoc Khanh, Le Thi Hong Nhung, Nguyen Xuan Ha, Tran Thu Huong, Katarina Bauerova, Young Ho Kim, Do Dinh Tung, Trinh Thi Thuy, Nguyen Thi Hoang Anh
Summary: From the root bark of Pinus krempfii Lecomte, four flavonoids were isolated and evaluated for their inhibitory activities against AChE and BChE enzymes in vitro and in silico. Tectochrysin (1) showed the highest inhibition activity against AChE and formed stable complexes with the protein. Galangin (2) exhibited significant inhibitory activity against BChE and formed hydrogen bonds with the protein. The study provided new insights for drug discovery and the development of neuroprotective substances for Alzheimer's disease treatment.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Anastasiya V. Petrova, Oxana B. Kazakova, Ivan S. Nazarov, Rene Csuk, Niels V. Heise
Summary: A series of new lupane, ursane, and oleanane type triterpenic A-seco-derivatives containing various functional groups have been synthesized and evaluated for their acetylcholinesterase inhibitory activities. The results showed that the bromo- and azido-derivatives of 28-oxo-allobetuline and betulinic acid exhibited the most potent inhibitory activity against AChE. Further experiments demonstrated the cyano-derivatives of betulinic acid as mixed-type inhibitors with low Ki values.
CHEMISTRY & BIODIVERSITY
(2023)
Article
Chemistry, Medicinal
Khan Viet Nguyen, Thu Oanh Thi Nguyen, Duc Viet Ho, Jyrki Heinamaki, Ain Raal, Hoai Thi Nguyen
Summary: Limited knowledge on the bioactivity of Alphonsea tonkinensis A.DC was observed. In vitro acetylcholinesterase inhibitory and antioxidant activities of extracts and pure compounds isolated from stems and leaves were investigated. Various extracts showed potential inhibitory and antioxidant activities, marking the first study to reveal such bioactivities of A. tonkinensis.
NATURAL PRODUCT COMMUNICATIONS
(2021)
Article
Biochemistry & Molecular Biology
Marlon P. Almeida, Flavio V. C. Kock, Hugo C. R. de Jesus, Rose M. Carlos, Tiago Venancio
Summary: Currently, commercially available anti-Alzheimer drugs are all acetylcholinesterase (AChE) inhibitors, which have dose-dependent effects lasting for no longer than two years. Researchers have synthesized a novel AChE inhibitor, RuEtPy, with high inhibitory activity and competitive mechanism, and identified the key role of the 4,2-Ethylamino-pyridine motif in the inhibitory action through NMR binding-target studies.
JOURNAL OF INORGANIC BIOCHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Linh Thuy Khanh Nguyen, Phu Quynh Dinh Nguyen, Chau Bao Hoai Nguyen, Hoai Thi Nguyen, Thi Van Anh Tran, Thanh-Tan Mai, Thai-Son Tran, Duc Viet Ho
Summary: This study evaluated the acetylcholinesterase inhibitory activities of sesquiterpenoids from the rhizomes of Homalomena pendula, and found that teucmosin exhibited significant anti-cholinesterase activity, along with good pharmacokinetic properties on common targets in Alzheimer's disease (AD).
Article
Plant Sciences
Jin-Bu Xu, Shi-Xing Miao, Feng Gao, Lin-Xi Wan
Summary: A series of arylated huperzine A derivatives were efficiently synthesized through late-stage modification of huperzine A using the Suzuki-Miyaura cross-coupling reaction. The acetylcholinesterase inhibitory activity of the synthesized compounds was evaluated, and it was found that introducing aryl groups at the C-1 position resulted in unsatisfactory activity. The study highlights the importance of the pyridone carbonyl group for maintaining the anti-acetylcholinesterase potency of huperzine A.
JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH
(2023)
Article
Plant Sciences
Yi Zhu, Junlin Wang, Lu Tang, Yuxin Shang, Weiyi Zhao, Wei Zhang, Ping Hai, Yongbiao Zheng, Wenbo Li, Yanfang Su
Summary: One new iridoid glucoside and two new lignan glycosides, along with three known compounds, were isolated from the whole plants of Lancea tibetica. The structures were determined by spectroscopic methods and X-ray crystallographic analysis. One of the new iridoid glucosides and the known compounds exhibited moderate antioxidant activity.
PHYTOCHEMISTRY LETTERS
(2024)
Article
Plant Sciences
Yi Deng, Minghua Chen, Junming Yi, Yuguo Zheng
Summary: This study successfully designed and synthesized a series of quinazolinone derivatives containing purine molecules, and found that some compounds exhibited strong antiviral activity against tobacco mosaic virus. The findings have important implications for further development of antiviral drugs.
PHYTOCHEMISTRY LETTERS
(2024)
