Anti-BACE1 and anti-AchE activities of undescribed spiro-dioxolane-containing meroterpenoids from the endophytic fungus Aspergillus terreus Thom

Publication date: September 2019Source: Phytochemistry, Volume 165Author(s): Changxing Qi, Qun Zhou, Weixi Gao, Mengting Liu, Chunmei Chen, Xiao-Nian Li, Yongji Lai, Yuan Zhou, Dongyan Li, Zhengxi Hu, Hucheng Zhu, Yonghui ZhangAbstractSpiroterreusnoids A–F, six undescribed spiro-dioxolane-containing adducts bearing 3,5-dimethylorsellinic acid-based meroterpenoid and 2,3-butanediol moieties were isolated from the endophytic fungus Aspergillus terreus Thom from Tripterygium wilfordii Hook. f. (Celastraceae). The structures of these adducts were established by spectroscopy, single-crystal X-ray diffraction, and experimental electronic circular dichroism (ECD) measurements. Spiroterreusnoids A–F represent the first examples of adducts composed of 3,5-dimethylorsellinic acid-based meroterpenoids. It is noteworthy that spiroterreusnoids A–F possessing a spiro-dioxolane moiety exhibited potential abilities in inhibiting BACE1 (IC50 values ranging from 5.86 to 27.16 μM) and AchE (IC50 values ranging from 22.18 to 32.51 μM), while the other analogues without this fragment displayed no such activities. Taken together, spiroterreusnoids A–F represent the first multitargeted natural adducts that could inhibit BACE1 and AchE, and might provide a new template for the development of new anti-Alzheimer's disease drugs.Graphical abstract
Source: Phytochemistry - Category: Chemistry Source Type: research

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Conclusions: Although persons with AD are often collectively considered as expensive patient group, there is large temporal and inter-individual variation in belonging to the highest decile of hospitalization and/or medication costs. It would be important to assess whether hospitalization rate could be decreased by, e.g., comprehensive outpatient care with more efficient management of comorbidities. In addition, other interventions that could decrease hospitalization rate in persons with dementia should be studied further in this context. Key messages Persons with AD had large individual fluctuation in hospital care costs ...
Source: Annals of Medicine - Category: Internal Medicine Tags: Ann Med Source Type: research
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Source: AARP.org News - Category: American Health Source Type: news
Skip to content ... Un paso m ás hacia un análisis de sangre para detectar la enfermedad de Alzheimer ... El prototipo es prometedor para la detección de proteínas que atacan las neuronas. ... por: ...
Source: AARP.org News - Category: American Health Source Type: news
Authors: Candido S, Lupo G, Pennisi M, Basile MS, Anfuso CD, Petralia MC, Gattuso G, Vivarelli S, Spandidos DA, Libra M, Falzone L Abstract There is recent evidence to indicate the existence of an inverse association between the incidence of neurological disorders and cancer development. Concurrently, the transcriptional pathways responsible for the onset of glioblastoma multiforme (GBM) and Alzheimer's disease (AD) have been found to be mutually exclusive between the two pathologies. Despite advancements being made concerning the knowledge of the molecular mechanisms responsible for the development of GB...
Source: Oncology Reports - Category: Cancer & Oncology Tags: Oncol Rep Source Type: research
Protective effect of ISO‑1 against advanced glycation end product aggravation of PC12 cell injury induced by Aβ1‑40. Mol Med Rep. 2019 Jul 09;: Authors: Yu M, Zang D, Xu Y, Meng J, Qian S Abstract Advanced glycation end products (AGEs) are important pathogenic substances involved in diabetes mellitus (DM) and its complications. AGEs also serve important roles in promoting the development of Alzheimer's disease (AD). Macrophage migration inhibitory factor (MIF), an inflammatory stimulant and a pathogenic factor involved in DM, was previously reported to be present at increased levels in the cer...
Source: Molecular Medicine Reports - Category: Molecular Biology Tags: Mol Med Rep Source Type: research
Authors: Wu W, Du S, Shi W, Liu Y, Hu Y, Xie Z, Yao X, Liu Z, Ma W, Xu L, Ma C, Zhong Y Abstract Accelerated forgetting has been identified as a feature of Alzheimer's disease (AD), but the therapeutic efficacy of the manipulation of biological mechanisms of forgetting has not been assessed in AD animal models. Ras-related C3 botulinum toxin substrate 1 (Rac1), a small GTPase, has been shown to regulate active forgetting in Drosophila and mice. Here, we showed that Rac1 activity is aberrantly elevated in the hippocampal tissues of AD patients and AD animal models. Moreover, amyloid-beta 42 could induce Rac1 activat...
Source: Protein and Cell - Category: Cytology Tags: Protein Cell Source Type: research
Publication date: Available online 19 July 2019Source: Biocatalysis and Agricultural BiotechnologyAuthor(s): Hafsa Sattar, Zainab Bibi, Aysha Kamran, Afsheen Aman, Shah Ali Ul QaderAbstractSerine metalloproteases have substantial scientific interest due to their unique physicochemical properties and capability to degrade complex casein polymer. In this contemporary study, the production of protease was enhanced by optimizing various physicochemical parameters and one-variable at a time approach used under submerged fermentation conditions. Among four different previously isolated Aspergillus species, Aspergillus niger KIBG...
Source: Biocatalysis and Agricultural Biotechnology - Category: Biotechnology Source Type: research
This study explores the effectiveness of thymol blue for the first time together with supramolecular solvent to develop green supramolecular solvent liquid–phase microextraction method to preconcentrate and separate of trace amount of Aluminum (III) in real samples.Graphical abstractThe procedure of the supramolecular solvent liquid–phase microextraction technique.
Source: Microchemical Journal - Category: Chemistry Source Type: research
Wei-Zhong Liu Three new γ-hydroxyl butenolides (1–3), a pair of new enantiomeric spiro-butenolides (4a and 4b), a pair of enantiomeric cyclopentenones (5a new and 5b new natural), and six known compounds (6–11), were isolated from Aspergillus sclerotiorum. Their structures were established by spectroscopic data and electronic circular dichroism (ECD) spectra. Two pairs of enantiomers [(+)/(–)-6c and (+)/(–)-6d] obtained from the reaction of 6 with acetyl chloride (AcCl) confirmed that 6 was a mixture of two pairs of enantiomers. In addition, the X-ray data confirmed tha...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research
Conclusions In conclusion, articles in this Research Topic made a very significant contribution to our understanding of the role played by environmental factors, dysbiotic conditions, and infections in triggering diseases. Since this is a rapidly expanding area of research, many other factors contributing to the onset of these diseases are not covered here. We are confident, however, that further studies will expand the list as well as bring a better understanding of mechanisms involved in the onset of autoimmune and autoinflammatory diseases. Author Contributions All authors listed have made a substantial, direct and i...
Source: Frontiers in Microbiology - Category: Microbiology Source Type: research
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