Rational design synthesis and evaluation of a novel near-infrared fluorescent probe for selective imaging of amyloid-β aggregates in Alzheimer's disease.

Alzheimer's disease (AD) is a degenerative neurological disorder that remains incurable to date, seriously affecting the quality of life and health of those affected. One of the key neuropathological hallmarks of AD is the formation of amyloid-β (Aβ) plaques. Near-infrared (NIR) probes that possess a large Stokes shift show great potential for imaging of Aβ plaques in vivo and in vitro.

Novel dual-target FAAH and TRPV1 ligands as potential pharmacotherapeutics for pain management.

Dual-acting drugs that simultaneously inhibit fatty acid amide hydrolase (FAAH) and antagonize the transient receptor potential vanilloid 1 (TRPV1) is a promising stronger therapeutic approach for pain management without side effects associated with single-target agents. Here, several series of dual FAAH/TRPV1 blockers were designed and synthesized through rational molecular hybridization between the pharmacophore of classical TRPV1 antagonists and FAAH inhibitors. The studies resulted in compound 2r, which exhibited strong dual FAAH/TRPV1 inhibition/antagonism in vitro, exerted powerful analgesic effects in formalin-induced pain test (phase II, in mice), desirable anti-inflammatory activity in carrageenan-induced paw edema in rats, no TRPV1-related hyperthermia side effect, and favorable pharmacokinetic properties.

Design, synthesis and biological evaluation of small molecule fluorescent probes targeting EGFR for tumor detection and treatment.

The epidermal growth factor receptor (EGFR) is a tyrosine kinase receptor that plays a crucial role in cell differentiation and tumor progression, and its overexpression is closely associated with the development and metastasis of multiple cancers. The development of a fluorescent probe capable of targeting EGFR while simultaneously integrating diagnostic and therapeutic functions could have a profound impact on the treatment of related cancers. In this study, we developed a series of EGFR-targeting probes that consisted of an environment-sensitive 1,8-naphthalimide fluorophore, a linker unit and a targeting unit (gefitinib), using a coupling strategy.

[Effects of berberine on LPS /NF-κB and MAPK signaling pathways in PCOS model rats].

To investigate the effects of berberine on glucose and lipid metabolism, sex hormone binding protein, adiponectin (LPS), NF-κB and MAPK signaling pathways in polycystic ovary syndrome (PCOS) model rats. Female SD rats were randomly divided into control group, PCOS model group, berberine (0.216 g/kg) group, metformin (0.

Chromone Derivatives with α-Glucosidase Inhibitory Activity from the Marine Fungus Maire.

The fungal strain YPGA3 was isolated from the sediments of the Yap Trench and identified as . Eight new chromone derivatives, named penithochromones M-T (-), along with two known analogues, and were isolated from the strain. The structures were established by detailed analyses of the spectroscopic data.

Antioxidant constituents of chrysanthemum 'jinsidaju' cultivated in Kaifeng.

Dendranthema morifolium cv. 'jinsidaju', cultivated only in Kaifeng, has been eaten for more than 1000 years. During the antioxidant-activity-guided studies on its chemistry and health care function, two new bisabolane-type sesquiterpenes, (6R,7R)-7-hydroxybisabol-2,9E,11-triene-4-one (jinsidajuol A, 1) and (6R,7R)-7-hydroxy-11-methoxybisabol-2,9E-diene-4-one (jinsidajuol B, 2), and thirteen known compounds (3-15) were isolated from the flowers.

Chemical constituents from Inonotus obliquus and their antitumor activities.

Four new lanostane-type triterpenes (inonotusanes D-G, 1-4), including a 24,25,26,27-tetranorlanostane, together with 11 known compounds (5-15), including 7 lanostane derivatives, 2 steroids and 2 aromatic compounds, were isolated from the sclerotia of Inonotus obliquus. Their structures were elucidated by 1D and 2D NMR spectroscopy and HRMS. To our knowledge, 1 is the first 24,25,26,27-tetranorlanostane-type triterpenoid from fungus, and this is the first time that 31-member lanostane-type triterpenes, 5 and 6, have been isolated from the sclerotia of I.

Triterpenoids from Inonotus obliquus and their antitumor activities.

Three new lanostane-type triterpenes, inonotusanes A-C (1-3), and a new naturally occurring one, 3β-hydroxy-25,26,27-trinorlanosta-8,22E-dien-24-oic acid (4), together with sixteen known triterpenoids (5-20), including 13 lanostane derivatives, 2 lupanes and 1 oleanane-type triterpene were isolated from the sclerotia of Inonotus obliquus. Their structures were elucidated by 1D and 2D NMR spectroscopy and HRMS. Compounds 6, 8, 18 and 20 exhibited strong cytotoxicity against A549 tumor cell lines, with IC50 values of 2.

[Triterpenoids from Inonotus obliquus protect mice against oxidative damage induced by CCl4].

To investigate the effects of lanosterol (1), inotodiol (2) and trametenolic acid (3) from Inonotus obliquus against oxidative damage induced by CCl4 in mice, 1, 2 and 3 (20, 10 and 5 mg x kg(-1)) were respectively administered to mice, once a day for 3 days. Then the mice were induced to oxidative damage by CCl4 on the third day 30 min after the administration. The activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-PX) and the content of malondialdehyde (MDA) and reductive glutathione (GSH) in serum and liver homogenate were determined.

WITHDRAWN: Jolkinolide B-induced mitochondria-dependent apoptosis in K562 cells.

This article has been withdrawn consistent with Elsevier Policy on Article Withdrawal (http://www.elsevier.com/locate/withdrawalpolicy).