Novel Caspase-1 inhibitor CZL80 improves neurological function in mice after progressive ischemic stroke within a long therapeutic time-window.

Progressive ischemic stroke (PIS) is featured by progressive neurological dysfunction after ischemia. Ischemia-evoked neuroinflammation is implicated in the progressive brain injury after cerebral ischemia, while Caspase-1, an active component of inflammasome, exaggerates ischemic brain injury. Current Caspase-1 inhibitors are inadequate in safety and druggability.

Melatonin receptor agonist ramelteon attenuates mouse acute and chronic ischemic brain injury.

Melatonin receptors (MTs) are potential drug targets for stroke therapy. Ramelteon is a selective melatonin receptor agonist used to treat insomnia. In this study we investigated whether ramelteon could attenuate cerebral ischemia in mice.

Urolithin A-activated autophagy but not mitophagy protects against ischemic neuronal injury by inhibiting ER stress in vitro and in vivo.

Aim: Mitochondrial autophagy (mitophagy) clears damaged mitochondria and attenuates ischemic neuronal injury. Urolithin A (Uro-A) activates mitophagy in mammal cells and Caenorhabditis elegans. We explored neuroprotection of Uro-A against ischemic neuronal injury.

Predictive value of thrombospondin-1 for outcomes in patients with acute ischemic stroke.

Background: Thrombospondin-1 is a potent regulator of angiogenesis. The expression of cerebral thrombospondin-1 is promoted in a rat model of intracerebral hemorrhage. The current study was designed to investigate the change of plasma thrombospondin-1 concentrations and assess the prognostic value of plasma thrombospondin-1 concentrations for long-term mortality and functional outcome of ischemic stroke patients.

Prognostic value of neuropeptide proenkephalin A in patients with severe traumatic brain injury.

High plasma proenkephalin A levels have been associated with poor clinical outcome of aneurysmal subarachnoid hemorrhage. This prospective observatory study was designed to investigate the relationship between plasma proenkephalin A levels and 1-week mortality, 6-month mortality and 6-month unfavorable outcome (defined as Glasgow Outcome Scale score of 1-3) in patients with severe traumatic brain injury. This study recruited 128 patients and 128 sex- and age-matched healthy controls.

Cytotoxic triterpenoid saponins from Vaccaria segetalis.

By the guidance of bioassay, one new cytotoxic triterpenoid saponin, 3-O-[beta-D-galactopyranosyl-(1-->2)-beta-D-glucuronopyranosyl] quillaic acid 28-O-beta-D-glucopyranosyl-(1-->3)-beta-D-xylopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-(1-->2)-[beta-D-fucopyranosyl-(1-->4)]-beta-D-fucopyranoside (1), and five known cytotoxic triterpenoid saponins, vaccaroside E (2), vaccaroside G (3), vaccaroside B (4), segetoside H (5) and segetoside I (6), were isolated from Vaccaria segetalis. Their structures were established on the basis of ESI-MS, IR, extensive NMR ((1)H NMR, (13)C NMR, TOCSY, (1)H-(1)H COSY, DEPT, HMQC, HMBC and ROESY) analyses, chemical degradation, and by comparing with previously reported data. Compounds 1-6 showed moderate cytotoxic activities against LNcap, P-388 and A-549 cell lines with IC(50) values in the range 0.

Semisynthesis and antitumor activities of new styryl-lactone derivatives.

Nineteen new derivatives of the naturally occurring compound, goniothalamin, were prepared by chemical modification and semi-synthetic methods. The antitumor activities of these derivatives and goniothalamin were evaluated in vitro against human tumor cell lines, and most of them showed an inhibitory effect against HL-60 cancer cells. The derivatives 10-nitro-goniothalamin and 10-amino-goniothalamin gave selective inhibition concentration (IC50) of 1.

Constituents from the stems of Goniothalamus griffithii.

A new cyclopeptide, grifficyclocin A (1), and a new aporphine alkaloid, griffinin (2) were isolated together with two known styryllactones from the stems of Goniothalamus griffithii. Their structures were identified spectroscopically and chemically. Among them, the griffinin (2) was isolated as the enol form in two tautomers, and the two known styryllactones, goniothalamin (3) and 8- O-acetylgoniotriol (4), showed selective in vitro antitumor activities.