One new and two known dammarane-type saponins were isolated from the leaves of Gynostemma pentaphyllum using various chromatographic methods. Their structures were identified by HR-ESI-MS,~( 1)H-NMR, ~(13)C-NMR, 2 D-NMR spectra as 2α,3β,12β,20,24(S)-tetrahdroxydammar-25-en-3-O-[β-D-glucopyranosyl(1→2)-β-D-glucopyranosyl]-20-O-β-D-xylopyranosyl(1→6)-β-D-glucopyranoside(1, a new compound, namely gypenoside J5) and 2α,3β,12β,20,24(R)-tetrahdroxydammar-25-en-3-O-[β-D-glucopyranosyl(1→2)-β-D-glucopyranosyl]-20-O-β-D-xylopyranosyl(1→6)-β-D-glucopyranoside(2) and 2α,3β,12β,20-tetrahydroxy-25-hydroperoxy-dammar-23-en-3-O-[β-D-glucopyranosyl(1→2)][β-D-glucopyranosyl]-20-O-[β-D-xylopyranosyl(1→6)]-β-D-glucopy-ranoside(3), respectively. Compounds 1 and 2 were a pair of C-24 epimers. All compounds showed weak cytotoxicity agxinst H1299, HepG2, PC-3, SH-SY5 Y cancer cell lines. However, they exerted protective effect against SH-SY5 Y cellular damage induced by H_2O_2 dose-dependently, of which compound 1 displayed the strongest antioxidant effect. The present study suggested that G. pentaphyllum has antioxidative potential and the saponins from G. pentaphyllum are considered as the active compounds with neuroprotecitve effect.
Gynostemma ; Molecular Structure ; Neuroprotective Agents/pharmacology* ; Saponins/pharmacology* ; Triterpenes/pharmacology*

Inert gas is a group of rare gases with very low activity, their application in medical field has increasingly drawn attentions. It is known that inert gases helium, xenon and argon have protective effects on nervous system and the mechanisms are related to eradicating free radicals, anti-inflammation, suppressing apoptosis, influencing ion channels and so on. Further study on the neuroprotective effect of inert gas will shed light on a new approach to treat neurological diseases.
Argon ; pharmacology ; Helium ; pharmacology ; Neuroprotective Agents ; pharmacology ; Noble Gases ; pharmacology ; Xenon ; pharmacology

Tetrahydroisoquinoline alkaloids distributed widely in the nature and some have a broad application in clinic. More attention has been paid in recent years on this type of alkaloid, owing to the diverse range of biological activities exhibited by these alkaloids and the discovery of new functional mechanisms and molecular targets underlying these activities. This article summarized the recent advances in the biological activities and functional mechanism of tetrahydroisoquinoline, which included the activities such as antitumor, antibiotic, antivirus, anti-inflammatory, anticoagulation, bronchodilation, and the action on central nervous system, with the purpose of providing some ideas in the study of biological activity of this type of alkaloid and in the search for lead-compound and rational drug design.
Animals ; Anti-Inflammatory Agents ; pharmacology ; Anticonvulsants ; pharmacology ; Antifungal Agents ; pharmacology ; Antineoplastic Agents ; pharmacology ; Antiviral Agents ; pharmacology ; Bronchodilator Agents ; pharmacology ; Central Nervous System Agents ; pharmacology ; Fibrinolytic Agents ; pharmacology ; Humans ; Neuroprotective Agents ; pharmacology ; Tetrahydroisoquinolines ; chemical synthesis ; chemistry ; pharmacology

OBJECTIVETo investigate neuroprotection of resveratrol against cytotoxicity of oxidized low density lipoprotein (oxLDL) in PC12 cells.

METHODSPC12 cells were pretreated with resveratrol for one hour as a neuron model and then exposed to oxLDL at varied concentrations. Effects of resveratrol on cell viability, permeability of cell membrane, cell nucleus and activity of caspase-3 were evaluated with MTT assay, lactic acid dehydrogenase (LDH) release assay, DNA fragmentation (TUNEL) assay and assay for caspase-3 activity (caspase assay).

RESULTSCell viability, LDH release rate, percentage of cells with positive TUNEL and activity of caspase-3 were (62 +/- 3)%, (23 +/- 3)%, (26 +/- 5)% and (0.811 +/- 0.049) mol.min(-1).microg(-1), vs (84 +/- 7)%, (13 +/- 4)%, (12 +/- 4)% and (0.553 +/- 0.048) mol.min(-1).microg(-1) in PC12 cells treated with 10 mg/L oxLDL vs in those treated with 10 mg/L oxLDL plus 50 micromol/L resveratrol, respectively, with statistically significant difference.

CONCLUSIONResveratrol could attenuate cytotoxicity induced by oxLDL in PC12 cells with neuroprotection.

Animals ; Cell Survival ; drug effects ; Lipoproteins, LDL ; toxicity ; Neuroprotective Agents ; pharmacology ; PC12 Cells ; Rats ; Stilbenes ; pharmacology

The PK-PD correlation models by using pharmacodynamics and pharmacokinetics were applied to study the material basis of Naomaitong,a clinical empirical prescription for the treatment of cerebral apoplexy,in inhibiting the death of PC12 nerve cells induced by Na_2S_2O_4 and Glu. In this experiment,PC12 cell death models induced by Na_2S_2O_4 and Glu were established respectively.With LDH lateral leakage and NO content as pharmacodynamic indexes,PK-PD model was established by SVM algorithm to evaluate the effective components of Naomaitong in inhibiting neural cell death. The results showed that the positive correlation of emodin methyl ether-8-O-β-D-glucopyranoside,aloe emodin,chrysophanol,rhein,emodin,ginsenoside Rg1,ginsenoside Rc,3'-methoxypuerarin and ligustilide was significant,obviously improving the LDH release and NO content. The results indicated that the contribution of Radix Puerariae Lobatae Radix and Rhei Radix et Rhizoma in Naomaitong could protect the nerve cell death induced by Na_2S_2O_4 and Glu respectively. PK-PD model was used to screen the neuroprotective components in Naomaitong,revealing the possible pharmacodynamic material basis of Naomaitong in the treatment of cerebral ischemia injury.
Animals ; Drugs, Chinese Herbal ; pharmacology ; Neurons ; cytology ; Neuroprotective Agents ; pharmacology ; PC12 Cells ; Rats

Mangosteen (Garcinia mangostana Linn.) is a well-known tropical tree indigenous to Southeast Asia. Its fruit's pericarp abounds with a class of isoprenylated xanthones which are referred as mangostins. Numerous in vitro and in vivo studies have shown that mangostins and their derivatives possess diverse pharmacological activities, such as antibacterial, antifungal, antimalarial, anticarcinogenic, antiatherogenic activities as well as neuroprotective properties in Alzheimer's disease (AD). This review article provides a comprehensive review of the pharmacological activities of mangostins and their derivatives to reveal their promising utilities in the treatment of certain important diseases, mainly focusing on the discussions of the underlying molecular targets/pathways, modes of action, and relevant structure-activity relationships (SARs). Meanwhile, the pharmacokinetics (PK) profile and recent toxicological studies of mangostins are also described for further druggability exploration in the future.
Animals ; Anti-Infective Agents ; pharmacology ; Anticarcinogenic Agents ; pharmacology ; Antineoplastic Agents, Phytogenic ; pharmacology ; Antioxidants ; pharmacology ; Cardiovascular Agents ; pharmacology ; Fruit ; chemistry ; Garcinia mangostana ; chemistry ; Humans ; Neuroprotective Agents ; pharmacology ; Phytotherapy ; Plant Extracts ; pharmacology ; Protective Agents ; pharmacology ; Xanthones ; pharmacology

OBJECTIVETo review the recent research progress in pharmacological actions and mechanisms of ginkgolide B. Data sources Information included in this article was identified by searching of PUBMED (1987 - 2006) online resources using the key terms "ginkgolide B", "platelet activating factor", and "pharmacological". Study selection Mainly original milestone articles and critical reviews written by major pioneer investigators of the field were selected.

RESULTSThe key issues related to the pharmacological actions and mechanisms of ginkgolide B were summarized. The ginkgolide B possesses a number of beneficial effects such as anti-inflammatory, anti-allergic, antioxidant, and neuroprotective effects. Meantime, their mechaniams were discussed.

CONCLUSIONSThe Ginkgolide B is the most potent antagonist of platelet activating factor (PAF) and exhibits therapeutic action in a variety of diseases mainly by the PAF receptor.

Acute Disease ; Animals ; Anti-Asthmatic Agents ; pharmacology ; Antineoplastic Agents ; pharmacology ; Ginkgolides ; chemistry ; pharmacology ; Humans ; Lactones ; chemistry ; pharmacology ; Neuroprotective Agents ; pharmacology ; Pancreatitis ; drug therapy ; Reperfusion Injury ; prevention & control

Liriope (Liliaceae) species have been used as folk medicines in Asian countries since ancient times. From Liriope plants (8 species), a total of 132 compounds (except polysaccharides) have been isolated and identified, including steroidal saponins, flavonoids, phenols, and eudesmane sesquiterpenoids. The crude extracts or monomeric compounds from this genus have been shown to exhibit anti-tumor, anti-diabetic, anti-inflammatory, and neuroprotective activities. The present review summarizes the results on phytochemical and biological studies on Liriope plants. The chemotaxonomy of this genus is also discussed.
Animals ; Anti-Inflammatory Agents ; pharmacology ; Antineoplastic Agents, Phytogenic ; pharmacology ; Flavonoids ; pharmacology ; Humans ; Hypoglycemic Agents ; pharmacology ; Liriope Plant ; chemistry ; Medicine, Traditional ; Neuroprotective Agents ; pharmacology ; Phenols ; pharmacology ; Phytotherapy ; Plant Extracts ; pharmacology ; Saponins ; pharmacology ; Sesquiterpenes ; pharmacology

In this paper, Xixian Tongshuan Preparation was used as the research object, and all the chemical components of the 13 traditional Chinese medicines were collected. The target finding technique was used to obtain the key targets of the neuroprotective effect of Xixian Tongshuan Preparation, including 5 glutamate receptors, TGFR-1 and VEGFR-2. Molecular docking technology was used to screen out the potential active components of the above targets and to analyze their mechanism of action. It was found that single component, such as neo-complanatoside and neo-carthamin, in Xixian Tongshuan Preparation could simultaneously act on different targets. The chemical constituents in Ligusticum chuanxiong, Angelica sinensis, Carthamus tinctorius, and Panax pseudo-ginseng could simultaneously act on different neuroprotective-related targets, which reflected the application of multi-components to multi-targets. Point and multiple sites played a key role in protecting neurons against cerebral ischemic injury. This study explains the multi-target mechanism of anti-cerebral ischemic injury in neuroprotection at the molecular level, and provides a certain direction for the clinical application and experimental research of Xixian Tongshuan Preparation.
Brain Ischemia ; Cerebral Infarction ; Drugs, Chinese Herbal ; pharmacology ; Humans ; Molecular Docking Simulation ; Neuroprotective Agents ; pharmacology ; Phytochemicals ; pharmacology

Apoptosis ; Humans ; Nerve Regeneration ; Neuroprotective Agents ; pharmacology ; Retinal Ganglion Cells ; drug effects ; physiology ; Stem Cell Transplantation