In vivo and in vitro evaluation of erianin, a novel anti-angiogenic agent.

This study evaluated the anti-angiogenic activities of erianin in vivo and in vitro. Erianin, a natural product from Dendrobium chrysotoxum, caused moderate growth delay in xenografted human hepatoma Bel7402 and melanoma A375 and induced significant vascular shutdown within 4 h of administering 100 mg/kg of the drug. Erianin also displayed potent anti-angiogenic activities in vitro: it abrogated spontaneous or basic fibroblast growth factor-induced neovascularisation in chick embryo; it inhibited proliferation of human umbilical vein endothelial cells (EC(50) 34.1+/-12.7 nM), disrupted endothelial tube formation, and abolished migration across collagen and adhesion to fibronectin. Erianin also exerted selective inhibition toward endothelial cells, and quiescent endothelium showed more resistance than in proliferative and tumour conditions. In a cytoskeletal study, erianin depolymerised both F-actin and beta-tubulin, more significantly in proliferating endothelial cells than in confluent cells. In conclusion, erianin caused extensive tumour necrosis, growth delay and rapid vascular shutdown in hepatoma and melanoma models; it inhibited angiogenesis in vivo and in vitro and induced endothelial cytoskeletal disorganisation. These findings suggest that erianin has the therapeutic potential to inhibit angiogenesis in vivo and in vitro.

Astragaloside IV and polysaccharide production by hairy roots of Astragalus membranaceus in bioreactors.

Hairy roots of Astragalus membranaceus were grown in bioreactors up to 30 l for 20 d. Cultures from a 30 l airlift bioreactor gave 11.5 g l dry wt with 1.4 mg g(-1) astragaloside IV, similar to cultures from 250 ml and 1 l flasks, but greater than yields from a 10 l bioreactor (dry wt 9.4 g l(-1), astragaloside IV 0.9 mg g(-1)). Polysaccharide yields were similar amongst the different bioreactors (range 25-32 mg g(-1)). The active constituent content of the cells approached that of plant extracts, indicating that large scale hairy root cultures of A. membranaceus has the potential to provide an alternative to plant crops without compromising yield or pharmacological potential.

[Studies on the chemical constituents of Evodia rutaecarpa (Juss.) Benth. var. officinalis (Dode) Huang].

AIM: To study the chemical constituents of the unriped fruits from Evodia rutaecarpa (Juss.) Benth. var. officinalis (Dode) Huang. METHODS: Various chromatographic techniques were used to separate and purify the constituents. Their structures were elucidated on the physico-chemical properties and spectral data. RESULTS: A lot of compounds were isolated of the unriped fruits from Evodia rutaecarpa (Juss.) Benth. var. officinalis (Dode) Huang. This paper reports mainly compounds identified as shihulimonin A, emodin, physcion, chrysophanol and limonin. CONCLUSION: Shihulimonin A is a new compound. Emodin, physcion and chrysophanol were isolated from the Evodia for the first time.

[Effect of satragaloside IV on the increase of microvascular permeability induced by histamine in pial microvessels of rat].

OBJECTIVE: To study the effect of satragaloside IV on the microvascular permeability induced by histamine in pial microvessels. METHOD: The microvascular permeability was expressed by changes in the transendothelial electrical resistance which was measured with technique using microelectrode impaled into the vascular lumen and based on cable analysis of vessels in rat. RESULT: The transendothelial electrical resistance of microvessels superfused with artificial cerebrospinal fluid was about 2500 omega.cm2, indicating a tight barrier with extremely low ion permeability, and application of 10(-4) mol.L-1 histamine in superfusate caused a rapid and reversible decrease in transendothelial electrical resistance. In paired experiment, the decrease of transendothelial electrical resistance induced by 10(-4) mol.L-1 histamine was inhibited by adding 0.8 x 10(-4) mol.L-1 satragaloside IV in superfusate. CONCLUSION: The results indicated that increases in the microvascular permeability induced by histamine, and satragaloside IV can inhibit the increases in the microvascular permeability induced by histamine. It is necessary that the cellular mechanism of permeability response induced by satragaloside IV be further elucidated.

[Effects of components isolated from Astragalus membranaceus Bunge on cardiac function injured by myocardial ischemia reperfusion in rats].

OBJECTIVE: To investigate the effects of components isolated from Astragalus membranaceus on myocardial ischemia reperfusion injury. METHODS: The myocardial ischemia reperfusion injury model was created by the left anterior descending coronary artery occlusion from the oracotouated rats, and the total saponins, total flavonids and astragaloside i.v. isolated from A. membranaceus on hemodynamics during acute myocardial ischemia, Na(+)-K(+)-ATPase activity, cAMP and malondialdehyede (MDA) contents in the ischemic myocardium were observed. RESULTS: The total saponins, total flavonids and astragaloside i.v. attenuated the declines of the amplitudes of LVSP and +/- LVdp/dtmax in rat heart injured by ischemia reperfusion in vivo, and decreased Na(+)-K(+)-ATPase activity in the ischemic myocardium. Otherwise, the total saponins increased the cAMP content and the total flavonids decreased the level of MDA production in the ischemic myocardium. CONCLUSION: The effects of different components isolated from A. membranaceus on protecting the cardiac function in the process of ischemia reperfusion may be related to the mechanism of improving energy metabolism, scavenging the oxygen free radicals and inhibiting the production of free radicals in the ischemic myocardium.

[Studies on constituents in Uncaria macrophylla Wall].

OBJECTIVE: To study the chemical constituents of Uncaria macrophylla. METHOD: Compounds were isolated by Columu Chromatography, and the structures were identified by NMR spectral data and other methods. RESULT AND CONCLUSION: Six compounds were isolated and identified as ursolic acid, 3 beta-6 beta-23-trihydroxyurs-12-en-28-oic acid, 3 beta, 6 beta, 19 alpha-trihydroxyurs-12-en-28-oic acid, epicatechin, beta-sitosterol and daucosterin. All the compounds were isolated for the first time from the plant.

Treatment of mycoplasma contamination in a large panel of cell cultures.

Mycoplasmal contamination remains a significant impediment to the culture of eukaryotic cells. For certain cultures, attempts to eliminate the infection are feasible alternatives to the normally recommended disposal of the contaminated culture. Here, three antibiotic regimens for mycoplasmal decontamination were compared in a large panel of naturally infected cultures: a 1-wk treatment with the fluoroquinolone mycoplasma removal agent (MRA), a 2-wk treatment with the fluoroquinolone ciprofloxacin, and three rounds of a sequential 1-wk treatment with BM-Cyclin containing tiamulin and minocyclin. These antibiotic treatments had a high efficiency of permanent cure: MRA 69%, ciprofloxacin 75%, BM-Cyclin 87%. Resistance to mycoplasma eradication was observed in some cell cultures: BM-Cyclin 0%, MRA 20%, ciprofloxacin 20%. Nearly all resistant contaminants that could be identified belonged to the species Mycoplasma arginini and M. orale. Detrimental effects of the antibiotics were seen in the form of culture death caused by cytotoxicity (in 5 to 13% of the cultures). Alterations of the cellular phenotypic features or selective clonal outgrowth might represent further untoward side effects of exposure to these antibiotics. Overall, antibiotic decontamination of mycoplasmas is an efficient, inexpensive, reliable, and simple method: 150/200 (75%) chronically and heavily contaminated cultures were cured and 50/200 (25%) cultures could not be cleansed and were either lost or remained infected. It is concluded that eukaryotic cell cultures containing mycoplasmas are amenable to antibiotic treatment and that a cure rate of three-quarters is a reasonable expectation.