Drugs, Chinese Herbal

Publication Title: 
Journal of Pharmaceutical and Biomedical Analysis

Spinosin, a major bioactive herbal ingredient isolated from Semen Ziziphi Spinosae, plays an important role in sedation and hypnosis. However, the pharmacokinetic behavior of spinosin in special sites has not been reported. Microdialysis (MD) technique, as a continuous, realtime monitoring sampling technique, is very suitable for the evaluation of the disposition of diverse drugs.

Ma, Rong-Hua
Yang, Jie
Qi, Lian-Wen
Xin, Gui-Zhong
Wang, Chong-Zhi
Yuan, Chun-Su
Wen, Xiao-Dong
Li, Ping
Publication Title: 
Journal of Ethnopharmacology

ETHNOPHARMACOLOGICAL RELEVANCE: Rhizoma Paridis saponins (RPS) have been well studied for antimicrobial, anti-hemorrhagic, and anticancer effects. However, scientific information on RPS regarding the toxic and neuropharmacological effects is limited. In this study, the acute oral toxicity, sedative-hypnotic activity and gastro-intestinal toxicity of RPS were investigated. MATERIALS AND METHODS: The acute toxicity was carried out by administering single doses (800-5000 mg/kg) of RPS to adult mice.

Liu, Zhen
Gao, Wenyuan
Man, Shuli
Wang, Jieyin
Li, Nan
Yin, Shuangshuang
Wu, Shanshan
Liu, Changxiao
Publication Title: 
The American Journal of Clinical Nutrition

Young female mice were fed torula-yeast-based diets deficient in vitamin E or selenium or supplemented with cod-liver oil to determine the effect of host antioxidant status on the therapeutic efficacy of the Chinese traditional antimalarial drug qinghaosu (QHS), a sesquiterpene endoperoxide. Vitamin E deficiency enhanced the antimalarial action of QHS against Plasmodium yoelii, both in terms of decreased parasitemia and improved survival but Se deficiency did not.

Levander, O. A.
Ager, A. L.
Morris, V. C.
May, R. G.
Publication Title: 
Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica

The cytotoxicities of 2 derivatives of artemisinin B and 2 derivatives of artemisic acid (designated as Compound A, B, C, and D) were investigated, using trypan blue dye exclusion test and colony-forming units assay. At the concentration of 5 micrograms.ml-1, the inhibition rates of these 4 compounds against murine leukemia cell line P388 were > 85%.

Sun, W. C.
Han, J. X.
Yang, W. Y.
Deng, D. A.
Yue, X. F.
Publication Title: 
Antimicrobial Agents and Chemotherapy

Artemisinin is an important new antimalarial agent containing a bridged endoperoxide. The in vitro antimalarial activity of an artemisinin derivative, arteether, is antagonized by two iron chelators, pyridoxal benzoylhydrazone and 1,2-dimethyl-3-hydroxypyrid-4-one. Similarly, the acute toxicity of artemisinin in mice is antagonized by another chelator, deferoxamine-hydroxyethylstarch. A combination of artemisinin and hemin oxidizes erythrocyte membrane thiols in vitro, and this oxidation is also inhibited by an iron chelator.

Meshnick, S. R.
Yang, Y. Z.
Lima, V.
Kuypers, F.
Kamchonwongpaisan, S.
Yuthavong, Y.
Publication Title: 
Bulletin of the World Health Organization

In-vitro drug sensitivity tests were performed on Philippine isolates of Plasmodium falciparum between 1991 and 1993, using the radioisotope microdilution method. The success of the tests varied significantly with the level of parasitaemia, the source of the strains, the period that elapsed before culturing, and the detectable concentrations of antimalarials in the blood. There was a significant positive correlation between the IC50 values for chloroquine and artesunate and the level of chloroquine in the blood before testing.

Bustos, M. D.
Gay, F.
Diquet, B.
Publication Title: 
The Journal of Biological Chemistry

Artemisinin and its derivatives are important new antimalarial drugs. When Plasmodium falciparum-infected erythrocytes are incubated with [10-3H]dihydroartemisinin, several malaria-specific proteins become labeled. One of these proteins is the P. falciparum translationally controlled tumor protein (TCTP) homolog. In vitro, dihydroartemisinin reacts covalently with recombinant TCTP in the presence of hemin. The association between drug and protein increases with increasing drug concentration, plateauing at approximately 1 drug/TCTP molecule.

Bhisutthibhan, J.
Pan, X. Q.
Hossler, P. A.
Walker, D. J.
Yowell, C. A.
Carlton, J.
Dame, J. B.
Meshnick, S. R.
Publication Title: 
The American Journal of Tropical Medicine and Hygiene

Eight healthy Vietnamese male subjects received 400 mg artemisinin formulated into fatty suppositories (FS), and six different subjects received 500 mg of artemisinin formulated in polyethylene glycol suppositories (PEGS). Plasma concentrations were measured by high-performance liquid chromatography with electrochemical detection; concentration versus time curves were analyzed with nonparametric methods. No statistically significant differences were found between the two formulations.

Koopmans, R.
Ha, L. D.
Duc, D. D.
Dien, T. K.
Kager, P. A.
Khanh, N. X.
van Boxtel, C. J.
de Vries, P. J.
Publication Title: 
The Journal of Biological Chemistry

Endoperoxide antimalarials based on the ancient Chinese drug Qinghaosu (artemisinin) are currently our major hope in the fight against drug-resistant malaria. Rational drug design based on artemisinin and its analogues is slow as the mechanism of action of these antimalarials is not clear. Here we report that these drugs, at least in part, exert their effect by interfering with the plasmodial hemoglobin catabolic pathway and inhibition of heme polymerization. In an in vitro experiment we observed inhibition of digestive vacuole proteolytic activity of malarial parasite by artemisinin.

Pandey, A. V.
Tekwani, B. L.
Singh, R. L.
Chauhan, V. S.
Publication Title: 
The American Journal of Tropical Medicine and Hygiene

The efficacy of artemisinin monotherapy was studied in 227 patients with uncomplicated falciparum malaria. They all received artemisinin at t = 0 hr, t = 8 hr, and thereafter once daily; treatment was extended at random until they had taken either 5 days of artemisinin followed by 2 days of placebo (A5), or 7 days (A7) of artemisinin. The adult artemisinin dose was 500 mg; children aged < 15 years received 10 mg/kg per dose. The median (range) parasite clearance time was 39 (8-112) hr for A5 and 43 (38-104) hr for A7 (P = 0.085). The recrudescence rates were similar between the groups.

Giao, P. T.
Binh, T. Q.
Kager, P. A.
Long, H. P.
Van Thang, N.
Van Nam, N.
de Vries, P. J.


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