Traditional Chinese Herbal Remedy Research Articles

Free radical scavenging and apoptotic effects of Cordyceps sinensis fractionated by supercritical carbon dioxide

Supercritical carbon dioxide (SC-CO 2) was used as the elution solvent for fractioning ethanolic extract (E) of Cordyceps sinensis (CS), a traditional Chinese herbal remedy, into R, F1, F2, and F3 fractions. This extractive fractionation method is amenable to large scale and is nontoxic. These four fractions were characterized in terms of total polysaccharides and cordycepin concentrations, scavenging ability of free radicals, and anti-tumor activities. Experimental results demonstrated that fractionation altered the distributions of total polysaccharides and cordycepin in fractions. Fraction R was the most active fraction to scavenge free radicals and inhibit the proliferation of carcinoma cells, followed by the fraction F1 and the extract E. The effect of scavenging on 1,1-diphenyl-2-picryl hydrazyl (DPPH) of CS extract and fractions at 2 mg/ml was R (93%), F1 (75%), E (66%), F2 (47%), and F3 (27%). The IC 50 (50% cell growth inhibitory concentration) of tumor cell proliferation and colony formation on human colorectal (HT-29 and HCT 116) and hepatocellular (Hep 3B and Hep G2) carcinoma cells by fraction R were around 2 μg/ml. Conversely, R did not affect the growth of normal dividing human peripheral blood mononuclear cells (PBMC) by exhibiting a large value of IC 50 over 200 μg/ml. Accumulation of tumor cells at sub-G 1 phase and the fragmentation of DNA, typical features of programmed cell death, were observed in a time and dose dependent manner. Scavenging of free radicals and anti-cancer activity (value of IC 50) correlated closely with the quantities of polysaccharides (Spearman’s rho = 0.901 and −0.870, respectively). Taken together, our findings suggest that fraction R, obtained by SC-CO 2 fluid extractive fractionation, showed strong scavenging ability and selectively inhibited the growth of colorectal and hepatocellular cancer cells by the process of apoptosis.

Effects of magnolol and honokiol derived from traditional Chinese herbal remedies on gastrointestinal movement

To study the effects of magnolol and honokiol on isolated smooth muscle of gastrointestinal tract and their relationship with Ca2+, and on the gastric emptying and the intestinal propulsive activity in mice. Routine experimental methods using isolated gastric fundus strips of rats and isolated ileum segments of guinea pigs were adopted to measure the smooth muscle tension. The effects of magnolol 10(-3), 10(-4), 10(-5) mol/L, and honokiol 10(-4), 10(-5), 10(-6) mol/L on the contractility of gastric fundus strips of rats and ileum of guinea pigs induced by acetylcholine (Ach) and 5-hydroxytryptamine (5-HT) was assessed respectively. The method using nuclein and pigment methylene blue was adopted to measure the gastric retention rate of nuclein and the intestinal propulsive ratio of a nutritional semi-solid meal for assessing the effect of magnolol and honokiol (0.5, 2, 20 mg/kg) on gastric emptying and intestinal propulsion. Magnolol and honokiol significantly inhibited the contractility of isolated gastric fundus strips of rats treated with Ach or 5-HT and isolated ileum guinea pigs treated with Ach or CaCl2, and both of them behaved as non-competitive muscarinic antagonists. Magnolol and honokiol inhibited the contraction induced by Ach in Ca2+-free medium and extracellular Ca2+-dependent contraction induced by Ach. Each group of magnolol and honokiol experiments significantly decreased the residual rate of nuclein in the stomach and increased the intestinal propulsive ratio in mice. The inhibitory effect of magnolol and honokiol on contractility of the smooth muscles of isolated gastric fundus strips of rats and isolated ileum of guinea pigs is associated with a calcium-antagonistic effect. Magnolol and honokiol can improve the gastric emptying of a semi-solid meal and intestinal propulsive activity in mice.

In vitro antiprotozoal effects of artemisinin on Neospora caninum

Neospora caninum is an intracellular apicomplexan parasite that infects a wide range of mammals and has been associated with abortion in cattle worldwide. Artemisinin is an effective antimalarial compound derived from a traditional Chinese herbal remedy, qinghao or Artemisia annua L. In the study reported, the cultured host cells (vero cells or mouse peritoneal macrophages) infected with N. caninum tachyzoites were incubated with α-MEM (minimal essential medium) 10%HS supplemented with various concentration or artemisinin (20, 10, 1, 0.1 and 0.01 μg/ml) to examine the efficacy of artemisinin against N. caninum tachyzoites intracellular multiplication. In long-term studies, at 20 or 10 μg/ml for 11 days, artemisinin reduced N. caninum and completely eliminated all microscopic foci of N. caninum. At 1 μg/ml for 14 days, artemisinin reduced N. caninum and completely achieved elimination of all microscopic foci of N. caninum. There was no apparent toxicity to host cells in long-term studies. In short-term studies, at ≥0.1 μg/ml, artemisinin reduced N. caninum tachyzoites intracellular multiplication, significantly ( P<0.05) and appeared to depend on the artemisinin concentrations. Pretreatment of host cells or N. caninum tachyzoites with artemisinin had no effect on N. caninum tachyzoites intracellular multiplication. These results demonstrate that artemisinin inhibited N. caninum tachyzoites intracellular multiplication.

Effect of preoperative interventions on outcome following liver resection in a rat model of cirrhosis

Background/Aims: High morbidity and mortality rates in cirrhotic patients undergoing resections for hepatocellular malignancies underscore the need for identifying a therapy that will decrease fibrosis or enhance hepatic regenerative activity in the perioperative period. Thus, in the present study, 104 carbon tetrachloride-induced cirrhotic rats received either saline (untreated cirrhotic controls) or one of the following agents that have been reported to decrease hepatic fibrosis or increase hepatic regeneration; pentoxifylline, ciprofloxacin or a traditional Chinese herbal remedy (TCHR). Twelve additional rats served as healthy, non-cirrhotic controls. Methods: Treatments were administered daily by gavage for 4 weeks followed by a 70% partial hepatectomy. Hepatic fibrosis was documented at the time of surgery by computer-assisted quantitation of collagen content. Liver function and hepatic regenerative activity were documented 24 h post partial hepatectomy by serum bilirubin determinations and a combination of 3[H]-Thymidine incorporation into hepatic DNA and proliferating cell nuclear antigen (PCNA) quantitation, respectively. Results: Compared to untreated cirrhotic controls (8.1±0.7%), fibrosis was significantly reduced in the pentoxifylline- and ciprofloxacin-treated groups (4.6±0.2%, p<0.005 and 5.5±0.6%, p<0.05) but unchanged in the TCHR-treated group (6.6±1.0%). Post-operatively, total serum bilirubin levels were lower in the pentoxifylline (1.40±0.15 mg/dl, p<0.01) and ciprofloxacin (1.87±0.25 mg/dl, p<0.05)-treated groups, but unchanged in the TCHR group (2.20±0.45 mg/dl), when compared to untreated cirrhotic controls (3.00±0.37 mg/dl). Hepatic regenerative activity was also significantly improved in the pentoxifylline-treated group (17.8±2.2 versus 9.9±1.9 DPM/μg DNA in untreated cirrhotic controls, p<0.05), but unchanged in the ciprofloxacin (16.1±1.8 DPM/μg DNA) and TCHR (10.9±1.2 DPM/μg DNA)-treated groups. PCNA protein determinations were in keeping with the 3[H]-Thymidine results. Conclusions: Pre-operative pentoxifylline holds promise as a useful therapeutic intervention for patients with cirrhosis requiring hepatic resection.

Artemisinin Enhances Heme-Catalysed Oxidation of Lipid Membranes

Artemisinin, a sesquiterpene endoperoxide derived from a traditional Chinese herbal remedy for fevers, is a promising new antimalarial drug, particularly useful against multidrug resistant strains of P. falciparum. Despite widespread clinical use, its mode of action remains uncertain. We investigated whether its antimalarial properties could be explained by an ability to enhance the redox activity of heme, formed in the parasite food vacuole from digested hemoglobin. Artemisinin caused a sustained threefold increase, followed by a gradual decline, in the peroxidase activity of heme. It also enhanced the ability of heme to oxidize membrane lipids about sixfold. An unexpected finding was the potentiation of heme-catalysed membrane lipid oxidation by Vitamin E. The changes in redox-catalytic activity induced by artemisinin were paralleled by major changes in the absorption spectrum of heme, culminating in loss of the Soret band. We propose a model in which artemisinin binds irreversibly to heme in the parasite food vacuole, preventing its polymerization to chemically inert hemozoin, and promoting heme-catalysed oxidation of the vacuolar membrane by molecular oxygen, which leads, ultimately, to vacuole rupture and parasite autodigestion. © 1997 Elsevier Science Inc.

Suppression of Spontaneous Development of Uterine Adenomyosis by a Chinese Herbal Medicine, Keishi-Bukuryo-Gan, in Mice

Keishi-bukuryo-gan (KBG) is a traditional Chinese herbal remedy and has been used for the treatment of gynecological disorders, such as hypermenorrhea, dysmenorrhea, and infertility. The effects of KBG on the development of uterine adenomyosis, which is characterized by an abnormal growth of glands and stroma into and beyond the smooth muscle layers of the uterus, were examined in an experimental animal model using the SHN strain of mice. Mice fed handmade chow containing relatively high doses of KBG (0.5% and 1%) showed a significantly lower incidence of adenomyosis and lower activity of thymidylate synthetase (TS) in the uteri than mice fed control handmade chow containing no KBG. The long-term exposure to KBG between 25 and 120 days of age hardly affected the estrous cycle, food intake and body weight. However, mice provided with chow containing a low dose of KBG (0.1%) showed no difference in the incidence of adenomyosis as compared with the controls. The inhibitory effects of the high doses of KBG were nullified by pituitary isografting, which has been proved to enhance the development of adenomyosis. The present mouse data support the view in humans that the oral administration of KBG is a useful tool for the treatment of uterine adenomyosis.

Ligustrazine is a vasodilator of human pulmonary and bronchial arteries

We have investigated the dilator effect of ligustrazine, the semisynthetic principle of a traditional Chinese herbal remedy, on human pulmonary and bronchial arteries in vitro. Ligustrazine caused a concentration-dependent relaxation of human small pulmonary arteries, which was independent of endothelium. Although ligustrazine was equally potent in inducing dilatation of pulmonary and bronchial arteries, it was about 10 times more potent in relaxing small pulmonary arteries (300–500 μm i.d.) compared with lobar pulmonary arteries (7–8 mm i.d.). By contrast, the relaxant responses of small and lobar pulmonary arteries to sodium nitroprusside was not significantly different. Ligustrazine was equally potent in relaxing prostaglandin F 2α- or 5-hydroxytryptamine-precontracted pulmonary arteries, suggesting that it is not a prostaglandin F 2α or 5-hydroxytryptamine antagonist. Preincubating the vessels with propranolol (1 μM) or indomethacin (10 μM) had no significant effect on the ligustrazine-induced vasodilatation. However, ligustrazine caused concentration-dependent inhibition of calcium-evoked contraction when applied to rat aorta in calcium-free K +-depolarizing medium. We conclude that ligustrazine is a dilator of human pulmonary and bronchial arteries, which is endothelium-independent and that ligustrazine preferentially relaxes pulmonary resistance vessels rather than large conduit pulmonary arteries.

Effects of a Chinese herbal medicine, Keishi-bukuryogan, on the gonadal system of rats

Keishi-bukuryo-gan (TJ-25) is a traditional Chinese herbal remedy containing five components: bark of Cinnamomum cassia, root of Poeerato lactiflora, seed of Prunus persica or P. persiba var. davidiana, carpophores of Porta cocos and root bark of Paeonia suffruticosa. This preparation has been used in the treatment of gynecological disorders such as hypermenorrhea, dysmenorrhea and infertility. In the present study, the effects of TJ-25 on plasma levels of luteinizing hormone (LH), follicle-stimulating hormone (FSH) and estradiol (E 2), and on uterine wet weight and thymidine kinase (TK) activity were documented in immature rats. Long-term daily oral administration of TJ-25 (300 mg/kg) for 14 days decreased plasma levels of LH, FSH and E 2 by 94%, 67% and 50%, respectively, compared to controls. Uterine wet weight and TK activity were reduced to 65% and 64% that of controls, respectively. Short-term effects of TJ-25 on E 2 were also examined. Thirty hours after administration of E 2 (1.0 μg/kg) alone, uterine wet weight and TK activity were elevated 2.4- and 21-fold, respectively, over controls. However, simultaneous administration of TJ-25 (three consecutive doses, every 12 h) with E 2 reduced E 2-induced increases in uterine wet weight and TK activity by 29% and 39%, respectively. Treatment with TJ-25 also enhanced LH-RH-induced increases in plasma LH and FSH levels 1.2- and 2.5-fold, respectively, as compared with controls. The results obtained in the present study indicate that TJ-25 may act as a LH-RH antagonist and/or as a weak anti-estrogen.