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Coptidis rhizoma has been used as traditional herb medicine in gastrointestinal disorders in the Eastern Asia. We investigated whether the anticancer effects of the C. rhizoma induced apoptosis on human colorectal cancer cells SNU-C4. The cytotoxic effect of C. rhizoma was assessed by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. To determine apoptotic cell death, 4,6-diamidino-2-phenylindole (DAPI) staining, terminal deoxynucleotidyl transferase (TdT)-mediated dUTP nick end labeling (TUNEL) assay, reverse transcription-polymerase chain reaction (RT-PCR) and caspase-3 enzyme assay were performed. In this study, C. rhizoma treatment (100 μg/ml) revealed typical morphological apoptotic features. Additionally, C. rhizoma treatment (100 μg/ml) increased levels of BAX and CASPASE-3, and decreased levels of BCL-2. Caspase-3 enzyme activity by treatment of C. rhizoma (100 μg/ml) also significantly increased compared to the control (p<0.05). These data indicate that C. rhizoma caused cell death by apoptosis through caspase pathways on human colorectal cancer cells SNU-C4.

Chunghyul-dan has inhibitory effects on HMG-CoA reductase and pancreatic lipase. We investigated whether Chunghyul-dan has therapeutic effects on humans with hypercholesterolemia. This study was a case-control, open-labeled clinical study. Subjects were treated with Chunghyul-dan (600 mg/day) or Atorvastatin (10 mg/day) for 8 weeks. Serum lipids were checked at baseline after 4 and 8 weeks of medication. While, Chunghyul-dan showed significant lipid-lowering effects, it was less effective than Atorvastatin. In comparison with the histological controls, Chunghyul-dan's effects were superior to placebo. On safety assessment, there was no adverse effect with the use of Chunghyul-dan in hepatic or renal toxicity. In conclusion, we suggest that Chunghyul-dan is a useful herbal medicine for hypercholesterolemia.

Hypertension is one of the modifiable risk factors for stroke. Lowering blood pressure is helpful for primary and secondary prevention of stroke. This study is aimed to assess the efficacy of Chunghyul-dan on stroke patients with stage 1 hypertension using 24 hours ambulatory blood pressure monitoring (24ABPM). Forty hospitalized stroke patients with stage 1 hypertension were included in the study and they were randomly assigned into two groups: group A was treated with Chunghyul-dan 1200 mg once a day for 2 weeks, while group B was not. Twelve subjects were dropped out because of unexpected early discharge or data errors, thus the remaining 28 subjects were included in the final analysis (15 in group A and 13 in group B). Blood pressure was monitored every 30 minutes for 24 hours at baseline and 2 weeks after medication. Blood pressure, pulse rate, trough/peak ratio (TPR) [the value calculated by dividing the blood pressure change at trough (22 to 24 hours after drug intake) by the change at peak (2 adjacent hours with a maximal blood pressure reduction between the second and eighth hour after drug intake)] and smoothness index (SI) (the value calculated as the ratio between the average of the 24 hours, treatment-induced blood pressure changes and its standard deviation) were compared to assess the efficacy of Chunghyul-dan. To assess the safety of Chunghyul-dan, any adverse effects during medication period were monitored. There was no significant difference in the baseline assessment between the two groups. Systolic blood pressure was lower in group A than in group B (141.37 ± 8.96 mmHg versus 132.28 ± 9.46 mmHg, P = 0.03), while diastolic blood pressure and pulse rate had no significant difference between the two groups. Systolic TPR and SI was 0.87 and 1.04 in group A, respectively. This suggests that Chunghyul-dan have anti-hypertensive effect on stroke patients with stage 1 hypertension.

A rapid and simple high-performance liquid chromatographic method for determination of berberine in rat thalamus was described in this study. Thalamus samples were pretreated by protein precipitation with methanol and acetonitrile. Berberine was determined using a Hypersil C₁₈ column with an isocratic mobile phase of acetonitrile — 0.05 M potassium dihydrogen phosphate (containing 0.5% triethylamine, pH 3.0) (30:70 v/v) and with UV detection at 265 nm. The lower limit of quantification for berberine in thalamus was 24 ng/ml, and the lowest concentration of berberine determined in rat thalamus samples was 47.5 ng/ml at 48 hours. The calibration curve for berberine was linear (r² = 0.9994) over the concentration range 24–6000 ng/ml. At this concentration range, the overall recoveries (91.20%–93.24%) for berberine were determined and the accuracy of the intra- and inter-day assays from rat thalamus were less than 6% RSD. Following intravenous administration of 10.2 mg/kg of Coptidis Rhizoma (CR) extract containing 3 mg/kg berberine into rats, the thalamus level of berberine increased rapidly (t_1/2α = 1.93 hours), peaked at 2.48 hours with a concentration of 271 ng/g, and had a slow elimination rate (t_1/2β = 14.6 hours), which suggested that berberine might directly act on certain regions of the thalamus, have pharmacological effects on some cerebral dysfunctions, and be an active ingredient of Huang Lian Jie Du Tang for the treatment of cerebral disease.

Coptidis Rhizoma (Chinese: Huanglian) and Phellodendri Chinensis Cortex (Chinese: Huangbo) are widely used Traditional Chinese Medicine, and often used in combination because of their similar pharmacological effects in clinical practice. However, the quality control methods of the two drugs are different and complicated, which is time consuming and laborious in practical application. In this paper, rapid and simultaneous determination of moisture and berberine in Coptidis Rhizoma (CR) and Phellodendri Chinensis Cortex (PC) was realized by near-infrared spectroscopy (NIRs) combined with global models. Competitive adaptive reweighted sampling (CARS) and successive projection algorithm (SPA) method were applied for variable selection. Principal component analysis (PCA) and partial least squares regression method (PLSR) were applied for qualitative and quantitative analysis, respectively. The characteristic variables of berberine showed similarity and consistency in distribution, providing basis for the global models. For moisture content, the global model had relative standard error of prediction set (RSEP) value of 3.04% and 2.53% for CR and PC, respectively. For berberine content, the global model had RSEP value of 5.41% and 3.97% for CR and PC, respectively. These results indicated the global models based on CARS-PLS method achieved satisfactory prediction for moisture and berberine content, improving the determination efficiency. Furthermore, the greater range and larger number of samples enhanced the reliance of the global model. The NIRs combined with global models could be a powerful tool for quality control of CR and PC.