Application of cocrystal separation technology in the separation and purification of genistein-puerarin-daidzein ternary system / 药学学报

Cocrystal separation technology is a technology that utilizes coformers to selectively form cocrystals with target compounds and separate them from mixed systems. Our study used puerarin (PUE), daidzein (DDZ), and genistein (GEN) as model drugs, which have similar structures and are the main isoflavones in Pueraria lobata root. The separation and purification processes in the modern traditional Chinese medicine (TCM) of these three components use conventional column chromatography, recrystallization, and other technologies, which have the issues of lengthy separation cycles, high solvent consumption, and inefficient preparation. Different with existing separation technology, our team used the early-found cocrystal separation method to design a step-by-step extraction and separation experiment of GEN-PUE-DDZ ternary mixture. Caffeine and L-proline were added to the mixed system in turn, GEN-caffeine cocrystal and PUE-proline cocrystal were prepared by suspension method. The cocrystals precipitated out of the solution. The purities of the GEN-caffeine cocrystal and the PUE-proline cocrystal could achieve 93% (the purity of GEN) and 99% (the purity of PUE). Besides, the purity of DDZ could also be increased by 6.76 times. This study proposed a simple operating, low cost and wide application range separation method different from the traditional separation method and realized the separation of structurally similar chemical components in TCM, laying a foundation for the application of cocrystal technology in the separation and refining of TCM.

Panax notoginseng saponins prevent colitis-associated colorectal cancer via inhibition IDO1 mediated immune regulation / 中国天然药物

Colorectal cancer (CRC) is the third most lethal cancer and leading cause of cancer mortality worldwide. A key driver of CRC development is colon inflammatory responses especially in patients with inflammatory bowl disease (IBD). It has been proved that Panax notoginseng saponins (PNS) have anti-inflammatory, anti-oxidant and anti-tumor effects. The chemopreventive and immunomodulatory functions of PNS on colitis-associated colorectal cancer (CAC) have not been evaluated.This present study was designed to study the potential protective effects of PNS on AOM/DSS-induced CAC mice to explore the possible mechanism of PNS against CAC. Our study showed that PNS significantly alleviated colitis severity and prevented the occurrence of CAC. Functional assays revealed that PNS relieved immunosuppression of Treg cells in the CAC microenvironment by inhibiting the expression of IDO1 mediated directly by signal transducer and activator of transcription 1 (STAT1) rather than phosphorylated STAT1. Ultimately, Rh1, one of the PNS metabolites, exhibited the best inhibitory effect on IDO1 enzyme activity. Our study showed that PNS exerted significant chemopreventive function and immunomodulatory properties on CAC. It could reduce macrophages accumulation and Treg cells differentiation to reshape the immune microenvironment of CAC. These findings provided a promising approach for CAC intervention.

Multidetector CT Characteristics of Fumarate HydrataseDeficient Renal Cell Carcinoma and Papillary Type II Renal Cell Carcinoma

Objective@#To investigate the multidetector computed tomography (MDCT) features of fumarate hydratase-deficient renal cell carcinoma (FH-deficient RCC) with germline or somatic mutations, and compare them with those of papillary type II RCC (pRCC type II). @*Materials and Methods@#A total of 24 patients (mean ± standard deviation, 40.4 ± 14.7 years) with pathologically confirmed FH-deficient RCC (15 with germline and 9 with somatic mutations) and 54 patients (58.6 ± 12.6 years) with pRCC type II were enrolled. The MDCT features were retrospectively reviewed and compared between the two entities and mutation subgroups, and were correlated with the clinicopathological findings. @*Results@#All the lesions were unilateral and single. Compared with pRCC type II, FH-deficient RCC was more prevalent among younger patients (40.4 ± 14.7 vs. 58.6 ± 12.6, p < 0.001) and tended to be larger (8.1 ± 4.1 vs. 5.4 ± 3.2, p = 0.002). Cystic solid patterns were more common in FH-deficient RCC (20/24 vs. 16/54, p < 0.001), with 16 of the 20 (80.0%) cystic solid tumors having showed typical polycystic and thin smooth walls and/or septa, with an eccentric solid component. Lymph node (16/24 vs. 16/54, p = 0.003) and distant (11/24 vs. 3/54, p < 0.001) metastases were more frequent in FH-deficient RCC. FHdeficient RCC and pRCC type II showed similar attenuation in the unenhanced phase. The attenuation in the corticomedullary phase (CMP) (76.3% ± 25.0% vs. 60.2 ± 23.6, p = 0.008) and nephrographic phase (NP) (87.7 ± 20.5, vs. 71.2 ± 23.9, p = 0.004), absolute enhancement in CMP (39.0 ± 24.8 vs. 27.1 ± 22.7, p = 0.001) and NP (50.5 ± 20.5 vs. 38.2 ± 21.9, p = 0.001), and relative enhancement ratio to the renal cortex in CMP (0.35 ± 0.26 vs. 0.24 ± 0.19, p = 0.001) and NP (0.43 ± 0.24 vs. 0.29 ± 0.19, p < 0.001) were significantly higher in FH-deficient RCC. No significant difference was found between the FH germline and somatic mutation subgroups in any of the parameters. @*Conclusion@#The MDCT features of FH-deficient RCC were different from those of pRCC type II, whereas there was no statistical difference between the germline and somatic mutation subgroups. A kidney mass with a cystic solid pattern and metastatic tendency, especially in young patients, should be considered for FH-deficient RCC.

Overview of human clonorchiasis sinensis in China.

The objective of the survey was to determine the current status, trends and transmission factors for Clonorchis sinensis infection in China and to provide updated information for development control strategies. This was part of a nationwide survey of major human parasitic diseases carried out during 2000-2002 sampled by the stratified randomized cluster sampling method. Fecal examination was conducted using the Kato-Katz thick smear method and egg count per gram of feces (EPG) was determined for the egg-positive patients. A questionnaire and a case-control study were applied to analyze the transmission factors for C. sinensis infection. The overall prevalence rate of C. sinensis infection was 0.58% in 356,629 residents from 688 sampled pilot sites in 31 provinces, autonomous regions and municipalities (PAM) of China. The infection rates of C. sinensis in Guangdong, Jilin, Guangxi Zhuang autonomous region, Anhui and Heilongjiang were higher than the other PAM, they were 5.35, 4.77, 3.71, 0.67 and 0.48%, respectively. In Guangxi, moderate and heavy infections were found in 29.14% and 11.52%, respectively, of the total infected. Heavy infections were not found in any of the other provinces except for 2 heavily infected cases in Heilongjiang. The prevalence rate increased with age for residents aged < 35 years and remained at high levels in those aged 25-60 years. The infection rate in males was 1.64 times that of females. The C. sinensis egg positivity rates in fishermen, businessmen, physicians and teachers were higher than others. Among the 38 ethnic groups, the prevalences in the Han (3.20%) and the Zhuang (3.15%) were the highest; no cases were found among the Zang, Miao, Man and other 29 ethnic groups. Significant differences in prevalences were also found among counties of different economic levels. C. sinensis infection is prevalent in hilly and plains regions of northeast and southcentral China, representing two highly endemic areas in the North and the South. An increasing trend in prevalence was seen in endemic areas. The infection was mainly detected in young and middle aged males. A higher prevalence was observed in those with a better education and a higher income. Consumption of raw (or under-cooked) fresh water fish or shrimp were the main risk factors responsible for transmission of the parasite.

[Cost-benefit analysis of comprehensive parasitic disease control project in Rongxian County, Guangxi Zhuang autonomous region].

OBJECTIVE: To evaluate the cost-benefit of comprehensive parasitic disease control project in Rongxian County of Guangxi, so as to provide the evidence for formulating the control strategy of soil-transmitted nematode. METHODS: The data of the overall input and output for soil-transmitted nematode control were collected from 2007 to 2009, and the cost-benefit was analyzed. RESULTS: The infection rates of soil-transmitted nematode dropped from 30.10% in 2007 to 12.30% in 2009. The overall cost of soil -transmitted nematode control was 969 185.6 Yuan from 2007 to 2009. The direct benefits arising from avoiding the incidence of the disease for populations reached 88.415 million Yuan in three years. The ratio of benefit-cost was 91:1. CONCLUSIONS: The soil -transmitted nematode infection brings a heavy financial burden on both the patients and society. The implementation of comprehensive control measures can effectively control the prevalence of the diseases and produce good social and economic benefits.