Isolation, synthesis and bioactivity evaluation of isoquinoline alkaloids from Corydalis hendersonii Hemsl. against gastric cancer in vitro and in vivo.

Isoquinoline alkaloid displays significant anti-gastric cancer effects due to its unique structure, which is attracting more and more attention for the development of anti-gastric cancer drugs. In this study, we explore the active components against gastric cancer from the Tibetan Medicine Corydalis hendersonii Hemsl, which is rich in isoquinoline alkaloids. 14 compounds including 2 previously undescribed natural products were obtained. Interestingly, an new active compound displays potent anti-gastric cancer activity. After accomplishing the total syntheses of the active compound and its derivatives, the anti-gastric cancer activity of the active compound was further investigated. In vitro experiments revealed that the active compound significantly attenuated the proliferative capacity, caused G2/M phase arrest, inhibited the cell migration and invasion, and induced cell apoptosis. Mechanistically, the active compound could increase the Bax/Bcl-2 ratio, elevate cytochrome c in the cytosol, and activate caspase-9/3, along with inactivating the upstream PI3K/Akt/mTOR signaling pathway. In addition, the active compound could also cause gastric cancer cell death by inhibiting topoisomerase I activity. More importantly, the anti-gastric cancer activity of the active compound was confirmed in MGC-803 xenograft nude mice in vivo. This work not only promotes the exploitation of Corydalis hendersonii Hemsl., but also provides some experience for discovering new entities from natural sources.

Brucea javanica oil emulsion improves the effect of radiotherapy on esophageal cancer cells by inhibiting cyclin D1-CDK4/6 axis.

BACKGROUND: Esophageal cancer is one of the most common cancers around the world, and it has high incidence and mortality rates. The conventional therapy for esophageal cancer is radiotherapy, although its effect is highly limited by the resistance of esophageal cancer cells. Thus, strong radiosensitizers can be very crucial during radiotherapy against esophageal cancer. Brucea javanica oil emulsion (BJOE) is a widely used drug against various cancers, such as liver, colon, and ovarian cancer. However, its anti-cancer effect and mechanism and the use of BJOE as a radiosensitizer have not been explored in esophageal cancer. AIM: To evaluate the anti-cancer effect and mechanism of BJOE and explore the potential use of BJOE as a radiosensitizer during radiotherapy. METHODS: The inhibitory effect of BJOE and its enhancement function with radiation on cell viability were examined with the calculated half-maximal effective concentration and half-maximal lethal concentration. The influence of BJOE on cell migration and invasion were measured with EC109 and JAR cells by wound-healing and transwell assay. Clonogenesis and apoptotic rate, which was measured by Hoechst staining, were investigated to confirm its enhancement function with radiation. To investigate the molecular pathway underlying the effect of BJOE, the expressions of several apoptosis- and cycle-related proteins was detected by western blotting. RESULTS: Our results demonstrated that BJOE inhibited the growth of esophageal cancer cell lines more than normal cell lines, and it markedly reduced migration and invasion in esophageal cancer cells (EC109 and JAR). Moreover, it promoted cell apoptosis and enhanced the effect of radiotherapy against esophageal cancerous cells. In the viability test, the values of half-maximal effective concentration and half-maximal lethal concentration were reduced. Compared to the control, only around 1/5 colonies formed when using BJOE and radiation together in the clonogenic assay. The apoptotic rate in EC109 was obviously promoted when BJOE was added during radiotherapy. Our study suggests that the expression of the apoptosis-proteins Bax and p21 were increased, while the expression of Bcl-2 was stable. Further detection of downstream proteins revealed that the expression of cyclin D1 and cyclin-dependent kinase 4/6 were significantly decreased. CONCLUSION: BJOE has a strong anti-cancer effect on esophageal cancer and can be used as a radiosensitizer to promote apoptosis in cancerous esophageal cells via the cyclin D1-cyclin-dependent kinase 4/6 axis.

[Efficiency and mechanics of surfactant modified zeolite with nitrate adsorbed to control nitrogen and phosphorus release from sediments].

Efficiency and mechanics of surfactant modified zeolite (SMZ) with nitrate adsorbed to control nitrogen and phosphorus release from sediments were researched. The results show that: 1) The optimal level of HDTMA adsorbed on SMZ for nitrate sorption was 276% ECEC. The sorption of nitrate on SMZ can be well described by the Langmuir sorption isotherm, and the sorption capacity was 1724 mg/kg. The nitrate sorption on SMZ was quick and the nitrate adsorbed on SMZ can be released. The sorption of ammonia and phosphorus on SMZ with nitrate adsorbed can also be well described by the Langmuir sorption isotherm, and the sorption capacity of ammonia and phosphorus are 12.0 mg/g and 0.597 mg/g respectively. 2) The barrier of SMZ with nitrate adsorbed can provide nitrate for surface sediments for a long time, and the quantity of released nitrate in overlying water was much less than that of nitrate directly added. This barrier can not only efficiently control ammonia release from sediments, but also control phosphorus release from sediment efficiently.

[Observation on therapeutic effect of acupuncture and moxibustion on hyperemesis gravidarum].

OBJECTIVE: To search for the best method for treatment of hyperemesis gravidarum. METHODS: One hundred and fifty cases of hyperemesis gravidarum were randomly divided into 3 groups, acup-moxibustion group, Chinese drug group and Western medicine group, 50 cases in each group. The acup-moxibustion group were treated with acupuncture at Zhongwan (CV 12), Neiguan (PC 6), Zusanli (ST 36) and Yinlingquan (SP 9), and after arrival of qi, mild warming moxibustion of 10-15 min was added; the Chinese drug group with oral administration of modified Suye Huanglian Decoction , and the Western medicine group with oral administration of phenobarbital and supplement of water and electrolyte. RESULTS: The total effective rate was 86.0% in the acup-moxibustion group, 42.0% in the Chinese drug group and 38.0% in the Western medicine group with a significant difference among the 3 groups (P < 0.05), the therapeutic effect in the acup-moxibustion group being the best. CONCLUSION: Acup-moxibustion is the best method for hyperemesis gravidarum.