1.Study on chemical constituents of sponge Mycale sp.from the South China Sea
Jiabao SUN ; Shuping WANG ; Jie WANG ; Li LIU ; Bingnan HAN ; Houwen LIN
Journal of Pharmaceutical Practice 2017;35(4):308-314
Objective To investigate the chemical constituents of marine sponge Mycale sp.collected from the South China Sea.Methods The ethyl acetate extract of the marine sponge Mycale sp.was separated and purified by repeated column chromatography on silica gel, Sephadex LH-20 and reversed-phase high-performance liquid chromatography (RP-HPLC).The structures of these compounds were identified by means of various modern spectroscopic techniques and comparison with their physicochemical properties to reported data.The tumor cell growth inhibitory activities of these compounds against human breast cancer cell lines MCF-7 and human lung cancer cell lines PC9 were tested by Cell Counting Kit-8 (CCK-8) method.Results Ten compounds were isolated and identified as cyclo-(Pro-Ile)(1),cyclo-(Pro-Leu)(2),cyclo-(Ile-Leu)(3),cyclo-(Phe-Pro)(4),cyclo-(Phe-Val)(5),cyclo-(Phe-Leu)(6),cyclo-(Phe-Ile)(7), 2′-deoxythymidine (8), thymine (9), 5-hydroxy-3,4-dimethyl-5-pentyl-2(5H)-furanone (10).These compounds showed weak tumor cell growth inhibitory activities toward cells MCF-7 and PC9 in vitro.Conclusion Compounds 1, 2, 4, 5, 6, 7 and 10 were isolated from the sponge Mycale sp.for the first time.It is the first time to report the antitumor activity evaluation for compounds 1~10.
3.Study on Anti-inflammatory Effect and Its Mechanism of the Extract of Dcsmodium microphyllum
Huazhen SU ; Xiuneng TANG ; Jiangcun WEI ; Jiabao MA ; Yong CHEN ; Liqing LIANG ; Xianzai JIANG ; Qian HAN
China Pharmacy 2019;30(18):2532-2536
OBJECTIVE: To study the anti-inflammatory effect and its mechanism of the extract of Dcsmodium microphyllum, so as to provide experiment reference for further study of D. microphyllum. METHODS: Acute inflammatory model was established by xylene,glacial acetic acid and carrageenan. Using dexamethasone as positive control (0.005 g/kg), inhibitory effects of intragastric different doses of the extract of D. microphyllum (50, 30, 15 g/kg) on xylene-induced ear swelling in normal mice and adrenalectomized mice, glacial acetic acid-induced permeability increasing of abdominal capillaries in normal mice, carrageenan- induced paw swelling in normal mice and adrenalectomized mice were investigated. The levels of MDA, SOD and NO in the inflammatory tissue of toes of adrenalectomized mice were detected in carrageenan-induced inflammation model. Blank group was set for control (ig. equal volumn of water). RESULTS: Compared with blank group, ear swelling degree of normal mice and adrenalectomized mice were decreased significantly in D. microphyllum extract high-dose and medium-dose groups while inhibitory rate of ear swelling was increased significantly; the permeability of abdominal capillaries of normal mice was significantly decreased in D. microphyllum extract groups; the swelling degree of toes in normal mice of D. microphyllum extract high-dose and middle-dose groups and adrenalectomized mice were significantly decreased while inhibitory rate of toe swelling was increased significantly (P<0.05 or P<0.01). The levels of MDA and NO in the toe inflammatory site of adrenalectomized mice were decreased significantly in D. microphyllum extract high-dose and medium-dose groups, while the level of SOD was increased significantly (P<0.05). CONCLUSIONS: D. microphyllum extract can inhibit acute inflammation in mice significantly. Its anti-inflammatory mechanism is associated with decreasing MDA and NO while increasing SOD levels, and the anti-inflammatory effect does not depend on the hypothalamus-pituitary-adrenal axis system.
4.Simultaneous Determination of Gallic Acid ,Cinnamic Acid and Catechin in 3 Processed Products of Rheum officinale by RP- HPLC
Jiangcun WEI ; Zhen XIE ; Zhengteng YANG ; Jiabao MA ; Zujie QIN ; Chenglong WANG ; Dongmei HUANG ; Wenrun ZHU ; Shengbin CHEN ; Qian HAN
China Pharmacy 2019;30(22):3053-3056
OBJECTIVE: To establish a method for simultaneous determination of gallic acid, cinnamic acid and catechin in 3 processed products of Rheum officinale. METHODS: RP-HPLC method was established. The determination was performed on Thermo ScientificTM Hypersil GOLD Dim column with mobile phase consisted of methanol-0.1% phosphoric acid solution (gradient elution) at the flow rate of 1.0 mL/min. The detection wavelength was set at 278 nm, and the column temperature was 30 ℃. The sample size was 10 μL. RESULTS: The linear range of gallic acid, cinnamic acid and catechin were 0.126 2-1.262 0 μg(r=0.999 9), 0.036 2-0.362 0 μg(r=0.999 9) and 0.177 9-1.779 4 μg(r=0.999 8), respectively. Quantitative limits were 25.4, 28.2, 62.5 ng, and detection limits were 6.2, 3.6, 11.8 ng, respectively. RSDs of precision, stability, repeatability and durability tests were all less than 3%. The recoveries ranged from 94.64%-102.71%(RSD=2.74%, n=9), 95.35%-102.49%(RSD=2.44%, n=9), 93.56%-103.66%(RSD=3.27%, n=9). The determination results showed that the contents of gallic acid and cinnamic acid in prepared R. officinale were higher, and the order of both were prepared R. officinale>steamed R. officinale>raw R. officinale. The content of catechin in raw R. officinale was higher, and the order of it was raw R. officinale> steamed R. officinale>prepared R. officinale. CONCLUSIONS: The method is sensitive, reliable and reproducible. It can be used to determine the contents of gallic acid, cinnamic acid and catechins in 3 processed products of R. officinale simultaneously.
5.Cause Analysis and Solution Strategy of Poor Solubility of Dioscoreae Rhizoma Formula Granules
Wei LIAO ; Dingkun ZHANG ; Zhiping GUO ; Shifa RUAN ; Chunli GE ; Jiabao LIAO ; Li HAN
Chinese Journal of Experimental Traditional Medical Formulae 2023;29(7):193-198
Dioscoreae Rhizoma formula granules are made from decoction pieces by decocting, extracting, separating, concentrating, drying and granulating, which have the advantages of simple dispensing, convenient use and easy to take without decoction. However, because Dioscoreae Rhizoma is rich in starch and mucus components, its extract powder and formula granules are poorly soluble and difficult to dissolve or disperse completely within 5 min, and the insoluble material is difficult to dissolve completely even after 24 h in water, which affects the quality evaluation of the formula granules and medication psychology of patients. Therefore, by studying the dissolution process and mechanism of Dioscoreae Rhizoma extract and its formula granules, it was found that the special chemical composition of Dioscoreae Rhizoma, the denaturation of starch and its compounding with protein and other substances during the high temperature extraction process, and the contraction of coating membrane during the spray drying process were combined to form the special microstructure of coating membrane covering starch granules, and it is the root cause of poor solubility of Dioscoreae Rhizoma formula granules. Based on the research on the structure, property and function of the powder, this paper proposed a technical strategy to improve the solubility of Dioscoreae Rhizoma formula granules by powder modification process, and experimentally demonstrated that the modified Dioscoreae Rhizoma formula granules could completely dissolve within 2 min, which solved the technical problem and could provide reference for the improvement of solubility of other similar varieties, and promote the high-quality development of traditional Chinese medicine formula granule industry.