1.Progress in oral drug-loaded nano-system
Zhiying DING ; Yue ZHANG ; Yaru DIAO ; Jihong CHI ; Yulin HU
Chinese Journal of Biochemical Pharmaceutics 2016;36(6):30-32
Oral drug-loaded nano-system include nano-gel drug delivery system, nano-suspension drug delivery system, nano-particle drug delivery system, liposomes drug delivery system, nano-micelles drug delivery system, alcohol liposoms,nano-framework drug delivery system, nano-emulsions drug delivery system, nano-self assembly drug delivery system.These nano-drug delivery systems can serve as multi-functional drug carriers.They may significantly improve the physicochemical and stabilization and biological properties of the free drug, enhance the therapeutic efficiency and reduce toxic side effects.This paper reviews the recent research progress in oral drug-loaded nano-systems.
2.Physicochemical properties of a polysaccharide RAP-B-1 from Rubus amabilis and its immunomodulating effects
Yulin DIAO ; Hao MA ; Jinwei REN ; Guiqiang ZHANG ; Shuai LI ; Junjie SHAN ; Bin LIU
Journal of International Pharmaceutical Research 2014;(4):461-467
Objective To investigate the physicochemica l properties and immunobiological activity of a polysaccharide (RAP-B-1) from stems of Rubus amabilis. Methods The crude polysaccharide (RAP) was obtained successively by boiling, ethanol precipitating and dialyzing. RAP was isolated with DEAE-cellulose and Sephadex G-100 to obtain a polysaccharide RAP-B-1. The physicochemical properties of RAP-B-1 were studied by hydrolysis, periodate oxidation, Smith degradation and methylation, CE, IR, NMR and GC-MS. The immunobiological activities were estimated by the proliferative activity of spleen lymphocytes and phagocytic activity of peritoneal macrophages in mice. Results The molecular weight of RAP-B-1 was 4.80×104 with specific optical rotation value [α] 20D+68.3 (c=1,H2O), and was composed of eight monosaccharides. The molar ratios were as Xyl: Ara: Glc: Rha:Gal: Man: GlcA: GalA = 1.0:6.9:0.8:1.1:6.9:0.3:0.5:3.3. RAP-B-1 was an arabinogalactan. The linkages of arabinose were →1) Ara (2,3→,→1) Ara(5→and→1) Ara, and the linkages of galactose were→1) Gal(4→,→1) Gal(6→and→1) Gal. RAP-B-1 could improve the proliferative activity of spleen T cells(P<0.05) and booste phagocytic activity of peritoneal macrophages at 50μg/ml concentration(P<0.01). Conclusion RAP-B-1 is an arabinogalactan and has immunobiological activity.
3.Determination and isolation of chemical constituents from the dried stems of Rubus amabilis Focke
Yulin DIAO ; Dongqing ZHU ; Bin LIU
Journal of Beijing University of Traditional Chinese Medicine 2017;40(10):864-871
Objective To study the chemical constituents from the dried stems of Rubus amabilis (Focke).Method The chemical constituents of R.amabilis were extracted with boiled water,then isolated and purified with various chromatographic columns including silica gel,reversed phase and gelatin chromatography and crystallization methods.The structure was identified by using different spectroscopic and chromatographic techniques including nuclear magnetic resonance and mass spectrum.The liquid chromatography-mass spectrometry-ion trap-time of flight (LC/MS-IT-TOF)method was also applied to analyze the ingredients.The chromatographic separation was performed on SunFireTM C18 column (4.6 mm x 150 mm,5 μm) with gradient elution of methanol (A)-0.5%formic acid aqueous solution (B).Multistage mass spectrometry data of different compounds was obtained by using electrospray ionization source and monitoring in positive and negative ion modes.Results There were 5 chemical constituents isolated from the plant including 1,2,8-trimethoxy-6-hydroxyxanthone,2α,3α,19α,23-tetraydroxy-urs-12-en-28-oic acid,oleanolic acid,(+)-catechin and (-)-epicatechin.Twenty-seven compounds including 5 diterpenoids,1 monoterpenoid,1 xanthone,11 flavones and 9 triterpenoids were identified based on the characteristic MS/MS fragment ions data with chemical standards and published literatures.These constituents were determined to be 1-hydroxyl-3,7,8-trimethoxylxanthone,7-epiphlomiol,ent-kaur-16-ene-9-ol,ent-16β,17-dihydroxy-kauran-19-oic acid,ent-kauran-3α (β),16β,17-triol,rubusoside,rubusoside B,pinfaenoic acid,isopinfaenoic acid,19α-hydroxylursolic acid,2α,19α-dihydroxyl-ursan-12-en-28-oic acid,2α-hydroxylursolic acid,2α,3α-dihydroxyl-oleanan-12-en-28-oic acid,camelliagenin A,camelliagenin C,tormentic acid,procyanidin B1-B8,isoquercitrin,quercetin and kumata kenin.Conclusion Compound 1 was isolated from Rosaceae for the first time.Compounds 20 and 21 were obtained from Rubus firstly.The rest constituents were firstly found from the plant.