In the present study, a gastric retention floating system for Brucea javanica oil, composed of alginate and carrageenan, was prepared using ionotropic gelation. Parameters for floatability, drug load, encapsulation ef...In the present study, a gastric retention floating system for Brucea javanica oil, composed of alginate and carrageenan, was prepared using ionotropic gelation. Parameters for floatability, drug load, encapsulation efficiency, bead morphology, in vitro release, and in vivo gastric retention were evaluated. The optimized formulation via Box–Behnken design consisted of 1.7% alginate(W/V), 1.02% carrageenan(W/V), 1.4% CaCO_3(W/V), and a gelling bath of pH 0.8. The alginate–carrageenan–Brucea javanica oil beads had a porous structure and exhibited up to 24 h of in vitro floatability with a load capacity of 45%–55% and an encapsulation efficiency of 70%–80%. A 6-h sustained release was observed in vitro. The beads had a prolonged gastric retention(> 60% at 6 h) in fasted rats, compared to non-floating beads(15% at 6 h), as measured by gamma scintigraphy with single-photon emission tomography/computed tomography(SPET/CT). In conclusion, the alginate–carrageenan–Brucea javanica oil system showed enhanced oil encapsulation efficiency, excellent floating and gastric retention abilities, and a favorable release behavior.展开更多
Results from the in vitro evaluation of the antiparasitaire activity of the aqueous extract, the 80% methanol extract and its fractions from the leaves of Brucea sumatrana against Trypanosoma brucei brucei, T. cruzi, ...Results from the in vitro evaluation of the antiparasitaire activity of the aqueous extract, the 80% methanol extract and its fractions from the leaves of Brucea sumatrana against Trypanosoma brucei brucei, T. cruzi, Leishmania infantum, the multidrug-resistant K1 and chloroquine-sensitive NF54 strains of Plasmodium falciparum indicated that all samples from the leaves extract presented interesting antiparasitaire activity at different extents. The 80% methanol extract, its chloroform acid, petroleum ether and 80% methanol soluble fractions and the aqueous extract exhibited strong activity against Trypanosoma b. brucei, T. cruzi, L. infantum and the multidrug-resistant K1 strain of P. falciparum with IC<sub>50</sub> values from <0.25 to 4.35 μg/ml as well as against chloroquine-sensitive NF54 strain of P. falciparum with IC<sub>50</sub> values ranging from <0.02 to 2.0.4 μg/ml. Most samples were cytotoxic against MRC-5 cell lines (0.2 <sub>50</sub>) < 34.24 μg/ml) and showed good selective effect against all tested parasites. In acute toxicity, the aqueous extract was found to be non-toxic and its LD<sub>50 </sub>was estimated to be greater than 5 g/kg. In addition, it did not significantly modify the concentration levels of some evaluated biochemical and hematological parameters in treated rats. These results constitute a scientific validation supporting and justifying the traditional use of the leaves of B. sumatrana for the treatment of malaria, sleeping sickness and at some extent Chagas disease.展开更多
The in vitro antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from Brucea sumatrana seeds were assessed against two Trypanosom...The in vitro antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from Brucea sumatrana seeds were assessed against two Trypanosoma (T. cruzi and T. brucei brucei), Leishmania infantum and chloroquine and pyrimethanine-resistant K1strain of P. falciparum and against MRC-5 cell-lines respectively. Results indicated that the 80% methanol extract showed a cytotoxic effect against MRC-5 cell lines with CC50 value of 0.54 μg/ml. It however exhibited pronounced and non selective activity against T. cruzi (IC50 = 1.52 μg/ml, SI = 0.03) and L. infantum (IC50 = 2.41 μg/ml, SI = 0.22). It however displayed pronounced and selective effect against T. brucei brucei (IC50 2.16) and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum (IC50 2.16). All soluble fractions and subfractions from the partition of the 80% methanol extract were found to exhibit an antiprotozoal activity with IC50 values ranging from T .cruzi, T. b. brucei, L. infantum and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values of 0.33, 81, 81 and >81 respectively. The chloroform soluble fraction rich in alkaloid was cytotoxic against MRC-5 cell lines (CC50 = 27.09 μg/ml) and showed good activity against T. b. brucei (IC50 = 8.36 and SI = 3.24) and moderate activity against T. cruzi, L. infantum and chloroquine-pyrimethane-resistant K1 strain of P. falciparum (20 50 50 = 1.55 and 0.43 μg/ml respectively), they however displayed pronounced antiprotozoal activity against T. cruzi, T. b. brucei and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values ranging from P. falciparum (SI = >6.2 and >1.72 respectively). These extracts however showed good and low activity respectively against L. infantum (IC50 = 24.05 and 6.82 μg/ml respectively).展开更多
Main observation and conclusion Quassinoids,a class of highly oxygenated triterpenes,have been isolated as bitter principles from the plants of Simaroubaceae family.Five new quassinoids,chouchunlactone A-E(1-5),and tw...Main observation and conclusion Quassinoids,a class of highly oxygenated triterpenes,have been isolated as bitter principles from the plants of Simaroubaceae family.Five new quassinoids,chouchunlactone A-E(1-5),and two known ones were identified from the root barks of Ailanthus altissima Swingle(Simaroubaceae).The chemical structures of the new compounds were deduced by spectroscopic data analyses,NMR calculations and DP4+probability analysis.The absolute configurations were defined by comparison of their experimental and calculated electronic circular dichroism(ECD)spectra data,and compounds 1-2 were further confirmed by single-crystal X-ray diffraction.Biologically,compound 5 showed potencies equivalent to sorafenib(IC50 value,9.70μmol·L–1)against HepG2 cells.The Hoechst 33342 staining,JC-1 fluorescent dye and Annexin V/PI analysis studies demonstrated that 5 can induce apoptosis and attenuate mitochondrial membrane potential(MMP)in HepG2 cells.展开更多
文摘研究臭椿Ailanthus altissima皮的化学成分。采用硅胶,Sephadex LH-20,ODS,HPLC等色谱方法,从臭椿干皮95%乙醇提取物中分离得到11个化合物,通过理化性质和波谱数据鉴定为木脂素类化合物,分别为(+)-新橄榄树脂素(1),prunustosanan AI(2),(7S,8R)-4,7,9,9'-四羟基-3,3'-二甲氧基-8-O-4'-新木脂素(3),(7R,8S)-4,7,9,9'-四羟基-3,3'-二甲氧基-8-O-4'-新木脂素(4),(7S,8R)-1-(4-hydroxy-3-methoxyphenyl)-2-[4-(3-hydroxypropyl)-2,6-dimethoxyphenoxy]-1,3-propanediol(5),pinnatifidanin B V(6),pinnatifidanin B VI(7),(7R,7'R,7″S,8S,8'S,8″S)-4',4″-dihydroxy-3,3',3″,5-tetramethoxy-7,9':7',9-diepoxy-4,8″-oxy-8,8'-sesquineolignin-7″,9″-diol(8),hedyotol D(9),5-(2-propenyl)-7-methoxy-2-(3,4-methylenediovxyphenyl)benzofuran(10),(7R,8S,7'E)-guaiacyl-glycerol-β-O-4'-sinapyl ether(11)。化合物均为首次从该植物中分离得到。
基金supported by the National Natural Science Foundation of China(No.81303233)Foundation of Shanghai Science and Technology Committee(No.13401900300)Shanghai Municipal Commission of Health and Family Planning(No.20124074)
文摘In the present study, a gastric retention floating system for Brucea javanica oil, composed of alginate and carrageenan, was prepared using ionotropic gelation. Parameters for floatability, drug load, encapsulation efficiency, bead morphology, in vitro release, and in vivo gastric retention were evaluated. The optimized formulation via Box–Behnken design consisted of 1.7% alginate(W/V), 1.02% carrageenan(W/V), 1.4% CaCO_3(W/V), and a gelling bath of pH 0.8. The alginate–carrageenan–Brucea javanica oil beads had a porous structure and exhibited up to 24 h of in vitro floatability with a load capacity of 45%–55% and an encapsulation efficiency of 70%–80%. A 6-h sustained release was observed in vitro. The beads had a prolonged gastric retention(> 60% at 6 h) in fasted rats, compared to non-floating beads(15% at 6 h), as measured by gamma scintigraphy with single-photon emission tomography/computed tomography(SPET/CT). In conclusion, the alginate–carrageenan–Brucea javanica oil system showed enhanced oil encapsulation efficiency, excellent floating and gastric retention abilities, and a favorable release behavior.
文摘Results from the in vitro evaluation of the antiparasitaire activity of the aqueous extract, the 80% methanol extract and its fractions from the leaves of Brucea sumatrana against Trypanosoma brucei brucei, T. cruzi, Leishmania infantum, the multidrug-resistant K1 and chloroquine-sensitive NF54 strains of Plasmodium falciparum indicated that all samples from the leaves extract presented interesting antiparasitaire activity at different extents. The 80% methanol extract, its chloroform acid, petroleum ether and 80% methanol soluble fractions and the aqueous extract exhibited strong activity against Trypanosoma b. brucei, T. cruzi, L. infantum and the multidrug-resistant K1 strain of P. falciparum with IC<sub>50</sub> values from <0.25 to 4.35 μg/ml as well as against chloroquine-sensitive NF54 strain of P. falciparum with IC<sub>50</sub> values ranging from <0.02 to 2.0.4 μg/ml. Most samples were cytotoxic against MRC-5 cell lines (0.2 <sub>50</sub>) < 34.24 μg/ml) and showed good selective effect against all tested parasites. In acute toxicity, the aqueous extract was found to be non-toxic and its LD<sub>50 </sub>was estimated to be greater than 5 g/kg. In addition, it did not significantly modify the concentration levels of some evaluated biochemical and hematological parameters in treated rats. These results constitute a scientific validation supporting and justifying the traditional use of the leaves of B. sumatrana for the treatment of malaria, sleeping sickness and at some extent Chagas disease.
文摘The in vitro antiprotozoal and cytotoxic activity of the aqueous extract, the 80% methanol extract, and its different soluble fractions and subfractions from Brucea sumatrana seeds were assessed against two Trypanosoma (T. cruzi and T. brucei brucei), Leishmania infantum and chloroquine and pyrimethanine-resistant K1strain of P. falciparum and against MRC-5 cell-lines respectively. Results indicated that the 80% methanol extract showed a cytotoxic effect against MRC-5 cell lines with CC50 value of 0.54 μg/ml. It however exhibited pronounced and non selective activity against T. cruzi (IC50 = 1.52 μg/ml, SI = 0.03) and L. infantum (IC50 = 2.41 μg/ml, SI = 0.22). It however displayed pronounced and selective effect against T. brucei brucei (IC50 2.16) and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum (IC50 2.16). All soluble fractions and subfractions from the partition of the 80% methanol extract were found to exhibit an antiprotozoal activity with IC50 values ranging from T .cruzi, T. b. brucei, L. infantum and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values of 0.33, 81, 81 and >81 respectively. The chloroform soluble fraction rich in alkaloid was cytotoxic against MRC-5 cell lines (CC50 = 27.09 μg/ml) and showed good activity against T. b. brucei (IC50 = 8.36 and SI = 3.24) and moderate activity against T. cruzi, L. infantum and chloroquine-pyrimethane-resistant K1 strain of P. falciparum (20 50 50 = 1.55 and 0.43 μg/ml respectively), they however displayed pronounced antiprotozoal activity against T. cruzi, T. b. brucei and chloroquine and pyrimethamine-resistant K1 strain of P. falciparum with IC50 values ranging from P. falciparum (SI = >6.2 and >1.72 respectively). These extracts however showed good and low activity respectively against L. infantum (IC50 = 24.05 and 6.82 μg/ml respectively).
基金This work was financially supported by the National Natural Science Foundation of China(No.81872767)the Career Development Support Plan for the Young and Middle-aged Teachers in Shenyang Pharmaceutical University(No.ZQN2018006)+1 种基金the Pro ject funded by China Postdoctoral Science Foundation(No.2020M680987)the Project of Innovation Team(No.LT2015027)of Liaoning in China.
文摘Main observation and conclusion Quassinoids,a class of highly oxygenated triterpenes,have been isolated as bitter principles from the plants of Simaroubaceae family.Five new quassinoids,chouchunlactone A-E(1-5),and two known ones were identified from the root barks of Ailanthus altissima Swingle(Simaroubaceae).The chemical structures of the new compounds were deduced by spectroscopic data analyses,NMR calculations and DP4+probability analysis.The absolute configurations were defined by comparison of their experimental and calculated electronic circular dichroism(ECD)spectra data,and compounds 1-2 were further confirmed by single-crystal X-ray diffraction.Biologically,compound 5 showed potencies equivalent to sorafenib(IC50 value,9.70μmol·L–1)against HepG2 cells.The Hoechst 33342 staining,JC-1 fluorescent dye and Annexin V/PI analysis studies demonstrated that 5 can induce apoptosis and attenuate mitochondrial membrane potential(MMP)in HepG2 cells.
