Limonoids from seeds of Azadirachta indica and their cytotoxic activity / 中国中药杂志

Eight limonoids were isolated from 95% ethanol extracts of neem(Azadirachta indica) seeds by various chromatographic methods. By comparison of their spectroscopic data with those reported in the literatures, these limonoids were determined as salannin(1), 1-detigloyl-1-isobutylsalannin(2), salannol-3-acetate(3), salannol(4), spirosendan(5), 1-detigloyloxy-3-deacetylsalannin-1-en-3-one(6), nimbin(7) and 6-deacetylnimbin(8). Compounds 2 and 5 were firstly isolated from this genus and 5 represented the only example of its type. And 6 is a new natural product. 6 showed inhibitory activity against HeLa and HL-60 cells, with IC₅₀ of(21.61±4.37) and(27.33±5.74) μmol·L⁻¹, respectively. Both 7 and 8 mildly inhibited the growth of HeLa cells, with IC₅₀ of (33.15±5.24) and (38.56±6.41) μmol·L⁻¹, respectively.

Chemical constituents from Pteris dispar and their anti-tumor activity in vitro / 中国中药杂志

The dried whole plant of Pteris dispar were milled and extracted with 95% EtOH. The resulting dried extract was isolated by kinds of chromatographic column, including polyamide, Sephadex LH-20, preparative HPLC. As a result, ten diterpenes were isolated from the plant. By analyzing of ESI-MS and NMR spectroscopic data, the structures were established as geopyxin B(1), geopyxin E(2), ent-11α-hydroxy-18-acetoxykaur-16-ene(3), ent-14β-hydroxy-18-acetoxykaur-16-ene(4), neolaxiflorin L(5), ent-3β,19-dihydroxy-kaur-16-ene(6), ent-3β-hydroxy-kaur-16-ene(7), 7β,17-dihydroxy-16α-ent-kauran-19-oic acid 19-O-β-D-glucopyranoside ester(8), crotonkinin C(9)and crotonkinin C(10). Compounds 1-10 were obtained from P. dispar for the first time. Compounds 1 and 2 showed moderate activities against Bel-7402 with IC₅₀ values of 7.50 and 10.60 μmol•L⁻¹, and against HepG2 with IC₅₀ values of 6.68,11.80 μmol•L⁻¹, respectively.

Bioactive lignans from Silybum marianum / 中国中药杂志

The seeds of Silybum marianum were extracted by hot water, and the extract was isolated by D101 macroporous resin, MCI resin, MPLC, HPLC, et al. As a result, 7 compounds including tricin 4'-O-[threo-β-guaiacyl-(7″-O-methyl)-glyceryl] ether(1), tricin 4'-O-[erythro-β-guaiacyl-(7″-O-methyl)-glyceryl] ether(2), 5'-methoxyhydnocarpin-D(3),palstatin(4),(8R,7'S,8'R)-5,5'-dimethoxy-7-oxolariciresinol 9'-O-D-xylopyranoside(5), 9-O-D-glucopyranoside(6), and(-)-haplomyrtoside(7) were isolated and identified for the first time. Compounds 1, 3, 4, and 5 exhibited activity against influenza A(H5N1)with IC₅₀ value of 0.65, 0.21, 0.32, and 0.56 μmol•L⁻¹, respectively. Compounds 1, 2, 6, and 7 exhibited cytotoxity against HepG-2 with IC₅₀ value of 0.35, 0.25, 0.53, 0.66 μmol•L⁻¹, respectively.

Bioactive quinolizidine alkaloids from Sophora tonkinensis / 中国中药杂志

Twelve quinolizidine alkaloids were isolated from Sophora tonkinensis by means of silica gel, preparative MPLC, and preparative HPLC. On analysis of NMR spectroscopic data, their structures were established as 3-(4-hydroxyphenyl)-4-(3-methoxy-4-hydroxyphenyl)-3,4-dehydroquinolizidine(1), lanatine A(2), cermizines C(3), senepodines G(4), senepodines H(5), jussiaeiines A(6), jussiaeiines B(7),(+)-5α-hydroxyoxysophocarpine(8),(-)-12β-hydroxyoxysophocarpine(9),(-)-clathrotropine(10),(-)-cytisine(11), and (-)-N-methylcytisine(12), respectively. Compounds 1-7 were first isolated from Sophora L. plant. In the in vitro assays,the isolated compounds 1, 3, 6-10 exhibited potent activity against CVB3 with IC₅₀ of 6.40, 3.25, 4.66, 3.21, 0.12, 0.23 and 1.60, and with selective index values(SI=TC₅₀/IC₅₀)of 12.0, 5.6, 13.0, 15.1, 50.1, 26.2, and 23.6, respectively. Compounds 1, 3, and 7 exhibited activity against staphylococcus aureus(ATCC 29213)with MICvalues of 8.0, 3.5, 6.0 g•L⁻¹, respectively. Compounds 1, 3, 7, and 12 exhibited activity against staphylococcus aureus(ATCC 33591)with MIC values of 18.0, 7.5, 8.0, 12.0 g•L⁻¹, respectively. Compounds 2, 6, 7 exhibited activity against Escherichia coli(ATCC 25922) with MIC values of 1.0, 3.2, 0.8 g•L⁻¹.

Chemical constituents from Pteris multifida and cytotoxic activity / 中国中药杂志

The materials were extracted by 95% ethanol, and the extracting solution was isolated by kinds of chromatographic columns including polyamide, MCI, preparative MPLC, and preparative HPLC. Eight diterpenes and two sesquiterpenes were isolated from the plant. On analysis of ESI-MS and NMR spectroscopic data, the structures were established as ent-3β-hydroxy-kaur-16-en-19-al (1), 4-epi-kaurenic acid (2), mitrekaurenone (3), 7β,16α,17-trihydroxy-ent-kauran-19-oic acid (4), crotonkinin E (5), crotonkinin F (6), pterisolic acid A (7), pterisolic acid C (8), (2R)-pterosin P (9), and dehydropterosin B (10). Compounds 1-6 were obtained from Pteris for the first time, and compounds 7-10 were obtained from P. ensiformis for the first time. Compounds 5-8 showed moderate activity against HCT-116, HepG2 and BGC-823 cell lines, separately.

Effect of α-GalCer-activated natural killer T cell on survival of allograft with high-risk rejection after retrobubar injection / 中华实验眼科杂志

BackgroundCorneal graft reject is a major cause of corneal transplantation failure.Although many immune-suppressing drugs have been utilized to reduce the reject response,their adverse effects on organ and tissue are still insoluble.The tolerance induction of natural killer T (NKT) cells is currently under investigation.However,the study on the application of NKT cells in high risk corneal transplantation is seldom.ObjectiveThe present study was to explore the effects of α-GalCer-activated NKT cella on allografts survival after high-risk corneal transplantation surgery via retro-bubar injection.Methods The lymphocytes were picked up from the spleen of SPF Lewis rats and cultured in RPMI 1640 medium with 100 mg/L α-GalCer.After one week,NKT cells were sorted by the FACSVantage system as CD161+ TCR-α+ cell from the lymphocytes with the cell densities 5×106/ml.Ten SPF Fisher344 rats were used to prepare the donor corneas,and 20 Lewis rats served as recipients.The high risk corneal transplantation models were created by corneal suturing in 20 recipient rats.Penetrating keratoplasty (PKP) was performed in the model rats.0.1 ml NKT cells or the same volume of normal saline solution were retro-bubarly injected at the end of surgery respectively.The corneal allografts were observed and scored based on Holland criteria at the three-day interval under the slit lamp for 30 days.Two weeks after surgery,three rats from each group were sacrificed by excessive anesthesia method and the eyeballs were obtained for histopathological examination.The inflammatory cell infiltration ( CD4+ and CD8+ ) in grafts was evaluated by immunochemistry and flow cytometry.The use of the animals complied with the Statement of ARVO.ResultsThe mean survival time of the allografts was (7.90± 1.37) days in normal saline solution group and (14.70± 1.49) days in NKT cell group,showing a statistically significant difference between the two groups ( t =10.61,P =0.00 ).Two weeks after surgery,all the allografts showed the severe opacity with lots of new blood vessels and edema in normal saline solution group.However,the corneal grafts were clear in NKT cell group.Abundant CD4+ and CD8+T lymphocytes were seen in the allografts in normal saline solution group,but the inflammatory cells were obviously less in NKT cell group.The percentage of NKT cells in the spleen was (5.67±0.25)％ in NKT cell group and ( 1.21±0.19)％ in normal saline solution group ( t =8.43,P =0.00 ).Conclusionsα-GalCer-activated NKT cells can prolong the survival time of allografts in high-risk corneal transplantation.Retro-bubar injection of α-GalCer-activated NKT cells probably is a new approach to the prevention of the rejection of corneal transplantation.

Review on investigations related to chemical constituents and biological activities of Periplaneta americana / 中国中药杂志

With the fast development of medicinal animals as new drugs, research on Periplaneta americana become hot recently. Several drugs which mainly consisted of P. americana were approved for clinical applications. The chemical constituents and pharmacological bioactivities of this insect were summarized herein, which provides informativon for further researches on this medicinal animal.

Efficacy of olanzapine combined with fluoxetine in treatment of depression / 中国基层医药

Objective To explore the efficacy of low dosage of olanzapine combined with fluoxetine in the treatment of depression.Methods A 8-week study was conducted in 130 patients met the diagnostic criteria for de- pression.Subjects were randomly assigned to two groups:fluoxetine(20mg/d)alone and olanzapine(2.5～5 mg/d) plus fluoxetine(20mg/d).They were evaluated with Hamilton depression scale(HAMD).Hamilton anxiety scale (HAMA)at baseline,the 1 week,2 weeks,4 weeks and 8 weeks subsequently.Results(1)There were significant differences in the total scores and reduction rates of HAMD between two groups in every interview.(2)The combi- nation group had greater reduction in depressive and anxiety symptoms than that in fluoxetine group.(3)The re- sponse rate in combination group was higher than that of fluoxetine group in 1 week,2 weeks and 4 weeks.There were no significant differences in response and remission rate between combination group and fluoxetine group.Con- clusion The combination of olanzapine with fluoxetine demonstrated a rapid,effective antidepressant action.