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1.
Fitoterapia ; 146: 104655, 2020 Oct.
Article in English | MEDLINE | ID: mdl-32502503

ABSTRACT

Two pairs of diastereoisomers (1/2 and 3/4) were isolated from the fruits of Rubus idaeus L. (Rosaceae). Their structures were elucidated on the basis of extensive spectroscopic analyses. Then chiral-phase HPLC resolution gave 1a/1b-4a/4b. Their absolute configurations were determined by comparison of the experimental ECD with the calculated data. Moreover, all isolated compounds were investigated for the neuroprotective effects against H2O2-induced neurotoxicity in human neuroblastoma SH-SY5Y cells, and 2a (66.04%) exhibited moderate neuroprotective effects, better than trolox (60.54%) at the concentration of 25 µM.


Subject(s)
Lignans/pharmacology , Neuroprotective Agents/pharmacology , Rubus/chemistry , Cell Line, Tumor , China , Fruit/chemistry , Humans , Lignans/isolation & purification , Molecular Structure , Neuroblastoma , Neuroprotective Agents/isolation & purification , Phytochemicals/isolation & purification , Phytochemicals/pharmacology
2.
J Nat Prod ; 82(10): 2696-2706, 2019 10 25.
Article in English | MEDLINE | ID: mdl-31556299

ABSTRACT

Fifteen new dihydro-ß-agarofuran-type sesquiterpenoids, tripterfordins A-O, were obtained from the aqueous EtOH extracts of the leaves of Tripterygium wilfordii. These constituted a class of highly oxygenated tricyclic sesquiterpenoid polyesters with a cinnamoyloxy group at C-1. The assignments of their structures were conducted via extensive analyses of the spectroscopic data and comparison of experimental and calculated ECD data. The absolute configurations of compounds 1, 4, 9, and 10 were established via single-crystal X-ray diffraction data. Additionally, compounds 1, 4, 9, 10, and 13 exhibited pronounced inhibitory effects on nitric oxide production in RAW 264.7 murine macrophages stimulated by lipopolysaccharide with IC50 values ranging from 11.9 to 31.0 µM.


Subject(s)
Sesquiterpenes/isolation & purification , Tripterygium/chemistry , Animals , Mice , Nitric Oxide/biosynthesis , Plant Extracts/analysis , Plant Leaves/chemistry , RAW 264.7 Cells , Sesquiterpenes/chemistry , Sesquiterpenes/pharmacology
3.
Mol Cancer Ther ; 10(6): 1082-92, 2011 Jun.
Article in English | MEDLINE | ID: mdl-21518728

ABSTRACT

Interleukin-2 (IL-2) has been shown to possess antitumor activity in numerous preclinical and clinical studies. However, the short half-life of recombinant IL-2 protein in serum requires repeated high-dose injections, resulting in severe side effects. Although adenovirus-mediated IL-2 gene therapy has shown antitumor efficacy, the host antibody response to adenoviral particles and potential biosafety concerns still obstruct its clinical applications. Here we report a novel nanopolymer for IL-2 delivery, consisting of low molecular weight polyethylenimine (600 Da) linked by ß-cyclodextrin and conjugated with folate (named H1). H1 was mixed with IL-2 plasmid to form H1/pIL-2 polyplexes of around 100 nm in diameter. Peritumoral injection of these polyplexes suppressed the tumor growth and prolonged the survival of C57/BL6 mice bearing B16-F1 melanoma grafts. Importantly, the antitumor effects of H1/pIL-2 (50 µg DNA) were similar to those of recombinant adenoviruses expressing IL-2 (rAdv-IL-2; 2 × 10(8) pfu). Furthermore, we showed that H1/pIL-2 stimulated the activation and proliferation of CD8+, CD4+ T cell, and natural killer cells in peripheral blood and increased the infiltration of CD8+, CD4+ Tcells, and natural killer cells into the tumor environment. In conclusion, these results show that H1/pIL-2 is an effective and safe melanoma therapeutic with an efficacy comparable to that of rAdv-IL-2. This treatment represents an alternative gene therapy strategy for melanoma.


Subject(s)
Immunotherapy/methods , Interleukin-2/administration & dosage , Melanoma, Experimental/immunology , Melanoma, Experimental/therapy , Nanoparticles/administration & dosage , Animals , CD4-Positive T-Lymphocytes/metabolism , CD8-Positive T-Lymphocytes/metabolism , Cell Line, Tumor , Drug Delivery Systems , Female , Folic Acid/chemistry , Humans , Interleukin-2/chemistry , Interleukin-2/genetics , Killer Cells, Natural/metabolism , Melanoma, Experimental/genetics , Melanoma, Experimental/metabolism , Mice , Mice, Inbred C57BL , Nanoparticles/chemistry , Polyethyleneimine/chemistry , Polymers/chemistry , Polymers/therapeutic use , T-Lymphocytes, Helper-Inducer/metabolism , Transgenes , beta-Cyclodextrins/chemistry
4.
World J Gastroenterol ; 15(24): 2987-94, 2009 Jun 28.
Article in English | MEDLINE | ID: mdl-19554651

ABSTRACT

AIM: To test whether oral L-81 treatment could improve the condition of mice with diabetes and to investigate how L-81 regulates microsomal triglyceride transfer protein (MTP) activity in the liver. METHODS: Genetically diabetic (db/db) mice were fed on chow supplemented with or without L-81 for 4 wk. The body weight, plasma glucose level, plasma lipid profile, and adipocyte volume of the db/db mice were assessed after treatment. Toxicity of L-81 was also evaluated. To understand the molecular mechanism, HepG2 cells were treated with L-81 and the effects on apolipoprotein B (apoB) secretion and mRNA level of the MTP gene were assessed. RESULTS: Treatment of db/db mice with L-81 significantly reduced and nearly normalized their body weight, hyperphagia and polydipsia. L-81 also markedly decreased the fasting plasma glucose level, improved glucose tolerance, and attenuated the elevated levels of plasma cholesterol and triglyceride. At the effective dosage, little toxicity was observed. Treatment of HepG2 cells with L-81 not only inhibited apoB secretion, but also significantly decreased the mRNA level of the MTP gene. Similar to the action of insulin, L-81 exerted its effect on the MTP promoter. CONCLUSION: L-81 represents a promising candidate in the development of a selective insulin-mimetic molecule and an anti-diabetic agent.


Subject(s)
Carrier Proteins/metabolism , Diabetes Mellitus, Experimental/drug therapy , Gene Expression Regulation/drug effects , Poloxamer , Surface-Active Agents , Animals , Carrier Proteins/genetics , Cell Line , Cholesterol/blood , Diabetes Mellitus, Experimental/metabolism , Diabetes Mellitus, Experimental/physiopathology , Drinking/drug effects , Eating/drug effects , Humans , Hypoglycemic Agents/pharmacology , Hypoglycemic Agents/therapeutic use , Liver/cytology , Liver/drug effects , Liver/metabolism , Male , Mice , Mice, Inbred C57BL , Poloxamer/pharmacology , Poloxamer/therapeutic use , Rosiglitazone , Surface-Active Agents/pharmacology , Surface-Active Agents/therapeutic use , Thiazolidinediones/pharmacology , Thiazolidinediones/therapeutic use , Triglycerides/blood , Weight Loss/drug effects
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