Epoxy Compounds

Publication Title: 
Cell

Traditional medicines provide fertile ground for modern drug development, but first they must pass along a pathway of discovery, isolation, and mechanistic studies before eventual deployment in the clinic. Here, we highlight the challenges along this route, focusing on the compounds artemisinin, triptolide, celastrol, capsaicin, and curcumin.

Author(s): 
Corson, Timothy W.
Crews, Craig M.
Publication Title: 
Current Drug Discovery Technologies

Traditional Chinese Medicines (TCM) are rapidly gaining attention in the West as sources of new drugs, dietary supplements and functional foods. However, lack of consistent manufacturing practices and quality standards, fear of adulteration, and perceived deficiencies in scientific validation of efficacy and safety impede worldwide acceptance of TCM. In addition, Western pharmaceutical industries and regulatory agencies are partial toward single ingredient drugs based on synthetic molecules, and skeptical of natural product mixtures.

Author(s): 
Graziose, Rocky
Lila, Mary Ann
Raskin, Ilya
Publication Title: 
Phytochemistry

Plants in the genus Tripterygium, such as Tripterygium wilfordii Hook.f., have a long history of use in traditional Chinese medicine. In recent years there has been considerable interest in the use of Tripterygium extracts and of the main bioactive constituent, the diterpene triepoxide triptolide (1), to treat a variety of autoimmune and inflammation-related conditions.

Author(s): 
Brinker, Anita M.
Ma, Jun
Lipsky, Peter E.
Raskin, Ilya
Publication Title: 
Diabetes, Obesity & Metabolism

AIM: To elucidate the mechanism by which rosiglitazone regulates adipose triglyceride lipase (ATGL). METHODS: Male C57Bl/6 mice were treated with rosiglitazone daily (10 mg/kg body weight), and adipose tissues were weighed and preserved for mRNA and protein analysis of ATGL. In parallel, preadipocyte (3T3-L1) cells were differentiated with insulin/dexamethasone/3-isobutyl-1-methlxanthine cocktail or rosiglitazone, and ATGL levels were measured with real-time PCR, western blotting and immunohistochemistry.

Author(s): 
Liu, L.-F.
Purushotham, A.
Wendel, A. A.
Koba, K.
DeIuliis, J.
Lee, K.
Belury, M. A.
Publication Title: 
Current Drug Discovery Technologies

Traditional Chinese Medicines (TCM) are rapidly gaining attention in the West as sources of new drugs, dietary supplements and functional foods. However, lack of consistent manufacturing practices and quality standards, fear of adulteration, and perceived deficiencies in scientific validation of efficacy and safety impede worldwide acceptance of TCM. In addition, Western pharmaceutical industries and regulatory agencies are partial toward single ingredient drugs based on synthetic molecules, and skeptical of natural product mixtures.

Author(s): 
Graziose, Rocky
Lila, Mary Ann
Raskin, Ilya
Publication Title: 
Journal of Immunology (Baltimore, Md.: 1950)

Triptolide is a biologically active component purified from Chinese herbal plant Tripterygium wilfordii Hook F. It is widely used in East Asia for treatment of systemic lupus erythematosus, rheumatoid arthritis, nephritis, Bechect's disease, psoriasis, atopic dermatitis, and asthma. However, its immunological mechanisms are poorly understood. IL-12 and IL-23 are closely related heterodimeric cytokines that share the common subunit p40. They are produced by APCs and are key factors in the generation and effector functions of Th1 and Th17 cells, respectively.

Author(s): 
Zhang, Yan
Ma, Xiaojing
Publication Title: 
Journal of Magnetic Resonance (San Diego, Calif.: 1997)

For mass-limited samples, the residual sample volume outside the detection coil is an important concern, as is good base line resolution. Here, we present the construction and evaluation of magnetic susceptibility-matched plugs for microcoil NMR sample cells which address these issues. Mixed-epoxy glue and ultem tube plugs that have susceptibility values close to those of perfluorocarbon FC-43 (fluorinert) and copper were used in small volume (0.5-2 microL) and larger volume (15-20 microL) thin glass capillary sample cells. Using these plugs, the sample volume efficiency (i.e.

Author(s): 
Kc, Ravi
Gowda, Yashas N.
Djukovic, Danijel
Henry, Ian D.
Park, Gregory H. J.
Raftery, Daniel
Publication Title: 
Zhongguo Yao Li Xue Bao = Acta Pharmacologica Sinica

Triptolide (Tri) is an active principle of Tripterygium hypoglaucum Hutch, which has been used to treat cancers and autoimmune diseases in folk medicine. The lymphocyte proliferation (LP) induced by Con A or Lipopolysaccharide (LPS) was suppressed by Tri at 50 and 500 ng/ml. At 5 ng/ml the suppressive effect on LP induced by Con A was much stronger than that by LPS. The humoral immune reaction monitored by quantitative hemolysis spectrophotometry (QHS) was suppressed by Tri 0.75 and 1 mg/kg ip.

Author(s): 
Pu, L. X.
Zhang, T. M.
Publication Title: 
The Journal of Nutrition

Hemoglobin adducts of acrylamide (HbAA) and glycidamide (HbGA) have been measured as biomarkers of acrylamide exposure and metabolism in a nationally representative sample of the U.S. population in the NHANES 2003-2004. We assessed the association of sociodemographic (age, sex, race-ethnicity, education, and income) and lifestyle (smoking, alcohol consumption, BMI, physical activity, and dietary supplement use) variables with these biomarkers in U.S. adults (aged ≥ 20 y).

Author(s): 
Vesper, Hubert W.
Sternberg, Maya R.
Frame, Tunde
Pfeiffer, Christine M.
Publication Title: 
Investigative Ophthalmology & Visual Science

PURPOSE: Extracts of the herb Tripterygium wilfordii hook f, the major component of which is triptolide, have been used in traditional Chinese medicine for the treatment of rheumatoid arthritis. Triptolide also exerts many other biological actions both in vitro and in vivo. The effect of this agent on collagen degradation by cultured corneal fibroblasts was examined. METHODS: Rabbit corneal fibroblasts were cultured in three-dimensional gels of type I collagen and in the absence or presence of interleukin (IL)-1beta or triptolide.

Author(s): 
Lu, Ying
Fukuda, Ken
Seki, Keisuke
Nakamura, Yoshikuni
Kumagai, Naoki
Nishida, Teruo

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