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provides coniferyl ferulate(CAS#:29554-26-5) MSDS, density, melting point, boiling point, structure, formula, molecular weight etc. Articles of coniferyl ferulate are included as well.>> amp version: coniferyl ferulate
Dihydrotestosterone is a more potent androgen than testosterone and plays an important role in endocrine function. We demonstrated that, like testosterone, dihydrotestosterone can be oxidized by human cytochrome P450 (P450) 19A1, the steroid aromatase. The products identified include the 19-hydroxy- and 19-oxo derivatives and the resulting Δ1,10-, Δ5,10-, and Δ9,10-dehydro 19-norsteroid products (loss of 19-methyl group). The overall catalytic efficiency of oxidation was ∼10-fold higher than reported for 3α-reduction by 3α-hydroxysteroid dehydrogenase, the major enzyme known to deactivate dihydrotestosterone. These and other studies demonstrate the flexibility of P450 19A1 in removing the 1- and 2-hydrogens from 19-norsteroids, the 2-hydrogen from estrone, and (in this case) the 1-, 5β-, and 9β-hydrogens of dihydrotestosterone. Incubation of dihydrotestosterone with human liver microsomes and NADPH yielded the 18- and 19-hydroxy products plus the Δ1,10-dehydro 19-nor product identified in the P450 19A1 reaction. The 18- and 19-hydroxylation reactions were attributed to P450 3A4, and 18- and 19-hydroxydihydrotestosterone were identified in human plasma and urine samples. The change in the pucker of the A ring caused by reduction of the Δ4,5 bond is remarkable in shifting the course of hydroxylation from the 6β-, 2β-, 1β-, and 15β-methylene carbons (testosterone) to the axial methyl groups (18, 19) in dihydrotestosterone and demonstrates the sensitivity of P450 3A4, even with its large active site, to small changes in substrate structure.
Cytochrome P450, Mass Spectrometry (MS), Metabolism, NMR, Oxidation-reduction, Steroid, Testosterone, Dihydrotestosterone
Oxidation of Dihydrotestosterone by Human Cytochromes P450 19A1 and 3A4*
Qian Cheng, Christal D. Sohl,1 Francis K. Yoshimoto, and F. Peter Guengerich2
2012 Aug 24
As in other countries of the Greater Mekong Sub-region (GMS), the private health sector constitutes a significant avenue where malaria services are provided and presents a unique opportunity for public-private collaboration. In September 2008, a public-private mix (PPM) strategy was launched initially in four northern and southern provinces in Lao PDR to increase access to rapid diagnostic tests (RDTs) and artemisinin-based combination therapy (ACT), improve quality of care, and collect routine malaria data from the private sector. Throughout the process, key stakeholders were involved in the planning, monitoring and supervision of project sites. Following an initial assessment in 2009, the PPM initiative expanded to an additional 14 district sites to a total of 245 private pharmacies and 16 clinics covering 8 provinces and 22 districts. By June 2016, a total of 317 pharmacies, 30 clinics in 32 districts of the 8 provinces were participating in the PPM network and reported monthly malaria case data.
This descriptive study documented the process of initiating and maintaining the PPM network in Lao PDR. Epidemiological data reported through the routine surveillance system from January 2009 to June 2016 were analyzed to illustrate the contribution of case reporting from the private sector.
A total of 2,301,676 malaria tests were performed in the PPM districts, which included all the PPM pharmacies and clinics (176,224, 7.7%), proportion of patients tested from 14,102 (4.6%) in 2009 to 29,554 (10.4%) in 2015. Over the same period of 90 months, a total of 246,091 positive cases (10.7%) were detected in PPM pharmacies and clinics (33,565; 13.6%), in the same districts as the PPM sites. The results suggest that the PPM sites contributed to a significant increasing proportion of patients positive for malaria from 1687 (7.4%) in 2009 to 5697 (15.8%) in 2015.
Ensuring adequate and timely supplies of RDTs and ACT to PPM sites is critical. Frequent refresher training is necessary to maintain data quality, motivation and feedback. In the context of malaria elimination, the PPM initiative should be expanded further to ensure that all febrile cases seen through the private sector in malaria transmission areas are tested for malaria and treated appropriately. Results from the PPM must be integrated into a centralized registry of malaria cases that should prompt required case and foci investigations and responses to be conducted as part of elimination efforts.
Public-private mix, Lao PDR, Malaria diagnosis, Treatment
Expanding malaria diagnosis and treatment in Lao PDR: lessons learned from a public-private mix initiative
Nouannipha Simmalavong,1 Sengkham Phommixay,1 Phoudaliphone Kongmanivong,1 Odai Sichanthongthip,1 Bouasy Hongvangthong,1 Deyer Gopinath,corresponding author2 and David M. Sintasath3
The total synthesis of amphidinolide B1 and the proposed structure of amphidinolide B2 has been accomplished. Key aspects of this work include the development of a practical, non-transition metal mediated method for the construction of the C13-C15 diene, the identification of α-chelation and dipole minimization models for diastereoselective methyl ketone aldol reactions, the discovery of a spontaneous Horner-Wadsworth-Emmons macrocyclization strategy and the development of a novel late stage method for construction of an allylic epoxide moiety. The originally proposed structure for amphidinolide B2 and diastereomers thereof display potent anti-tumor activities with IC50 values ranging from 3.3 nM to 94.5 nM against human solid and blood tumor cells. Of the different stereoisomers, the proposed structure of amphidinolide B2 is over 12-fold more potent than the C8,9-epimer and C18-epimer in human DU145 prostate cancer cells. These data suggest that the epoxide stereochemistry is a significant factor for anticancer activity.
Amphidinolide B: Total Synthesis, Structural Investigation and Biological Evaluation
Liang Lu,a Wei Zhang,a Sangkil Nam,b,† David A. Horne,b Richard Jove,b and Rich G. Cartercorresponding authora
2014 Mar 15.