2,6,16-Kauranetriol

Efficient Synthesis of 1,9-Substituted Benzo[h][1,6]naphthyridin-2(1H)-ones and Evaluation of their Plasmodium falciparum Gametocytocidal Activities.[Pubmed:29024590]

ACS Comb Sci. 2017 Dec 11;19(12):748-754.

A novel three-component, two-step, one-pot nucleophilic aromatic substitution (SNAr)-intramolecular cyclization-Suzuki coupling reaction was developed for the synthesis of benzo[h][1,6]naphthyridin-2(1H)-ones (Torins). On the basis of the new efficiently convergent synthetic route, a library of Torin analogs was synthesized. The antimalarial activities of these compounds were evaluated against asexual parasites using a growth inhibition assay and gametocytes using a viability assay.

Synthesis and Antimicrobial Evaluation of Fire Ant Venom Alkaloid Based 2-Methyl-6-alkyl-Delta(1,6)-piperideines.[Pubmed:29023124]

J Nat Prod. 2017 Oct 27;80(10):2795-2798.

The first synthesis of 2-methyl-6-pentadecyl-Delta(1,6)-piperideine (1), a major alkaloid of the piperideine chemotype in fire ant venoms, and its analogues, 2-methyl-6-tetradecyl-Delta(1,6)-piperideine (2) and 2-methyl-6-hexadecyl-Delta(1,6)-piperideine (3), was achieved by a facile synthetic method starting with glutaric acid (4) and urea (5). Compound 1 showed in vitro antifungal activity against Cryptococcus neoformans and Candida albicans with IC50 values of 6.6 and 12.4 mug/mL, respectively, and antibacterial activity against vancomycin-resistant Enterococcus faecium with an IC50 value of 19.4 mug/mL, while compounds 2 and 3 were less active against these pathogens. All three compounds strongly inhibited the parasites Leishmania donovani promastigotes and Trypanosoma brucei with IC50 values in the range of 5.0-6.7 and 2.7-4.0 mug/mL, respectively.

Social vulnerabilities as determinants of overweight in 2-, 4- and 6-year-old Spanish children.[Pubmed:29020368]

Eur J Public Health. 2018 Apr 1;28(2):289-295.

Background: Differences in obesity prevalence among vulnerable groups exist in childhood but it remains unclear whether these differences may be partly determined by socioeconomic status (SES), parental body mass index (BMI) and early life risk factors. We aimed to explore (i) longitudinal associations between belonging to a minority group and being overweight/obese at age 2, 4 and 6 and (ii) associations between accumulation of social vulnerabilities and being overweight/obese at age 6. Methods: In total, 1031 children (53.8% boys) were evaluated at birth and re-examined during a 6-year follow-up in a representative cohort of Aragon (Spain). Children from minority (vulnerable) groups included Spanish Roma/gypsies, Eastern Europeans, Latin Americans and Africans. Two more vulnerable groups were defined at baseline as children whose parents reported low occupation and education. Ethnicity, SES and parental BMI were collected via interviews. We used logistic mixed-effects models and adjusted for parental BMI, SES, mother's tobacco use, maternal weight gain, birth weight, infant weight gain and breastfeeding practices. Results: Regardless of confounders, Roma/gypsy children (OR = 4.63;[1.69-12.70]95%CI) and with Latin American background (OR = 3.04;[1.59-5.82]95%CI) were more likely to be overweight/obese at age 6 compared with non-gypsy Spanish group. Children with three vulnerabilities (OR = 2.18;[1.31-3.64]95%CI) were more likely to be overweight/obese at age 6 compared with children with no vulnerabilities. No associations were found between belonging to a minority group and overweight/obesity in children under 6. Conclusion: Interventions should target Roma/gypsy children, Latin American children and those who accumulate more vulnerabilities as they are at higher risk of being overweight/obese at age 6.

Characterization of immortalized human mammary epithelial cell line HMEC 2.6.[Pubmed:29022488]

Tumour Biol. 2017 Oct;39(10):1010428317724283.

Primary human mammary epithelial cells have a limited life span which makes it difficult to study them in vitro for most purposes. To overcome this problem, we have developed a cell line that was immortalized using defined genetic elements, and we have characterized this immortalized non-tumorigenic human mammary epithelial cell line to establish it as a potential model system. human mammary epithelial cells were obtained from a healthy individual undergoing reduction mammoplasty at SIU School of Medicine. The cells were transduced with CDK4R24C followed by transduction with human telomerase reverse transcriptase. Post all manipulation, the cells displayed a normal cell cycle phase distribution and were near diploid in nature, which was confirmed by flow cytometry and karyotyping. In vitro studies showed that the cells were anchorage dependent and were non-invasive in nature. The cell line expressed basal epithelial markers such as cytokeratin 7, CD10, and p63 and was negative for the expression of estrogen receptor and progesterone receptor. Upon G-band karyotyping, the cell line displayed the presence of a few cytogenic abnormalities, including trisomy 20 and trisomy 7, which are also commonly present in other immortalized mammary cell lines. Furthermore, the benign nature of these cells was confirmed by multiple in vitro and in vivo experiments. Therefore, we think that this cell line could serve as a good model to understand the molecular mechanisms involved in the development and progression of breast cancer and to also assess the effect of novel therapeutics on human mammary epithelial cells.