Elevated protein kinase C alpha expression may be predictive of tamoxifen treatment failure

We previously reported that stable transfection of protein kinase C alpha (PKCα) into T47D human breast cancer cells results in tamoxifen (TAM)-resistant tumour growth. Relevance of PKCα expression in clinical specimens was determined by comparing PKCα expression in tumours from patients exhibiting disease recurrence with patients remaining disease-free following TAM treatment. Our results suggest that PKCα expression may predict TAM treatment failure

A rapid method for preparation of sarcolemma from frog skeletal muscle

A rapid method for the preparation of sarcolema from frog skeletal muscle has been described. The purified cell segments were transparent and devoid of contractile material. The Na+, K+ -ATPase and 5'-nucleotidase activities in sarcolemma purified by this method were comparable to those reported for sarcolemmal preparations purified by density gradient centrifugation. The preparation also possessed acid phosphatase, alkaline phosphatase and K+ -activated, ouabain-sensitive p-nitrophenyl phosphatase activities. The cholesterol to phospholipid ratio of the sarcolemma was 0.33, indicating its high purity; further, the preparation was free from mitochondria and contractile proteins

Solvent free hydroxylation of the methyl esters of Blighia unijugata seed oil in the presence of cetyltrimethylammonium permanganate

Extraction of oil from the seed of Blighia unijugata gave a yield of 50.82 ± 1.20% using hexane in a soxhlet extractor. The iodine and saponification values were 67.60 ± 0.80 g iodine/100 g and 239.20 ± 1.00 mg KOH/g respectively with C18:1 being the dominant fatty acid. Unsaturated methyl esters of Blighia unijugata which had been previously subjected to urea adduct complexation was used to synthesize methyl 9, 10-dihydroxyoctadecanoate via hydroxylation in the presence of cetyltrimethylammonium permanganate (CTAP). The reaction was monitored and confirmed using FTIR and GC-MS. This study has revealed that oxidation reaction of mono unsaturated bonds using CTAP could be achieved under solvent free condition

Simultaneous Comparison of Many Triphasic Defibrillation Waveforms

Biphasic defibrillation waveforms are now accepted as being more effective at terminating ventricular fibrillation (VF) than monophasic waveforms. If two phases are better than one, this naturally leads to the hypothesis that additional phases improve efficacy. This study tests the hypothesis by adding one additional phase. We examined the efficacy of 18 different triphasic waveforms simultaneously

Cycloreversion of beta-lactams via photoinduced electron transfer

The radical anions of beta-lactams, photogenerated in the presence of DABCO as an electron donor, undergo cycloreversion via N-C4 bond cleavage, back electron transfer and final C2-C3 bond cleavage, leading to olefins. The involved intermediates are 1,4-radical anions and 1,4-biradicals. The experimental observations are consistent with the results of DFT calculations.Financial support from the Spanish Government (CTQ2013-47872-C2-1-P, SEV-2012-0267, BES-2011-043706, JCI-2010-06204), from CSIC (JAEDOC 101-2011 co-funded by FSE) and from the Generalitat Valenciana (PROMETEOII/2013/005) is gratefully acknowledged. J. A. S. acknowledges the computational facilities provided by the Theoretical Computational Chemistry Group of Prof. L. R. Domingo at the Universitat de Valencia.Pérez Ruiz, R.; Sáez Cases, JA.; Jiménez Molero, MC.; Miranda Alonso, MÁ. (2014). Cycloreversion of beta-lactams via photoinduced electron transfer. Organic and Biomolecular Chemistry. 12(42):8428-8432. https://doi.org/10.1039/c4ob01416bS842884321242Von Nussbaum, F., Brands, M., Hinzen, B., Weigand, S., & Häbich, D. (2006). Antibacterial Natural Products in Medicinal Chemistry—Exodus or Revival? Angewandte Chemie International Edition, 45(31), 5072-5129. doi:10.1002/anie.200600350β-Lactams in the New Millennium. Part-I: Monobactams and Carbapenems. (2004). Mini-Reviews in Medicinal Chemistry, 4(1), 69-92. doi:10.2174/1389557043487501β-Lactams in the New Millennium. Part-II: Cephems, Oxacephems, Penams and Sulbactam. (2004). Mini-Reviews in Medicinal Chemistry, 4(1), 93-109. doi:10.2174/1389557043487547Buynak, J. (2004). The Discovery and Development of Modified Penicillin- and Cephalosporin- Derived β-Lactamase Inhibitors. Current Medicinal Chemistry, 11(14), 1951-1964. doi:10.2174/0929867043364847Veinberg, G., Vorona, M., Shestakova, I., Kanepe, I., & Lukevics, E. (2003). Design of β-Lactams with Mechanism Based Nonantibacterial Activities. Current Medicinal Chemistry, 10(17), 1741-1757. doi:10.2174/0929867033457089Chemistry and Biology of β-Lactam Antibiotics , ed. R. B. Morin and M. Gorman , Academic Press , New York , 1982 , pp. 1–3Nathwani, D., & Wood, M. J. (1993). Penicillins. Drugs, 45(6), 866-894. doi:10.2165/00003495-199345060-00002Fischer, M. (1968). Photochemische Reaktionen, IV. Photochemische Fragmentierungen von β-Lactamen. Chemische Berichte, 101(8), 2669-2678. doi:10.1002/cber.19681010809Fabre, H., Ibork, H., & Lerner, D. A. (1994). Photoisomerization Kinetics of Cefuroxime Axetil and Related Compounds. Journal of Pharmaceutical Sciences, 83(4), 553-558. doi:10.1002/jps.2600830422Rossi, E., Abbiati, G., & Pini, E. (1999). Substituted 1-benzyl-4-(benzylidenimino)-4-phenylazetidin-2-ones: Synthesis, thermal and photochemical reactions. 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Kinetics of Fluorescence Quenching by Electron and H-Atom Transfer. Israel Journal of Chemistry, 8(2), 259-271. doi:10.1002/ijch.197000029Kavarnos, G. J., & Turro, N. J. (1986). Photosensitization by reversible electron transfer: theories, experimental evidence, and examples. Chemical Reviews, 86(2), 401-449. doi:10.1021/cr00072a005Gandon, V., Bertus, P., & Szymoniak, J. (2000). A Straightforward Synthesis of Cyclopropanes from Aldehydes and Ketones. European Journal of Organic Chemistry, 2000(22), 3713-3719. doi:10.1002/1099-0690(200011)2000:223.0.co;2-1Wang, S. C., Troast, D. M., Conda-Sheridan, M., Zuo, G., LaGarde, D., Louie, J., & Tantillo, D. J. (2009). Mechanism of the Ni(0)-Catalyzed Vinylcyclopropane−Cyclopentene Rearrangement. The Journal of Organic Chemistry, 74(20), 7822-7833. doi:10.1021/jo901525uKashima, C., Fukusaka, K., & Takahashi, K. (1997). Synthesis of optically active β-lactams by the reaction of 2-acyl-3-phenyl-l-menthopyrazoles with CN compounds. Journal of Heterocyclic Chemistry, 34(5), 1559-1565. doi:10.1002/jhet.5570340529Andreu, I., Delgado, J., Espinós, A., Pérez-Ruiz, R., Jiménez, M. C., & Miranda, M. A. (2008). Cycloreversion of Azetidines via Oxidative Electron Transfer. Steady-State and Time-Resolved Studies. Organic Letters, 10(22), 5207-5210. doi:10.1021/ol802181uBelger, C., Neisius, N. M., & Plietker, B. (2010). A Selective Ru-Catalyzed Semireduction of Alkynes to Z Olefins under Transfer-Hydrogenation Conditions. Chemistry - A European Journal, 16(40), 12214-12220. doi:10.1002/chem.201001143Eicher, T., Böhm, S., Ehrhardt, H., Harth, R., & Lerch, D. (1981). Zur Reaktion von Diphenylcyclopropenon, seinen funktionellen Derivaten und Imoniumsalzen mit Aminen. Liebigs Annalen der Chemie, 1981(5), 765-788. doi:10.1002/jlac.198119810503Mazzocchi, P. H., & Thomas, J. J. (1972). Photolysis of N-methyl-2-pyrrolidone. Journal of the American Chemical Society, 94(23), 8281-8282. doi:10.1021/ja00778a085Platz, M. 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Prostate-specific antigen and hormone receptor expression in male and female breast carcinoma

<p>Abstract</p> <p>Background</p> <p>Prostate carcinoma is among the most common solid tumors to secondarily involve the male breast. Prostate specific antigen (PSA) and prostate-specific acid phosphatase (PSAP) are expressed in benign and malignant prostatic tissue, and immunohistochemical staining for these markers is often used to confirm the prostatic origin of metastatic carcinoma. PSA expression has been reported in male and female breast carcinoma and in gynecomastia, raising concerns about the utility of PSA for differentiating prostate carcinoma metastasis to the male breast from primary breast carcinoma. This study examined the frequency of PSA, PSAP, and hormone receptor expression in male breast carcinoma (MBC), female breast carcinoma (FBC), and gynecomastia.</p> <p>Methods</p> <p>Immunohistochemical staining for PSA, PSAP, AR, ER, and PR was performed on tissue microarrays representing six cases of gynecomastia, thirty MBC, and fifty-six FBC.</p> <p>Results</p> <p>PSA was positive in two of fifty-six FBC (3.7%), focally positive in one of thirty MBC (3.3%), and negative in the five examined cases of gynecomastia. PSAP expression was absent in MBC, FBC, and gynecomastia. Hormone receptor expression was similar in males and females (AR 74.1% in MBC vs. 67.9% in FBC, p = 0.62; ER 85.2% vs. 68.5%, p = 0.18; and PR 51.9% vs. 48.2%, p = 0.82).</p> <p>Conclusions</p> <p>PSA and PSAP are useful markers to distinguish primary breast carcinoma from prostate carcinoma metastatic to the male breast. Although PSA expression appeared to correlate with hormone receptor expression, the incidence of PSA expression in our population was too low to draw significant conclusions about an association between PSA expression and hormone receptor status in breast lesions.</p

Serum immunoglobulin G, M and A response to Cryptosporidium parvum in Cryptosporidium-HIV co-infected patients

<p>Abstract</p> <p>Background</p> <p><it>Cryptosporidium parvum</it>, the protozoan parasite, causes a significant enteric disease in immunocompromised hosts such as HIV patients. The present study was aimed to compare serum IgG, IgM and IgA responses to crude soluble antigen of <it>C. parvum </it>in HIV seropositive and seronegative patients co-infected with <it>Cryptosporidium </it>and to correlate the responses with symptomatology.</p> <p>Methods</p> <p><it>Cryptosporidium parvum </it>specific serum antibody (IgG, IgM and IgA) responses were assessed by ELISA in 11 HIV seropositive <it>Cryptosporidium </it>positive (Group I), 20 HIV seropositive <it>Cryptosporidium </it>negative (Group II), 10 HIV seronegative <it>Cryptosporidium </it>positive (Group III), 20 HIV seronegative <it>Cryptosporidium </it>negative healthy individuals (Group IV) and 25 patients with other parasitic diseases (Group V).</p> <p>Results</p> <p>A positive IgG and IgA antibody response was observed in significantly higher number of <it>Cryptosporidium </it>infected individuals (Gp I and III) compared to <it>Cryptosporidium </it>un-infected individuals (Gp II, IV and V) irrespective of HIV/immune status. Sensitivity of IgG ELISA in our study was found to be higher as compared to IgM and IgA ELISA. The number of patients with positive IgG, IgM and IgA response was not significantly different in HIV seropositive <it>Cryptosporidium </it>positive patients with diarrhoea when compared to patients without diarrhoea and in patients with CD4 counts <200 when compared to patients with CD4 counts >200 cells/μl.</p> <p>Conclusion</p> <p>The study showed specific serum IgG and IgA production in patients infected with <it>Cryptosporidium</it>, both HIV seropositive and seronegative as compared to uninfected subjects suggesting induction of <it>Cryptosporidium </it>specific humoral immune response in infected subjects. However, there was no difference in number of patients with positive response in HIV seropositive or seronegative groups indicating that HIV status may not be playing significant role in modulation of <it>Cryptosporidium </it>specific antibody responses. The number of patients with positive IgG, IgM and IgA response was not significantly different in patients with or without history of diarrhoea thereby indicating that <it>Cryptosporidium </it>specific antibody responses may not be necessarily associated with protection from symptomatology.</p

Ring splitting of azetidin-2-ones via radical anions

The radical anions of azetidin-2-ones, generated by UV-irradiation in the presence of triethylamine, undergo ring-splitting via N-C4 or C3-C4 bond breaking, leading to open-chain amides. This reactivity diverges from that found for the neutral excited states, which is characterised by alpha-cleavage. The preference for beta-cleavage is supported by DFT theoretical calculations on the energy barriers associated with the involved transition states. Thus, injection of one electron into the azetidin-2-one moiety constitutes a complementary activation strategy which may be exploited to produce new chemistry.Financial support from the MICINN (Grants CTQ-2010-14882, CTQ-2009-13699 and JCI-2010-06204), Generalitat Valenciana (Prometeo 2008/90), from CSIC (JAEDOC 101-2011) and from the UPV (Grant No. 20100994 and MCI Program) is gratefully acknowledged.Pérez Ruiz, R.; Sáez Cases, JA.; Domingo, LR.; Jiménez Molero, MC.; Miranda Alonso, MÁ. (2012). Ring splitting of azetidin-2-ones via radical anions. Organic and Biomolecular Chemistry. 10(39):7928-7932. https://doi.org/10.1039/c2ob26528aS79287932103