Med. Sci., Volume 3, Issue 4 (December 2015) – 4 articles , Pages 93-137

This study examined how the 1199G > A polymorphism in the ABCB1 gene encoding P-glycoprotein (P-gp) affects the protein’s expression, ATPase activity, and ability to pump female steroid sex hormones out of LLC-PK1 cells. The ABCB1 (1199G) or ABCB1 (1199A) allele was transfected into cells, which were incubated for 48 h with various hormone concentrations, then analyzed by Western blotting to examine expression of P-gp protein and by reverse transcription-polymerase chain reaction (RT-PCR) to examine expression of mRNA. Cells were also compared in terms of their transepithelial permeability to steroid sex hormones in the presence and absence of the specific P-gp inhibitor GF120918. P-gp ATPase activity induced by steroid sex hormones was also assayed. Estriol and ethynyl estradiol up-regulated levels of ABCB1 mRNA in a concentration-dependent manner, with ABCB1 (1199A) mRNA showing greater up-regulation than ABCB1 (1199G) mRNA. Estrone, estriol, and ethynyl estradiol were substrates of both types of P-gp in transepithelial permeability assays, and the ABCB1 (1199A) protein showed a significantly higher net efflux ratio for estrone (13.4 vs. 7.4, p < 0.005), estriol (5.6 vs. 3.3, p < 0.05), and ethynyl estradiol (12.7 vs. 5.3, p < 0.005). Induction of P-gp ATPase activity by ethynyl estradiol and progesterone increased with increasing hormone concentration, and the magnitude of stimulation was greater for ABCB1 (1199A) P-gp than for ABCB1 (1199G) P-gp. These results indicate that the ABCB1 (1199G > A) polymorphism influences steroid sex hormone-induced expression and function of P-gp, which may help to explain inter-patient differences in P-gp-mediated chemotherapy resistance in vivo. Full article

A dry sample of Nostoc commune from an organic farm in Pingtung city (Taiwan) was used to prepare polysaccharide-rich (NCPS) extract. The conditioned medium (CM) from NCPS-treated human peripheral blood (PB)-mononuclear cells (MNC) effectively inhibited the growth of human leukemic U937 cells and triggered differentiation of U937 monoblast cells into monocytic/macrophagic lines. Cytokine levels in MNC-CMs showed upregulation of granulocyte/macrophage-colony stimulatory factor and IL-1β and downregulation of IL-6 and IL-17 upon treatment with NCPS. Moreover, murine macrophage RAW264.7 cells treated with NCPS exhibited the stimulatory effects of nitric oxide and superoxide secretion, indicating that NCPS might activate the immunity of macrophages. Collectively, the present study demonstrates that NCPS from N. commune could be potentially used for macrophage activation and consequently inhibited the leukemic cell growth and induced monocytic/macrophagic differentiation. Full article

Dennettia tripetala (commonly known as Pepperfruit) is widely consumed by the inhabitants of West Africa due to its distinctive spicy taste. It is also used traditionally as a remedy for cough, fever, toothache, diabetes, and nausea. The highly nutritious fruit is rich in protein, carbohydrates, as well as the antioxidant vitamins A, C, and E. The plant possesses phytochemicals that have been shown to elicit antimicrobial, insecticidal, analgesic, and anti-inflammatory properties. The plant has also been shown to possess chemotherapeutic, antihyperglycemic, and antioxidant properties. In addition, D. tripetala finds application in food preservation and seasoning. This review is the first attempt to pool together scientific evidence for the ethnomedicinal uses of D. tripetala. A critique of the literature is provided, as well as suggestions for future studies that can pave the way for further discoveries on the medicinal effects of D. tripetala. Full article

A large number of drugs are introduced every year, and newer interactions between medications are increasingly reported. Clinically significant drug interactions can occur when two or more drugs are taken in combination. With the continuing increase in the list of drugs capable of interactions, detection of these interactions from prescriptions becomes more important to ensure effective patient care. The aim of this study is to identify the possible drug interactions in the prescriptions of diabetic inpatients and to make physicians aware of these interactions to prevent the occurrence of clinically adverse effects. In a specially designed and validated data entry format, data for the following criteria were collected: drugs prescribed, major drug class prescribed, pharmacological classification of the observed drug interaction, and frequently occurring drug interactions. All the possible drug interactions were identified and evaluated using standard drug interaction reference books and databases. During the study period, 50 prescriptions of diabetic inpatients were screened randomly. Out of these prescriptions, 35 (70%) prescriptions had at least one possible drug-drug interaction. The major classes of drugs causing interactions included cardiac drugs (92%), analgesic drugs (66%), antibiotic drugs (52%), antidiabetic drugs (26%), diuretic drugs (26%), and antipsychotic drugs (24%). This study showed that 34 (68%) of the above prescriptions had minor interactions, 33(66%) had moderate interactions, and 10 (20%) had severe interactions. Of these, the drugs prescribed specifically for diabetes caused only nine moderate interactions. Thus, screening of prescriptions by the clinical pharmacist will help to minimize clinical occurrence of major/severe drug interactions in diabetic patients. Full article