Sastav eteričnog ulja biljke Teucrium scordium L.

Composition of the essential oil obtained from dried flowering aerial parts of Teucrium scordium L. (Labiatae) was analyzed by GC and GC/MS. Fifty-six components were identified in the essential oil of T. scordium. The major constituents of the oil were betha-caryophyllene (22.8%), (E)-betha-farnesene (10.4%), caryophyllene oxide (8.6%), 1,8-cineole (6.1%) and betha-eudesmol (5.1%).Sastav eteričnog ulja iz osušenih nadzemnih dijelova biljke Teucrium scordium L. (Labiatae) u cvatu analiziran je pomoću GC i GC/MS. Identificirano je pedeset šest komponenata, a najvažniji sastojci ulja su beta-kariofilen (22,8%), (E)-beta-farnesen (10,4%), oksid kariofilen (8,6%), 1,8-cineol (6,1%) i beta-eudezmol (5,1%)

The effect of aqueous and methanolic extracts of Prangos ferulacea on formalin-induced pain in mice

Introduction:Prangos ferulacea has been used for GI disorders in traditional medicine. It has been known as an analgesic and anti-inflammatory herb among the communities. However, the analgesic effect of this plant has not been scientifically evaluated. Therefore, the aim of this study was to investigate the analgesic effect of Prangos ferulacea in mice.Material and Methods:30 minutes after intraperitoneal administration of different doses of aqueous or methanolic extracts of Prangos ferulacea, its analgesic effect was evaluated in mice using formalin test. The durations of paw licking and biting were recorded at 5 min. intervals for 30 min. after injection of formalin.Results:The aqueous extract at the dose of 100mg/kg reduced pain at phase 2 and at doses of 300, 900 and 1350 mg/kg it reduced pain at phases 1 and 2 of formalin test. The methanolic extract reduced pain at the dose of 200mg/kg at phase 2, and at doses of 400 and 800 mg/kg at phases 1 and 2 of formalin test. Conclusion:The results of this study showed that the aqueous and methanolic extracts of Prangos ferulacea have analgesic properties. Both extracts contain compounds which exert both peripheral and central analgesia. Future studies are needed to isolate the effective compound and to find the analgesic mechanism of this plant

A Comparative Study of the Antibacterial, Antifungal and Antioxidant Activity and Total Content of Phenolic Compounds of Cell Cultures and Wild Plants of Three Endemic Species of

molecule

Dihydropyridine derivatives to overcome atypical multidrug resistance : design, synthesis, QSAR studies, and evaluation of their cytotoxic and pharmacological activities

Multidrug resistance (MDR) is defined as resistance of tumor cells to the cytotoxic action of multiple structurally dissimilar and functionally divergent drugs commonly used in chemotherapy. Until now, there is no evidence for the effect of 1,4-dihydropyridines (DHPs) on atypical MDR, although there are some indications about the effect of DHPs on p-glycoprotein-mediated MDR. However, it was reported that a DHP derivative (Dexniguldipine) inhibited human DNA topoisomerase I through a non-competitive mechanism. Therefore, some derivatives of DHP were synthesized and their effect in reversing atypical MDR was evaluated. The results showed that two compounds were the potent reversals of atypical MDR. In addition, the intrinsic cytotoxicity of compounds was determined on four different cell lines. Furthermore, their Ca2+ channel blocking activity was evaluated and showed a clear structure-activity relationship (SAR) trend according to the moieties in C-4 position which confirmed the importance of C-4 moiety on Ca2+ channel blocking

Cytotoxic activity and cell cycle analysis of quinoline alkaloids isolated from Haplophyllum canaliculatum Boiss.

Bioassay-guided fractionation of Haplophyllum canaliculatum Boiss. (Rutaceae) extract resulted in isolation of five quinoline alkaloids: 7-isopentenyloxy-gamma-fagarine, atanine, skimmianine, flindersine and perfamine. This is the first isolation of these compounds from this endemic species. The antitumor activity of these five isolates was evaluated against RAJI, Jurkat, KG-1a, HEP-2, MCF-7, HL-60 and HL-60/MX1 tumor cell lines. The highest cytotoxic effect was observed on acute lymphoblastic leukemia cell lines. 7-Isopentenyloxy-gamma-fagarine, atanine, skimmianine and flindersine exhibited very high cytotoxicity against the RAJI cell line with IC50 values of 1.5, 14.5, 15.6 and 14.9 mu g/mL, respectively and 7-isopentenyloxy-gamma-fagarine, atanine and skimmianine exhibited very high cytotoxicity against the Jurkat cell line with IC50 values of 3.6, 9.3 and 11.5 mu g/mL, respectively. 7-isopentenyloxy-gamma-fagarine was also highly cytotoxic against the MCF-7 cell line (IC50 = 15.5 mu g/mL), while atanine, skimmianine, flindersine and perfamine showed moderate to low activity against these cells. All alkaloids had moderate to low cytotoxicity against KG-1a and HEP-2. Investigation of the toxic potential of the alkaloids on HL-60 and HL-60/MX1 showed a significantly higher effect against HL-60/MX1, a multidrug-resistant cell line, compared with the control etoposide (p < 0.05). In all cytotoxicity experiments, peripheral blood mononuclear cells (PBMC) were used as a control for normal hematopoietic cells. Flow cytometry analysis of the compounds resulted in the arrest of cell cycle progression at the sub-G1 phase of the RAJI and Jurkat cell lines in a dose-dependent manner. According to computational analyses, the similar cytotoxic trend in the cell lines could be indicative of the fact that these compounds may act through parallel mechanisms

Antihypertensive effects of some new nitroxyalkyl 1,4-dihydropyridine derivatives in rat model of two-kidney, one-clip hypertension

Dihydropyridine calcium channel blockers consist one of the widely-used groups of drugs for the management of hypertension. In this study, antihypertensive effects of 5 newly synthesized derivatives of DHP was examined the in rat model of two-kidney, one-clip renal hypertension. The results showed that those compounds containing two nitroxy groups had less decreasing effect on MAP ( Men Arterial Pressure) compared to those having one nitroxy group in 5 position. On the other hand, conformational analysis indicated that in two compounds with two chains ( A and E), a great steric hindrance existed; therefore, steric hindrance is the most important factor for interaction of compounds with their receptors

Heavy Metals (Zn, Cu, Pb, Cd and Hg) Contents and Fatty Acids Ratios in Two Fish Species (Scomberomorus commerson and Otolithes ruber) of the Persian Gulf: Heavy metals contents of fish from the Persian Gulf

This study was conducted to determine the concentrations of metals (Zn, Cu, Pb, Cd and Hg) in two commercial fish species of the Persian Gulf (coast of Bushehr Province in Iran), as well as in the sea waters. The concentrations of metals were determined by using differential pulse anodic stripping voltammetry (DPASV). Two selected species were narrow-barred Spanish mackerel and tiger tooth croaker.The same fish were also used to determine the ratios of fatty acids including saturated fatty acids (SFA), monounsaturated fatty acids (MUFA), and polyunsaturated fatty acids (PUFA). Fish and water samples were collected from three different areas, namely Bushehr (station 1), Tangestan (station 2) and Dayyer (station 3). Results showed that all metals contents had lower concentration of the mean values than the permissible limits set by FAO/WHO. It can be concluded that both fish species studied are safe to be consumed. In the present study, for the first time correlation of metals concentrations with fatty acids ratios in both species was statistically analyzed and showed no correlation except for Pb mean value which had negative correlation with PUFA% in tiger tooth croaker species

Reversal of multidrug resistance in cancer cells by novel asymmetrical 1,4-dihydropyridines

Multidrug resistance (MDR) is an important obstacle that limits the efficacy of chemotherapy in many types of cancer. In this study, 14 novel asymmetrical DHPs possessing pyridyl alkyl carboxylate substitutions at C3 and alkyl carboxylate groups at C5 in addition to a nitroimidazole or nitrophenyl moiety at C4 position were synthesized. Calcium channel blocking (CCB) activity was measured in guinea pig ileal longitudinal smooth muscle. Cytotoxicity was tested on 4 human cancer cell lines, while MDR reversal capacity was examined on P-glycoprotein overexpressing doxorubicin resistant MES-SA-DX5 and compared with non-resistant MES-SA cells. Compounds showed different CCB (IC50: 29.3 nM-4.75 μM) and cytotoxic activities (IC50: 6.4 to more than 100 μM). Several compounds having nitrophenyl moiety at C4, could significantly reverse resistance to doxorubicin at 0.5 and 1 μM. The most active ones were 7e and 7g containing ethyl carboxylate and isopropyl carboxylate at C5, respectively. CCB activity, which is considered an undesirable effect for these agents, of 7e and 7g were 33 and 20 times lower than nifedipine, respectively. In conclusion, the newly synthesized asymmetrical DHP compounds showed promising MDR reversal and antitumoral activities with low CCB effects and could be of therapeutic value in drug resistant cancer

Cytotoxic effect of some 1,4-dihydropyridine derivatives containing nitroimidazole moiety

The 1,4-dihydropyridine (DHP) derivatives are a known class of calcium channel blockers. Some derivatives of DHP showed significant cytotoxicity. It was shown that this effect may not be the result of interaction with Ca2+ channels. In this study, we performed an investigation about the intrinsic cytotoxicity of some derivatives of DHP containing nitroimidazole moiety on their C4 position on four different cancer cell lines (Raji, K562, Fen and HeLa). The result showed that these compounds had moderate-good cytotoxic activity. In addition, QSAR model shows the importance of N atom in cytotoxicity; Ca2+ channels