Pomegranate (<Emphasis Type="Italic">Punica granatum</Emphasis>) pure chemicals show possible synergistic inhibition of human PC-3 prostate cancer cell invasion across Matrigel™

Summary Four pure chemicals, ellagic acid (E), caffeic acid (C), luteolin (L) and punicic acid (P), all important components of the aqueous compartments or oily compartment of pomegranate fruit (Punica granatum), and each belonging to different representative chemical classes and showing known anticancer activities, were tested as potential inhibitors of in vitro invasion of human PC-3 prostate cancer cells in an assay employing Matrigel™ artificial membranes. All compounds significantly inhibited invasion when employed individually. When C, P, and L were equally combined at the same gross dosage (4 μ g/ml) as when the compounds were tested individually, a supradditive inhibition of invasion was observed, measured by the Kruskal-Wallis non-parametric test.An erratum to this article can be found at     

Effects of conjugated equine estrogen vs. raloxifene on serum insulin-like growth factor-i and insulin-like growth factor binding protein-3: a 2-year, double-blind, placebo-controlled study

OBJECTIVE: To assess and compare the effect of conjugated estrogen and of the selective estrogen receptor modulator raloxifene on serum levels of insulin-like growth factor-I (IGF-I) and insulin-like growth factor binding protein-3 (IGFBP-3) and on the IGF-I/IGFBP-3 ratio. DESIGN: A 2-year randomized, double-blind, placebo-controlled study. SETTING: Endocrinology outpatient department. PATIENT(S): Fifty-six postmenopausal, hysterectomized women. INTERVENTION(S): Women received raloxifene hydrochloride in doses of 60 mg/day (n = 15) or 150 mg/day (n = 13), conjugated equine estrogen (CEE) in doses of 0.625 mg/day (n = 15), or a placebo (n = 13) over the course of 2 years. MAIN OUTCOME MEASURE(S): At baseline and after 6, 12, and 24 months of treatment, serum levels of IGF-I, IGFBP-3, and insulin were measured, and an IGF-I/IFGBP-3 ratio was calculated. RESULT(S): Both raloxifene and CEE decreased serum IGF-I concentration. In contrast to CEE, which had no effect, both raloxifene doses of 60 and 150 mg/day significantly increased serum IGFBP-3 during the 2 years. Compared with placebo, the decrease in IGF-I/IGFBP-3 ratio was -32.5% (95% CI: -20.1; -44.8%) for CEE; -16.4% (95% CI: -3.6; -29.2%) for raloxifene at 150 mg/day; and -15.4% (95% CI: -1.0; -29.8%) for raloxifene at 60 mg/day. No effect of CEE or raloxifene was found on insulin concentration at any time point. CONCLUSION(S): Long-term use of both CEE and raloxifene decreases serum IGF-I and the IGF-I/IGFBP-3 ratio, but, unlike CEE, raloxifene produced a significant yet small increase in IGFBP-3.     

n‐Type Copolymers with Fluorene and 1,3,4‐Heterodiazole Moieties

Summary: The successful realization of n‐channel field‐effect transistors requires the application of semiconducting polymers with high electron mobility (n‐type). However, reports on n‐type polymers are rather scarce in the literature. Therefore, the development of polymers with suitable electron transport properties is particularly challenging for the synthetic chemistry. Main chain polymers with strong acceptor units, such as 1,3,4‐heterodiazoles, are potential candidates for electron transport materials in electronic devices. The fluorene unit is another ring system with interesting physical and chemical properties, which is often used in rigid‐rod, main chain polymers. The present work introduces the synthesis of organo‐soluble copolymers consisting of alternating fluorene‐, 1,3,4‐heterodiazole, and, in some cases, additional 2,5‐dialkoxyphenylene units in the main chain. The reported synthesis involves modified classical polycondensation as well as the tetrazole route. We demonstrate the possibility of exchanging oxygen in the heteroaromatic ring with sulfur using Lawesson's reagent during the ring closure reaction. An alternative structure of the heterocyclic ring with N‐phenyl in the oxygen position is feasible using the tetrazole synthetic route. The chemical and electrochemical properties of the copolyfluorenes are investigated in detail. Some of the synthesized copolyfluorenes have also been used for the preparation of “electron‐only” devices enabling the calculation of the electron mobilities. Further, an organic field‐effect transistor (OFET) characteristic was shown.

OFET characteristics of the polymer 12b .     

Novel Carbazole‐Based Ladder‐Type Polymers for Electronic Applications

Summary : New carbazole‐based ladder‐polymers have been prepared utilising a 3,6‐diacyl‐2,7‐dibromocarbazole building block 4 . Suzuki polycondensation of 4 with carbazole‐2,7‐diboronic acid followed by addition of methyl lithium and ring closure with boron trifluoride gave ladder‐polymers 9 with all methine bridges, analogous to ladder‐type poly(para‐phenylene). In very dilute solution, these polymers show blue‐green fluorescence similar to that from the corresponding LPPP. At higher concentrations, a broader red‐shifted emission is seen which suggests that the chains are aggregating in solution. Homopolymerisation of 4 followed by condensation of the carbonyls with boron sulfide produced a novel ladder‐type structure 13 with alternating five‐ and six‐membered rings. This ladder‐polymer displays bright yellow‐green fluorescence. Cyclic voltammetry indicated that these materials have HOMO energy levels comparable to the work function of ITO, making them good candidates for use as hole accepting emissive materials for LEDs.

The ladder polymers synthesised.     

Dietary seed oil rich in conjugated linolenic acid from bitter melon inhibits azoxymethane-induced rat colon carcinogenesis through elevation of colonic PPARgamma expression and alteration of lipid composition

Our previous short-term experiment demonstrated that seed oil from bitter melon (Momordica charantia) (BMO), which is rich in cis(c)9, trans(t)11, t13-conjugated linolenic acid (CLN), inhibited the development of azoxymethane (AOM)-induced colonic aberrant crypt foci (ACF). In our study, the possible inhibitory effect of dietary administration of BMO on the development of colonic neoplasms was investigated using an animal colon carcinogenesis model initiated with a colon carcinogen AOM. Male F344 rats were given subcutaneous injections of AOM (20 mg/kg body weight) once a week for 2 weeks to induce colon neoplasms. They also received diets containing 0.01%, 0.1% or 1% BMO for 32 weeks, starting 1 week before the first dosing of AOM. At the termination of the study (32 weeks), AOM induced 83% incidence (15/18 rats) of colonic adenocarcinoma. Dietary supplementation with 0.01% and 0.1% BMO caused significant reduction in the incidence (47% inhibition by 0.01% BMO, p<0.02; 40% inhibition by 0.1% BMO, p<0.05; and 17% inhibition by 1% BMO) and the multiplicity (64% inhibition by 0.01% BMO, p<0.005; 58% inhibition by 0.1% BMO, p<0.02; and 48% inhibition by 1% BMO, p<0.05) of colonic adenocarcinoma, though a clear dose response was not observed. Such inhibition was associated with the increased content of CLA (c9,t11-18:2) in the lipid composition in colonic mucosa and liver. Also, BMO administration in diet enhanced expression of peroxisome proliferator-activated receptor (PPAR) gamma protein in the nonlesional colonic mucosa. These findings suggest that BMO rich in CLN can suppress AOM-induced colon carcinogenesis and the inhibition might be caused, in part, by modification of lipid composition in the colon and liver and/or increased expression of PPARgamma protein level in the colon mucosa.     

Synthesis of π‐Conjugated Organometallic Polymer Networks

The present paper reports the synthesis of π‐conjugated organometallic polymer networks based on poly[2,5‐dioctyloxy‐1,4‐diethynyl‐phenylene‐alt‐2,5,‐bis(2′‐ethylhexyloxy)‐1,4‐phenylene] (EHO‐OPPE), a soluble poly(p‐phenylene ethynylene) (PPE) derivative. The ethynylene moieties of the polymer coordinate to Pt⁰ centers, which act as conjugated cross‐links. These materials are readily accessible through ligand‐exchange reactions between the linear PPE and Pt(styrene)₃. The in‐situ NMR investigation of model reactions of Pt(styrene)₃ with diphenylacetylene (DPA) has shown that the ethynylene moieties comprised in the PPE readily coordinate to Pt⁰ centers under release of the relatively weakly‐bound styrene ligands. Spin‐coating has resulted in cross‐linked films of good optical quality. We also have been able to produce PPE‐Pt‐gels with high solvent content (> 95 wt.‐%). As expected, the coordination of Pt markedly influences the photophysical characteristics of the PPE. The photoluminescence is efficiently quenched, and the absorption maximum in the visible regime experiences a hypsochromic shift.

Ligand‐exchange reaction between EHO‐OPPE and [Pt(PhCH?CH₂)₃] leading to the target EHO‐OPPE‐Pt⁰ networks.     

^99Tc-MDP治疗大鼠佐剂型关节炎的实验研究

目的:用99Tc-MDP(锝[99Tc]亚甲基二膦酸盐注射液)治疗大鼠佐剂型关节炎,探讨其疗效并进行分析。方法:将30只SD大鼠随机分成对照组、佐剂型关节炎组和99Tc-MDP治疗组,每组10只,治疗组于造模后的第10 d起给予99Tc-MDP(2.5×10-3μg/kg,以99Tc含量计算)腹腔内注射,每2d重复注射1次,观察大鼠左踝关节的左右径宽度、关节炎指数、血清肿瘤坏死因子(TNF)和白细胞介素-1β(IL-1β)水平、关节核素显像及关节病理的变化。结果:与佐剂型关节炎组相比,99Tc-MDP治疗组大鼠左踝关节左右径宽度及关节炎指数相对较小,血清TNF和IL-1β水平低,关节核素显像感兴趣区放射性比(T/NT)小,组织病理检查提示滑膜组织增生和炎性细胞浸润程度相对较轻。结论:99Tc-MDP治疗大鼠佐剂型关节炎疗效肯定,可用于类风湿性关节炎(RA)患者的全身治疗。     

An evaluation of clinical response to piperazine oestrone sulphate ('Harmogen') in menopausal patients

Summary

The results are reported of a controlled, double-blind, crossover trial of piperazine oestrone sulphate (‘Harmogen’) compared with ethinyl oestradiol and placebo in menopausal patients with features of endogenous oestrogen withdrawal. The oestro-genicity of both active substances was well substantiated by vaginal epithelial maturation indices. Piperazine oestrone sulphate was superior to ethinyl oestradiol, at the dosage levels used, in producing a more pronounced relief of menopausal symptoms without any notable adverse effects. The incidence of side-effects was greater during treatment with ethinyl oestradiol. Piperazine oestrone sulphate is considered to be at least as effective an oestrogenic substance as ethinyl oestradiol and worthy of further therapeutic evaluation.     

Dietary conjugated linoleic acid and long-chain n-3 fatty acids in mammary and prostate cancer protection: a review

The role of dietary fatty acids on cancer is still controversial. To examine the current literature on the protective role of conjugated linoleic acid (CLA) and marine long-chain fatty acids [eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA)] and the risk of breast and prostate cancer, data from 41 case-control and cohort studies and relevant in vitro and animal experiments were included in this 2000–2010 revision. Epidemiological studies on CLA intake or its tissue concentration related to breast and prostate tumorigenesis are not conclusive; EPA and DHA intake have shown important inverse associations just in some studies. Additional research on the analysed association is required.     

Differential effect of guanethidine on dopamine and norepinephrine pools in urine,heart and superior cervical ganglion in the rat

Summary The time-related changes of dopamine (DA) and norepinephrine (NE) pools were investigated in heart, superior cervical ganglion (SCG) and urine in rats treated chronically with guanethidine (50 mg/kg i.p. five days each week). The efficiency of sympathectomy was assessed by the great loss of NE in heart and superior cervical ganglion (SCG) (–96% and –76% respectively of control values on day 18) together with the ready reduction of NE and 3-methoxy-4-hydroxyphenylglycol (MHPG) in urine.The pattern of changes was quite different for DA, which was less readily affected and at a lesser extent than NE in heart and SCG thus suggesting the presence of norepinephrine-independent DA stores. Similarly the urinary excretion of free DA, free 3, 4-dihydroxyphenylacetic acid (DOPAC) and free homovanillic acid (HVA) was slightly decreased only from the 9th day, whereas urinary conjugated DA remained unaltered. These results indicate that the greatest portion of urine free and conjugated DA, free DOPAC and free HVA derives from peripheral pools located outside noradrenergic neurons. Alternatively, the time-course of DA sensitivity to guanethidine suggests that a portion of urine DA may originate from DA stored independently from NE in noradrenergic neurons.