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PubMedDate not supplied

Designing and testing of an effective oil-in-water microemulsion drug delivery system for in vivo application.

The phase behavior of a new psedoternary system of clove oil/Tween 20 has been studied. Several compositions from the single-phase region were selected and their stability toward time, temperature, and electrolytes has been examined. A particular composition(clove oil/Tween 20/water as 5/30/65) was chosen as the drug delivery system from the clear oil-in-water zone of the pseudoternary system. The droplet dimension and the polydispersity state of the particular composition was determined by dynamic light scattering. A bioactive compound quarcetin was encapsulated in the vehicle. The efficacy of the drug in the vehicle was examined against leishmaniasis in hamster models. The hepatotoxicity of the vehicle (o/w microemulsion) with and without the drug quarcetin was examined by estimating serum alkaline phosphatase, glutamate pyruvate transaminase, urea, and creatinine.

Animals↗
PubMed2005

A geranylated biphenyl derivative from Garcinia malvgostana.

Extracts of root bark, stem bark and the latex collected from the green fruits of Garcinia mangostana gave alpha-mangostin, beta-mangostin, gamma-mangostin, garcinone-E, methoxy-beta-mangostin and a new geranylated biphenyl derivative 3-hydroxy-4-geranyl-5-methoxybiphenyl. The latex of G. mangostana consists of more than 75% of xanthones which have strong antibacterial (anti-MRSA and -VRE), anti-inflammatory, antifungal and a number of other biological activities. Hence the presence of the above highly bioactive compounds in large quantities should be the causative factor for G. mangostana's medicinal value in indigenous medicine.

Biphenyl Compounds↗
PubMedDate not supplied

New glycosyl-(carboxamide)-1,2,3-triazole-N-nucleosides: synthesis and antitumor activity.

A series of potential bioactive compounds, 1-glucopyranosyl- 1,2,3-triazole-4,5-dimethylcarboxylate, 1-glucopyranosyl-1,2,3-triazole-4,5-N-dicarboxamide,-dialkyl-dicarboxamide-N-nucleosides and 6-amino-4H-1-(beta-D-glucopyranosyl)-8-hydroxy-1,2.3-triazolo[4,5-e][1,3]-diazepin-4-one, were synthesized. Primary activity screening of the novel nucleosides showed poor or no anticancer activity against breast, lung and CNS tumors.

Antineoplastic Agents↗
PubMed2004

PEG-PLA nanoparticles as carriers for nasal vaccine delivery.

This report presents an overview of the potential of nanoparticles as nasal carriers for drug/vaccine administration. In addition, this report shows, for the first time, the efficacy of polylactic acid nanoparticles coated with a hydrophilic polyethyleneglycol coating (PEG-PLA nanoparticles) as carriers for the nasal transport of bioactive compounds. For this purpose, tetanus toxoid (TT), a high molecular weight protein (Mw 150,000 Da), was chosen as a model antigen and encapsulated in the PEG-PLA nano- and microparticles (200 nm and 1.5 microm respectively). These nanosystems were first characterized for their stability in the presence of lysozyme and also for their size, electrical charge, loading efficiency, in vitro release of antigenically active toxoid and afterwards, these formulations were administered intranasally to mice and the systemic and mucosal anti-tetanus responses were evaluated for up to 24 weeks. Additionally, PEG-PLA particles labeled with rhodamine 6G were administered intranasally to rats in order to visualize their interaction with the nasal mucosae by fluorescence microscopy. Their behavior was compared with that of the well known PLA nanoparticles (200 nm). The results showed that PLA nanoparticles suffered an immediate aggregation upon incubation with lysozyme, whereas the PEG-coated nanoparticles remained totally stable. The antibody levels elicited following i.n. administration of PEG-coated nanoparticles were significantly higher than those corresponding to PLA nanoparticles. Furthermore, PEG-PLA nanoparticles generated an increasing and a long lasting response. The qualitative fluorescence microscopy studies revealed that PEG-PLA particles are able to cross the rat nasal epithelium. These studies indicate that the PEG coating around the particles has a role in stabilizing PLA particles in mucosal fluids and that it facilitates the transport of the nanoencapsulated antigen, hence eliciting a high and long lasting immune response.

Administration, Intranasal↗
PubMed2004

High-throughput screening with quantitation of ATP consumption: a universal non-radioisotope, homogeneous assay for protein kinase.

A number of assays have been developed for high-throughput screening (HTS) of potentially bioactive compounds. To screen millions of chemical compounds efficiently, the best detection technology prior to initiating HTS must be chosen. Ideally, a non-radioisotope (non-RI), homogeneous method, equivalent to the most reliable assay for a particular target, should be selected as an HTS method. Protein kinases are among the most important classes for drug discovery because they participate in various signaling pathways. Several HTS technologies are available for kinase activity: SPA (Amersham, Piscataway, NJ, U.S.A.), HTRF (CIS-US, Inc., Bedford, MA, U.S.A.), IMAP (Molecular Devices, Sunnyvale, CA, U.S.A.), and Z'-LYTE (Invitrogen, Carlsbad, CA, U.S.A.). The amount of phosphorylated product is detected by different methods in these assays. Recently, Kinase-Glo Luminescent Kinase Assay, a non-RI, homogeneous, adenosine triphosphate (ATP) quantitative kit useful for kinase activity detection, has become available from Promega (Madison, WI, U.S.A.). ATP is a universal substrate for kinases. Thus, the Kinase-Glo assay shows promise for becoming the primary method of determining kinase activity in HTS. We have developed a Kinase-Glo system for cyclin-dependent kinase 4 (Cdk4), and compare its results with those of the filtration method, the most reliable assay for in vitro Cdk4 activity. In addition, the reliability and sensitivity of the Kinase-Glo are discussed.

Adenosine Triphosphate↗
PubMed1996

Tissue-engineered skeletal muscle organoids for reversible gene therapy.

Genetically modified murine skeletal myoblasts were tissue engineered in vitro into organ-like structures (organoids) containing only postmitotic myofibers secreting pharmacological levels of recombinant human growth hormone (rhGH). Subcutaneous organoid implantation under tension led to the rapid and stable appearance of physiological sera levels of rhGH for up to 12 weeks, whereas surgical removal led to its rapid disappearance. Reversible delivery of bioactive compounds from postmitotic cells in tissue engineered organs has several advantages over other forms of muscle gene therapy.

Animals↗
PubMed2005

Effects of soy protein and soy phytochemicals on mammary tumor development in female transgenic mice overexpressing human pituitary growth hormone.

The objective of this study was to determine the effect of soy-based diets on mammary tumors in female cancer- prone mice. Transgenic virgin female mice expressing human pituitary growth hormone and their respective phenotypically normal littermates were fed a diet containing either casein (C), low-isoflavone soy protein (LIS), or high-isoflavone soy protein (HIS). Indices of tumor development were measured throughout the study. Both days from birth until death and days on diet until death were increased [by 20% (P = .01) and 19% (P = .02), respectively] in the LIS group when compared with the C group. Both intervals were increased also (by 16% and 17%, respectively; P < .05) in the HIS group when compared with the C group. Days from birth to first tumor were increased by 7% (P < .05), as was days on diet to first tumor by 5% (P < .05), in the LIS group when compared with the C group. First-onset number of tumors was decreased (P = .02) by 41% and 34% in the LIS and C groups, respectively, when compared with the HIS group. Final onset of tumors was decreased (P < .05) by 44% and 9% in the LIS and HIS groups, respectively, when compared with the C group. Total area of final tumors was decreased (P < .05) by 30% in the LIS group when compared with the C group. Taken cumulatively, these data suggest that a diet rich in soy protein may provide protective benefits regarding tumor development in female cancer-prone mice. Furthermore, some bioactive compounds in the HIS diet appeared to confound the soy protein-induced beneficial effects.

Animals↗
PubMed2006

Effects of the aerial parts of Orostachys japonicus and its bioactive component on hepatic alcohol-metabolizing enzyme system.

In the course of screening medicinal plants that modulate hepatic alcohol-metabolizing enzymes and lipid peroxidation, effects of the methanol extract (ME) of Orostachys japonicus and its major bioactive compound, gallic acid (GA), were investigated in rats treated with 10% ethanol solution for 6 weeks. The ME and GA greatly enhanced the activities of hepatic alcohol dehydrogenase (ADH), the microsomal ethanol-oxidizing system (MEOS), and aldehyde dehydrogenase (ALDH) in a dose-dependent manner, but had no effect on catalase. The hepatic lipid peroxide level increased by ethanol administration was moderately reduced by treatment with ME or GA. The results suggest that the detoxification of hepatic alcohol by O. japonicus ME under our experimental conditions was due to the enhanced activities of the alcohol-oxidizing enzymes, ADH, MEOS, and ALDH. In addition, GA may be partly responsible for the effects.

Alcohol Dehydrogenase↗
PubMed2006

Effect of genistein with carnitine administration on lipid parameters and obesity in C57Bl/6J mice fed a high-fat diet.

Soy products are mainly composed of proteins, phytochemicals such as isoflavones, soy lipids, and carbohydrates. It is unclear whether an individual component alone or a combined effect of multiple bioactive compounds contributes to the beneficial properties of soy. We investigated the effect of dietary genistein (the principal soy isoflavone) alone and combined with L-carnitine to evaluate possible synergistic effects on the intentionally induced prediabetic state characterized by insulin resistance and obesity in C57Bl/6J mice fed a high-fat diet (HD). In the HD-alone group, abdominal and back fat relative to total body weight were significantly higher compared with other groups including those fed normal diet (ND). Among the HD groups, final weight gains of the HD plus genistein (HD+G) and HD plus genistein plus L-carnitine (HD+G+C) groups were lower compared with that of the control (HD-alone). Especially in liver, the results showed that genistein with carnitine transcriptionally up-regulated expressions of acyl-coenzyme A synthetase (ACS) and carnitine palmitoyltransferase-I (CPT-I) by approximately 50% and 40%, respectively, compared with genistein alone. However, the up-regulation of CPT-I did not directly reflect the enzyme activity of CPT-I. On the other hand, the effects of genistein and genistein with carnitine on the expressions of ACS and CPT-I in muscle were not significant. Our study suggests that genistein with carnitine exerts anti-obesity effects, probably by modulating peroxisome proliferator-activated receptor-associated genes. However, further work is needed to elucidate the possible mechanisms by which genistein and carnitine intervene.

Adipose Tissue↗
PubMed2006

Antiproliferative activities of parthenolide and golden feverfew extract against three human cancer cell lines.

The medicinal herb feverfew [Tanacetum parthenium (L.) Schultz-Bip.] has long been used as a folk remedy for the treatment of migraine and arthritis. Parthenolide, a sesquiterpene lactone, is considered to be the primary bioactive compound in feverfew having anti-migraine, anti-tumor, and anti-inflammatory properties. In this study we determined, through in vitro bioassays, the inhibitory activity of parthenolide and golden feverfew extract against two human breast cancer cell lines (Hs605T and MCF-7) and one human cervical cancer cell line (SiHa). Feverfew ethanolic extract inhibited the growth of all three types of cancer cells with a half-effective concentration (EC50) of 1.5 mg/mL against Hs605T, 2.1 mg/mL against MCF-7, and 0.6 mg/mL against SiHa. Among the tested constituents of feverfew (i.e., parthenolide, camphor, luteolin, and apigenin), parthenolide showed the highest inhibitory effect with an EC50 against Hs605T, MCF-7, and SiHa of 2.6 microg/mL, 2.8 microg/mL, and 2.7 microg/mL, respectively. Interactions between parthenolide and flavonoids (apigenin and luteolin) in feverfew extract also were investigated to elucidate possible synergistic or antagonistic effects. The results revealed that apigenin and luteolin might have moderate to weak synergistic effects with parthenolide on the inhibition of cancer cell growth of Hs605T, MCF-7, and SiHa.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed2026

Integrative chemical genetics platform identifies condensate modulators linked to neurological disorders.

Dysregulation of biomolecular condensates is implicated across multiple neurological disorders. However, approaches to systematically identify their modulators remain limited. Here, we expand the utility of MLF2 as a versatile condensate biomarker and develop CondenScreen, an integrated high-content screening and bioinformatics pipeline enabling identification of condensate modulators across chemical and genetic space. Screening 1760 bioactive compounds in a cellular DYT1 dystonia model, we validate the platform for condensate-targeted drug discovery, identifying drugs that prevent the accumulation of the MLF2 reporter into nuclear envelope condensates. In parallel, a genome-wide CRISPR/Cas9 screen correlates nuclear condensate abundance with genes implicated in microcephaly and over eight additional neurodevelopmental disorders. Machine learning and confocal imaging resolve distinct condensate phenotypes, with RNF26 deletion provoking nuclear envelope condensates that phenocopy hallmarks of torsin deficiency. Our study provides a scalable platform for identifying modulators of condensates and establishes a correlative connection between nuclear condensate accumulation and genes implicated in neurodevelopmental disorders.

Humans↗
PubMed1991

Beyond dietary fiber.

The complexity of plant foods high in dietary fiber poses new challenges to clinical investigators and leads to many study-design dilemmas. There are basic differences in studying purified polymers, highly concentrated but not purified fibers, and diets high in high-fiber whole foods. The fibrils of the plant cell wall are most likely altered when prepared as a pure chemical entity, and when fiber concentrates (eg, wheat bran) are used, the method of preparation may alter the composition of the final product. Whole-plant, high-fiber foods are complex storehouses of a diversity of polymers, including resistant starch, and of bioactive compounds. Furthermore, the addition of a reasonable amount of high-fiber food to the diet not only adds dietary fiber but many digestible, caloric macronutrients that alter the entire diet composition. These problems and dilemmas are reviewed.

Cell Wall↗
PubMed1995

Epidemiologic evidence for vitamin C and vitamin E in cancer prevention.

Antioxidant nutrients have been hypothesized to be protective against cancer. Vitamin C is a major circulating water-soluble antioxidant, and vitamin E is a major lipid-soluble antioxidant. Many case-control and cohort studies have related cancer risk to estimates of nutrient intake derived from food intake reports. Diets high in fruit and vegetables, and hence high in vitamin C, have been found to be associated with lower risk for cancers of the oral cavity, esophagus, stomach, colon, and lung. Diets high in added vegetable oils, and hence high in vitamin E, have been less consistently shown to be associated with cancer protection. This may be because vitamin E offers less protection against cancer or because the estimation of vitamin E intake is less accurate than is the estimation of vitamin C intake. In contrast with the findings from epidemiologic studies based on foods, observational studies of nutrients consumed in supplements and recent experimental trials provide little support for a strong protective role for vitamins C or E against cancer. If vitamins C or E are indeed protective against cancer, that protection may derive from their consumption in complex mixtures with other nutrients and with other bioactive compounds as found in the matrix provided by whole foods.

Ascorbic Acid↗
PubMed2000

Bitter taste, phytonutrients, and the consumer: a review.

Dietary phytonutrients found in vegetables and fruit appear to lower the risk of cancer and cardiovascular disease. Studies on the mechanisms of chemoprotection have focused on the biological activity of plant-based phenols and polyphenols, flavonoids, isoflavones, terpenes, and glucosinolates. Enhancing the phytonutrient content of plant foods through selective breeding or genetic improvement is a potent dietary option for disease prevention. However, most, if not all, of these bioactive compounds are bitter, acrid, or astringent and therefore aversive to the consumer. Some have long been viewed as plant-based toxins. As a result, the food industry routinely removes these compounds from plant foods through selective breeding and a variety of debittering processes. This poses a dilemma for the designers of functional foods because increasing the content of bitter phytonutrients for health may be wholly incompatible with consumer acceptance. Studies on phytonutrients and health ought to take sensory factors and food preferences into account.

Cardiovascular Diseases↗
PubMed2004

Role of calcium and dairy products in energy partitioning and weight management.

Dietary calcium plays a pivotal role in the regulation of energy metabolism because high-calcium diets attenuate adipocyte lipid accretion and weight gain during the overconsumption of an energy-dense diet and increase lipolysis and preserve thermogenesis during caloric restriction, which thereby markedly accelerates weight loss. Intracellular Ca(2+) plays a key regulatory role in adipocyte lipid metabolism and triacylglycerol storage; increased intracellular Ca(2+) results in the stimulation of lipogenic gene expression and lipogenesis and the suppression of lipolysis, which results in increased lipid filling and increased adiposity. Moreover, the increased calcitriol produced in response to low-calcium diets stimulates adipocyte Ca(2+) influx and, consequently, promotes adiposity, whereas higher-calcium diets inhibit lipogenesis, inhibit diet-induced obesity in mice, and promote lipolysis, lipid oxidation, and thermogenesis. Notably, dairy sources of calcium markedly attenuate weight and fat gain and accelerate fat loss to a greater degree than do supplemental sources of calcium. This augmented effect of dairy products relative to supplemental calcium is likely due to additional bioactive compounds, including the angiotensin-converting enzyme inhibitors and the rich concentration of branched-chain amino acids in whey, which act synergistically with calcium to attenuate adiposity. These concepts are confirmed by epidemiologic data and recent clinical trials, which indicate that diets that include > or =3 daily servings of dairy products result in significant reductions in adipose tissue mass in obese humans in the absence of caloric restriction and markedly accelerate weight and body fat loss secondary to caloric restriction compared with diets low in dairy products. These data indicate an important role for dairy products in both the prevention and treatment of obesity.

Adipose Tissue↗
PubMed2006

Effects of cultivar, fruit number and reflected photosynthetically active radiation on Fragaria x ananassa productivity and fruit ellagic acid and ascorbic acid concentrations.

BACKGROUND AND AIMS: A number of strawberry varieties were surveyed for their total ellagic acid concentration, and attempts were made to determine if ellagic acid and ascorbic acid concentrations of two strawberry cultivars could be increased by polythene reflective mulches. METHODS: After adjusting crop yields and cultivation using polythene mulches with two different PAR reflective capacities, field- and polytunnel-grown strawberries were analysed for ellagic acid and ascorbic acid concentrations by HPLC. Comparative measurements of yield and fruit quality were determined along with plant developmental changes. KEY RESULTS: Ellagic acid concentration varied widely with strawberry cultivar (60-341 microg g(-1) frozen weight), as did the ratio of conjugated ellagic acid : free ellagic acid. Also, there was significant year-to-year variation in total ellagic acid concentration with some cultivars. Mulches with different reflective capacities impacted on strawberry production; highly reflective mulches significantly increased growth and yield, the latter due to increases in fruit size and number. CONCLUSIONS: Highly reflective mulches significantly increased total concentrations of ellagic acid and ascorbic acid relative to control in fruit of different cultivars. The potential of agronomic practices to enhance the concentration and amounts of these important dietary bioactive compounds is discussed.

Ascorbic Acid↗
PubMed2004

Soy processing influences growth of estrogen-dependent breast cancer tumors.

Soy-based products consumed in Asian countries are minimally processed whereas in the USA many of the soy foods and soy ingredients are highly processed. Soy foods contain complex mixtures of bioactive compounds, which may interact with one another. The objective of this study was to evaluate the ability of various soy products containing genistin, the glycoside form of genistein, to affect growth of MCF-7 cells transplanted into ovariectomized athymic mice. Products investigated included soy flour, two crude extracts of soy (soy molasses and Novasoy(R)), a mixture of isoflavones and genistin in pure form. Each of the soy flour-processed products was added to the diet to provide equivalent amounts of genistein aglycone equivalents (750 p.p.m.). Tumors in the negative control animals regressed throughout the study while the tumors in the soy flour-fed animals remained basically the same size (neither grew nor regressed). In animals consuming soy molasses, Novasoy(R), mixed isoflavones or genistin alone, tumor growth was stimulated when compared with animals consuming a control diet devoid of soy. These same dietary treatments resulted in increased cellular proliferation. Changes in mRNA expression of gene targets (estrogen responsiveness, cell cycle progression, apoptosis and aromatase activity) in tumors induced by the different diets were evaluated. The relative expression of pS2, progesterone receptor and cyclin D1 was increased in animals consuming the Novasoy(R), mixed isoflavones and genistin. Bcl2 mRNA expression was low in most of the dietary treatment groups compared with positive (estradiol implant) controls. Aromatase expression was not affected in any of the treatment groups. The degree of soy flour processing affects the estrogenicity of products containing a constant amount of genistein. Collectively, these findings suggest that for postmenopausal women with estrogen-dependent breast cancer, the consumption of foods containing soy flour is more advisable than consuming isoflavones in more purified forms.

Animals↗
PubMed2006

Identification of cyanidin glycosides as constituents of freeze-dried black raspberries which inhibit anti-benzo[a]pyrene-7,8-diol-9,10-epoxide induced NFkappaB and AP-1 activity.

Dietary freeze-dried black raspberries inhibit tumor induction by N-nitrosomethylbenzylamine in the rat esophagus, but the constituents responsible for this chemopreventive activity have not been identified. We fractionated freeze-dried black raspberries and used mouse epidermal JB6 Cl 41 cells stably transfected with either a nuclear factor kappa B (NFkappaB)- or an activator protein 1 (AP-1)-luciferase reporter, and treated with racemic anti-benzo[a]pyrene-7,8-diol-9,10-epoxide (BPDE), to assess the inhibitory effects of the fractions. The ethanol and water extracts of the freeze-dried black raspberries had inhibitory activity and these extracts were fractionated by HPLC to give several bioactive fractions. Further HPLC analysis yielded multiple subfractions, some of which inhibited BPDE-induced NFkappaB activity. Major constituents of the most active subfractions were identified by their spectral properties and in comparison with standards as cyanidin-3-O-glucoside, cyanidin 3-O-(2(G)-xylosylrutinoside) and cyanidin 3-O-rutinoside. Analysis of freeze-dried black raspberries indicated that these three components comprised approximately 3.4% of the material by dry weight. Consistent with these results, standard cyanidin-3-O-glucoside and cyanidin chloride were also good inhibitors of BPDE-induced NFkappaB activity. The results of this study demonstrate that cyanidin glycosides of freeze-dried black raspberries are bioactive compounds which could account for at least some of the chemopreventive activity observed in animal models.

7,8-Dihydro-7,8-dihydroxybenzo(a)pyrene 9,10-oxide↗