RESUMEN
Taiwan produces large quantities of bananas in the southern area. Recently, due to the export quantity has been greatly reduced, in order to efficiently maintain the banana agriculture and economy, the development of alternate uses of bananas has become urgently in need. Bananas contain a fair amount of nutrients with low glycemic index. Currently, as the bread consumption is increasing, we tried to manufacture banana-assorted breads. The desiccated powders of Musa sapientum var TC2-425 Linn [(genomically, called as Musa (AAA) (MA)] and Musa basjoo "Nam Wa" (MB) were separately incorporated at 15%, 20%, and 25% (denoted as MA15-MA25 and MB15-MB25). Results indicated that MA exhibited higher contents of moisture, ash, crude protein, and lutein, while with lower crude fat, crude fibers, carbohydrate, sodium, total soluble sugars, and pectin. The contents of taste compounds (name, samples in decreasing order) were as follows: 5'-CMP (MB25, MB20); 5'-GMP (MA25, MA20); 5'-AMP (MB25, MA15); 5'-XMP (MA25, MA20); 5'-IMP (MA25, MB20, MB25); and 5'-UMP (MA20, MA25, MB20). Hedonic scoring (HS) indicated MA15, MA20, MB15, and MB20 were more acceptable. Textural profile analysis (TPA; for 0-6 days, only 0-4 days are shown) revealed that "flavor," "mouthfeel," "hardness," "gumminess," and "chewiness" were the determinant key roles. Conclusively, due to different chemical constituent of banana, different recipes must be considered. The bread acceptability is affected by the fermentative profile which in turn is governed by the contents of soluble sugars, pectin, taste compounds, and the overall activity of yeast cells.
RESUMEN
Rhizoma Alpinia officinarum (Hance) Farw, Zingiberaceae (AO), a ginger family herb exhibiting stimulant and a carminative bioactivity, is widely used in European and Asian countries as spicy condiment and medicinal uses. Allyl isothiocyanate (AITC) is the main pungent taste of native Wasabi (Wasabia japonica). The cytotoxicity of AITC has been implicated in thymus, adrenals, and white blood cells. Considering food safety, apparently a safer substitute for wasabi is worthy commercialized. Previously, we found AO crude paste to be rather feasible for use as a "Wasabi-substitute" in fresh meat and cold salads. A process linking cold ethyl acetate (EtAc) extraction with silica gel adsorption and reversed phase high-performance liquid chromatography (RP-HPLC) (mobile phase, 75% methanol) was used to isolate galangal acetate, the Wasabi-like taste constituent. AO contained abundant galangal acetate (3.84 ± 0.07%) compared to A. galangal (0.57 ± 0.16%), and as already confirmed by thin layer chromatography (TLC), gas chromatography (GC)/mass spectrometry (MS)/MS and Nuclear Magnetic Resonance Spectroscopy (NMR), galangal acetate was particularly thermally labile. The steam distilled essential oil (SDEO) of AO (0.14% on wet basis) contained 80 compounds (number of component, %): monoterpene hydrocarbon (21, 13.83%); oxygenated monoterpene (17, 27.08%); sesquiterpene hydrocarbon (20, 31.03%), and oxygenated sesquiterpene (20, 21.85%), respectively. However, no spicy wasabi-like constituent remained in SDEO. Alternatively, n-hexane, EtAc, and methanol extracts of AO all showed potent DPPH- and superoxide anion-scavenging activity. Conclusively, SDEO although contains 80 volatiles, galangal acetate is absent due to thermal instability. Galangal acetate exhibits pleasant "Wasabi-like taste" for which we have successively developed an integrated process for mass production.
Asunto(s)
Acetatos/análisis , Alpinia/química , Manipulación de Alimentos , Aceites Volátiles/análisis , Rizoma/química , Antioxidantes/análisis , Asia , Cromatografía de Gases y Espectrometría de Masas , Hexanos/química , Isotiocianatos/análisis , Metanol/química , Extractos Vegetales/análisis , Espectrometría de Masas en Tándem , GustoRESUMEN
Rhizoma A. officinarum (Hance) Farw, synonymously is called rhizoma galangae or smaller galangal (hereafter abbreviated as AO). Numerous studies reported that AO possesses anti-inflammatory, anticancer, chemoprotective, antibacterial, antifungal and diuretic properties. To understand whether AO exhibits antihyperlipidemic bioactivity and what is the mechanism of action, we performed chemical and animal studies using hamsters (age: 4 weeks, body weight: 45 ± 4 g). The grouping of the animals was as follows: control, high fat (HF) diet, HF + AO2%, HF + AO4%, HF + AO6%, HF + AO8% and HF + AO10%. AO contained curcumin 5.67 mg g(-1) (on wet basis), crude fiber 1.3% ± 0.0%, soluble diet fiber 92 ± 2 mg g(-1), insoluble diet fiber 502 ± 5 mg g(-1), and phytosterols 63.9 ± 1.6 mg/100 g. Its methanolic extract consisted of high polyphenolics 4927.8 ± 101.1 mgGAE/100 g and flavonoids 593.2 ± 22.2 mgQE/100 g. The enlarged organs, including liver, kidney, and spleen, which were elicited by HF were completely alleviated by AO supplement diets. Levels of serum cholesterol, triglyceride, LDL-C, HDL-C and LDL-C/HDL-C ratio for the control originally were 138 ± 6, 98 ± 4, 40 ± 5, 168 ± 7 mg dL(-1) and 0.24, which were elevated by HF to 319 ± 12, 223 ± 13, 108 ± 11, 194 ± 6 mg dL(-1) and 0.05, and alleviated completely by HF + AO8% and HF + AO10%. In vitro, AO extracts showed potent DPPH free radical-scavenging and superoxide anion scavenging capabilities. In vivo, AO (at dose ≥8%) dose-dependently alleviated levels of superoxide dismutase, catalase, GSH, and MDA to 117 ± 6.9 U mL(-1), 32.9 ± 3.7 U mL(-1), 7.0 ± 1.7 µmol mL(-1) and 1.8 ± 0.4 nmol L(-1), respectively, exhibiting the remarkable antioxidative and antihyperlipidemic effects of AO. Conclusively, we are the first to report the occurrence of curcumin in rhizoma A. officinarum. Curcumin synergistically elicits promising anti-dyslipidemic bioactivity with coexisting total polyphenolics, dietary fibers and phytosterols.
Asunto(s)
Alpinia/química , Curcumina/administración & dosificación , Fibras de la Dieta/administración & dosificación , Medicamentos Herbarios Chinos/administración & dosificación , Hiperlipidemias/tratamiento farmacológico , Hipolipemiantes/administración & dosificación , Fitosteroles/administración & dosificación , Animales , Colesterol/sangre , Cricetinae , Sinergismo Farmacológico , Humanos , Hiperlipidemias/sangre , Masculino , Mesocricetus , Triglicéridos/sangreRESUMEN
Gallic acid (3,4,5-trihydroxybenzoic acid) (GA) occurs in many plants. The adverse effects of GA are seldom cited. GA (6-14 µM) provoked the hemorrhagic liposis of the cervical muscles and intracranial hemorrhage. The cause of these pathological events and the method for prevention are still lacking. Using the chicken embryo model and some selected nutraceutics such as folate, glutathione (GSH), N-acetylcysteine, and vitamin E (Vit E), we carried out this study. Results revealed that the action mechanism of GA involved (i) inducing hypoxia with upregulated gene hif-1α and downregulated ratio vegf-r2/vegf-a, leading to dys-vascularization and myopathy; (ii) impairing cytochrome c oxidase; (iii) stimulating creatine kinase and lactate dehydrogenase release; (iv) eliciting carnitine accumulation and liposis via downregulating gene CPT1; (v) suppressing superoxide dismutase and stimulating NO, H2O2, and malondialdehyde; and (vi) depleting erythrocytic and tissue GSH, resulting in hemorrhage. When both Vit E and GSH were applied to the day 1 chicks, a better alleviation effect was revealed. Conclusively, GA potentially exhibits adverse effect by eliciting hemorrhagic liposis of cervical muscles and cerebral hemorrhage. Supplementation with GSH, Vit E, and N-acetylcysteine is able to ameliorate these adverse effects, warranting the importance of restricting the clinical phytotherapeutic doses of GA and related compounds.
Asunto(s)
Hemorragia Cerebral/inducido químicamente , Ácido Gálico/efectos adversos , Músculos del Cuello/efectos de los fármacos , Acetilcisteína/farmacología , Animales , Embrión de Pollo , Suplementos Dietéticos , Relación Dosis-Respuesta a Droga , Dislipidemias/inducido químicamente , Ácido Gálico/farmacología , Glutatión/farmacología , Subunidad alfa del Factor 1 Inducible por Hipoxia/metabolismo , Músculos del Cuello/patología , Factor A de Crecimiento Endotelial Vascular/metabolismo , Receptor 2 de Factores de Crecimiento Endotelial Vascular/metabolismo , Vitamina E/farmacologíaRESUMEN
Schisandra chinensis (Turz Baill) (S. chinensis) (SC) fruit is a hepatoprotective herb containing many lignans and a large amount of polysaccharides. A novel polysaccharide (called SC-2) was isolated from SC of MW 841 kDa, which exhibited a protein-to-polysaccharide ratio of 0.4089, and showed a characteristic FTIR spectrum of a peptidoglycan. Powder X-ray diffraction revealed microcrystalline structures within SC-2. SC-2 contained 10 monosaccharides and 15 amino acids (essential amino acids of 78.12%w/w). In a HepG2 cell model, SC-2 was shown by MTT and TUNEL assay to be completely non-cytotoxic. A kinetic analysis and fluorescence-labeling technique revealed no intracellular disposition of SC-2. Combined treatment of lignans with SC-2 enhanced the intracellular transport of schisandrin B and deoxyschisandrin but decreased that of gomisin C, resulting in alteration of cell-killing bioactivity. The Second Law of Thermodynamics allows this type of unidirectional transport. Conclusively, SC-2 alters the transport and cell killing capability by a "Catcher-Pitcher Unidirectional Transport Mechanism".
Asunto(s)
Frutas/química , Lignanos/metabolismo , Moduladores del Transporte de Membrana/farmacología , Peptidoglicano/farmacología , Extractos Vegetales/farmacología , Schisandra/química , Análisis de Varianza , Transporte Biológico/efectos de los fármacos , Transporte Biológico/fisiología , Células Hep G2 , Humanos , Etiquetado Corte-Fin in Situ , Peptidoglicano/análisis , Extractos Vegetales/análisis , Espectroscopía Infrarroja por Transformada de Fourier , Sales de Tetrazolio , Tiazoles , Difracción de Rayos XRESUMEN
Ferulic acid (4-hydroxy-3-methoxycinnamic acid) (FA) is a ubiquitous health beneficial phenolic acid. Although FA has shown a diversity of biological activities including anti-inflammatory, antihypercholesterolemic and anticancer bioactivities, studies revealing its adverse effects are accumulating. Recently, 3D-cultures are shown to exhibit uniquely biological behaviors different from that of 2D cultures. To understand whether the cytotoxicity of FA against the T24 cell line (a bladder cancer cell line) in 2D-culture could consistently retain similar bioactivity if cultured in the 3D-systems, we conducted this experiment with 2 mM FA. Much higher cytotoxicity was found for 3D- than 2D-culture, showing (2D vs. 3D): apoptotic rates, 64% and 76%; cell killing rates, 3.00 × 10(5) cells mmol(-1)·h(-1) and 2.63 × 10(6) cells mmol(-1)·h(-1), attaining a 8.77-fold. FA upregulated the activities at 72 h (2D vs. 3D in folds that of control): SOD, 1.73-folds (P < 0.05) versus 3.18 folds (P < 0.001); and catalase, 2.58 versus 1.33-folds. Comparing to the control (without FA), Bcl-2 was prominently downregulated while Bax, caspase-3 and cleaved caspase-9 were more upregulated in 3D-cultures (P < 0.05). Conclusively, different microenvironments could elicit different biological significance which in part can be ascribed to different mass transport rate.
Asunto(s)
Microambiente Celular/efectos de los fármacos , Ácidos Cumáricos/toxicidad , Neoplasias de la Vejiga Urinaria/patología , Transporte Biológico/efectos de los fármacos , Western Blotting , Caspasa 3/metabolismo , Caspasa 9/metabolismo , Catalasa/metabolismo , Técnicas de Cultivo de Célula , Muerte Celular/efectos de los fármacos , Línea Celular Tumoral , Forma de la Célula/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Humanos , Mitocondrias/efectos de los fármacos , Mitocondrias/metabolismo , Modelos Biológicos , Transducción de Señal/efectos de los fármacos , Superóxido Dismutasa/metabolismo , Neoplasias de la Vejiga Urinaria/enzimología , Neoplasias de la Vejiga Urinaria/ultraestructura , Proteína X Asociada a bcl-2/metabolismo , Proteína Letal Asociada a bcl/metabolismoRESUMEN
BACKGROUND: Guava leaf tea (GLT), exhibiting a diversity of medicinal bioactivities, has become a popularly consumed daily beverage. To improve the product quality, a new process was recommended to the Ser-Tou Farmers' Association (SFA), who began field production in 2005. The new process comprised simplified steps: one bud-two leaves were plucked at 3:00-6:00 am, in the early dawn period, followed by withering at ambient temperature (25-28 °C), rolling at 50 °C for 50-70 min, with or without fermentation, then drying at 45-50 °C for 70-90 min, and finally sorted. RESULTS: The product manufactured by this new process (named herein GLTSF) exhibited higher contents (in mg g(-1), based on dry ethyl acetate fraction/methanolic extract) of polyphenolics (417.9 ± 12.3) and flavonoids (452.5 ± 32.3) containing a compositional profile much simpler than previously found: total quercetins (190.3 ± 9.1), total myricetin (3.3 ± 0.9), total catechins (36.4 ± 5.3), gallic acid (8.8 ± 0.6), ellagic acid (39.1 ± 6.4) and tannins (2.5 ± 9.1). CONCLUSION: We have successfully developed a new process for manufacturing GLTSF with a unique polyphenolic profile. Such characteristic compositional distribution can be ascribed to the right harvesting hour in the early dawn and appropriate treatment process at low temperature, avoiding direct sunlight.
Asunto(s)
Agricultura/métodos , Bebidas , Hojas de la Planta/química , Polifenoles/análisis , Psidium/química , Luz Solar , Temperatura , Catequina/análisis , Ácido Elágico/análisis , Manipulación de Alimentos/métodos , Ácido Gálico/análisis , Preparaciones de Plantas/química , Quercetina/análisis , Taninos/análisisRESUMEN
CONTEXT: The extraction method and the crude wound healing effects of sacchachitin from Ganoderma tsugae Murr. (Ganodermataceae) has been cited. However, its purity is still largely limited. OBJECTIVE: An improvement of the fractionation protocol to purify the sacchachitin from Ganoderma lucidum L. (Ganodermataceae) (SGL) is needed. METHODS: Fruiting bodies were extracted with double distilled water and subsequently the residue treated with 95% ethanol and then 40% ethanol. After being filtered, the pH of the supernatant was adjusted to 4.0 with 1 N HCl and lyophilized. The supernatant was added (3:1 v/v) ethanol, the precipitate was collected, 2% NaOH was added and refluxed. The supernatant was collected with pH adjusted to 4.0, then treated with 10% potassium hydroxide (KOH) with repeating acid precipitation and (3:1) ethanol precipitation twice more to obtain the sacchachitin. RESULTS: SGL had a hexosamine content 16.3% (w/w), firmly linked to a talomannan. Its Fourier Transform Infrared Spectroscopy (FTIR) spectrum revealed specific absorption (in cm(-1)) ν(O-H) 3455.5 b,s, amide ν(C=O) 1678.5, and amide I° δ(N-H) 1550.4. The percentage deacetylation degree was 37.6 and 39.4% for SGL and MSC, respectively. As contrast, MSC contained only 6.6% of hexosamine with a low protein/carbohydrate ratio 0.35 comparing to 0.82 for SGL. SGL was only moderately strong antioxidant regarding the anti-DPPH, antihydroxyl free radical, and antisuperoxide anion capabilities, exhibiting an IC(33) values of 10 mg/mL (the highest scavenging capability never exceeding 33%), 0.9 mg/mL, and 4.8 mg/mL, respectively. CONCLUSION: We have successfully isolated the pure sacchachitin from the fruiting bodies of G. lucidum that exhibits potent antioxidative activity and may be useful in fabrication of the artificial skin composite substitute.
Asunto(s)
Antioxidantes/farmacología , Quitina/farmacología , Polisacáridos/farmacología , Reishi/química , Antioxidantes/química , Antioxidantes/aislamiento & purificación , Quitina/química , Quitina/aislamiento & purificación , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/aislamiento & purificación , Cuerpos Fructíferos de los Hongos , Radical Hidroxilo/metabolismo , Polisacáridos/química , Polisacáridos/aislamiento & purificación , Espectroscopía Infrarroja por Transformada de Fourier , Superóxidos/metabolismoRESUMEN
Antrodia cinnamomea has a diversity of therapeutic effects including anticancer properties. Its neuroprotective effect is rarely cited. We hypothesized that due to its high phenol, triterpenoid, and adenosine contents, it might exhibit a potent neuroprotective effect. The PC12 cell model was used to investigate its pharmaceutical effects. Congo red staining was used to identify the activation of Aß25-35. Chemical analysis indicated that the ethanolic extract of Antrodia cinnamomea contained a huge amount (mg/g ethanolic extract of Antrodia cinnamomea) of polyphenolics (133 ± 7), flavonoids (114 ± 6), triterpenoids (175 ± 26), and adenosine (370 ± 17). When tested with Aß25-35 (15 µM), the cell viability was suppressed in a dose-dependent fashion with an IC50 value of 10 µM. The biochemical parameters upregulated by Aß25-35 (15 µM) involved TNF-α, ROS, MDA, NO, and the intracellular calcium ions. These adverse effects were effectively ameliorated by the ethanolic extract of Antrodia cinnamomea (1 µg/mL). The Western blot analysis revealed that Aß25-35 downregulated BcL-2/Bax and upregulated cleaved caspases-9 and - 3 without affecting cleaved caspase-8. The G2/M arrest elicited by Aß25-35 was ameliorated by the ethanolic extract of Antrodia cinnamomea. TUNEL assay confirmed the apoptosis, and the ethanolic extract of Antrodia cinnamomea downregulated adenosine A1 and adenosine A2A receptors. Taken together, Aß25-35 tends to induce neurotoxicity on PC12 cells. The ethanolic extract of Antrodia cinnamomea is capable of suppressing its neurotoxicity by rescuing the mitochondrial apoptosis pathway and simultaneously by downregulating adenosine A1 and adenosine A2A receptors to retard neurodegeneration and memory dysfunction.
Asunto(s)
Péptidos beta-Amiloides/farmacología , Antrodia/química , Apoptosis/efectos de los fármacos , Mitocondrias/metabolismo , Fragmentos de Péptidos/farmacología , Agonistas del Receptor Purinérgico P1/metabolismo , Péptidos beta-Amiloides/análisis , Animales , Relación Dosis-Respuesta a Droga , Flavonoides/farmacología , Mitocondrias/efectos de los fármacos , Fármacos Neuroprotectores , Células PC12 , Fragmentos de Péptidos/análisis , Polifenoles/farmacología , Ratas , Triterpenos/farmacologíaRESUMEN
BACKGROUND: Valproic acid (VPA) is an antiepileptic and anti-migraine prophylactic drug. VPA exhibits two severe side effects, namely acute liver toxicity and teratogenicity. These side effects are usually seen at the genetic and somatic levels. The cited action mechanisms involve inhibition of histone deacetylase, hypofolatenemia, hyperhomocysteinemia, and reactive oxidative stress. The proteomic information associated with VPA teratogenicity is still unavailable. We hypothesized that proteomic analysis might help us identify functional proteins that could be relevantly affected by VPA, and this phenomenon could be very sensitive in early embryonic stage, resulting in VPA teratogenicity. METHODOLOGY/PRINCIPAL FINDINGS: Proteomic analysis on the chicken embryos at Hamburger and Hamilton (HH) stage 28 showed that there were significant downregulations of ovotransferrins, carbonic anhydrase-2, retinol binding protein-4 (RBP4), NADH cytochrome b5 reductase 2 (CYB5R2), apolipoprotein A1, and protein SET, together with upregulation of 60S ribosomal protein L22. Among these, RBP4 was the most significantly downregulated (-32%). Kinetic analysis suggested that this situation could trigger hypervitaminosis A (+39.3%), a condition that has been well known to induce teratogenesis.. CONCLUSIONS/SIGNIFICANCE: This is the first report showing that VPA dowregulates RBP4. Our finding not only has led to a possible mechanism of VPA teratogenesis, but also has initiated new preventive strategies for avoiding VPA teratogeneis.
Asunto(s)
Hipervitaminosis A/genética , Proteínas Plasmáticas de Unión al Retinol/genética , Teratógenos/metabolismo , Ácido Valproico/farmacología , Vitamina A/metabolismo , Anomalías Inducidas por Medicamentos , Animales , Embrión de Pollo , Desarrollo Embrionario/efectos de los fármacos , Desarrollo Embrionario/genética , Histona Desacetilasas/metabolismo , Homeostasis/efectos de los fármacos , Homeostasis/genética , Peróxido de Hidrógeno/metabolismo , Hipervitaminosis A/metabolismo , Cinética , Fenotipo , Proteómica , Proteínas Plasmáticas de Unión al Retinol/metabolismo , Superóxido Dismutasa/metabolismo , Teratógenos/toxicidad , Ácido Valproico/toxicidad , Vitamina A/toxicidadRESUMEN
BACKGROUNDS & AIMS: The long term therapeutic effect of ferulic acid (FA) and gallic acid (GA) in treatment of chronic kidney disease (CKD) has been lacking. METHODS: Doxorubicin (DR, Adriamycin)-induced CKD rat model was established for this study. RESULTS: DR significantly reduced levels of serum albumin, GOT, GPT, RBC, TNF-α, and urinary creatinine and elevated serum cholesterol, TG, BUN, creatinine, uric acid, WBC, platelet count, and IL-6. In DRCKD rats, FA and GA significantly increased kidney weight and glomerular volume. FA reduced glomerular filtration rate but GA did not. FA enhanced more collagen deposition than GA in renal cortex and glomeruli. Both FA and GA showed crucial hyperlipidemic activity. The inhibitory effects of FA and GA on MMP-2 were very comparable. GA suppressed MMP-2 more effectively than FA in DRCKD rats. Both FA and GA induced SOD elevation and MDA elimination. In DRCKD rats, Western blot analysis indicated that FA further up-regulated CD34, α-SMA, tissue pDGFR, p-PDGFR, and TGF-ß; and down-regulated p-PI3K, and p-Akt. Since both PDGF-BB and TGF-ß are considered to induce kidney prefibrosis stage, GA was proved to be more beneficial in this regard. CONCLUSIONS: GA tends to protect the CKD while FA is not recommended for the long term CKD therapy.
Asunto(s)
Antioxidantes/efectos adversos , Ácidos Cumáricos/efectos adversos , Suplementos Dietéticos/efectos adversos , Ácido Gálico/efectos adversos , Riñón/patología , Insuficiencia Renal Crónica/dietoterapia , Animales , Antioxidantes/uso terapéutico , Colágeno/metabolismo , Ácidos Cumáricos/uso terapéutico , Modelos Animales de Enfermedad , Fibrosis , Ácido Gálico/uso terapéutico , Regulación de la Expresión Génica , Tasa de Filtración Glomerular , Hiperlipidemias/etiología , Hiperlipidemias/prevención & control , Riñón/metabolismo , Riñón/fisiopatología , Masculino , Tamaño de los Órganos , ARN Mensajero/metabolismo , Ratas , Ratas Sprague-Dawley , Insuficiencia Renal Crónica/metabolismo , Insuficiencia Renal Crónica/patología , Insuficiencia Renal Crónica/fisiopatología , Transducción de Señal , Pruebas de Toxicidad CrónicaRESUMEN
The teratogenicity of antiepilepsy drug valproic acid (VPA) mostly is found in genetic and somatic levels, causing teratogenesis involving neurotubular defects (NTDs), anencephaly, lumbosacral meningomyelocele, and leg dysfunction due to spina bifida aperta. A diversity of nutraceutics have been tried to alleviate the risk of VPA-teratogenicity. The effect was varying. In order to promote the preventive prescription, to find out its action mechanism can be rather crucial. We used chicken embryo model to try the effect of folic acid (FA), ascorbic acid (AA), and N-acetyl cysteine (NAC). VPA at 30mM showed the higher malformation rate (66.7%) with the least mortality (22.2%). Pathological findings indicated that the cervical muscle was more susceptible to VPA injury than the ankle muscle. VPA downregulated levels of superoxide dismutase (SOD), glutathione (GSH), histone deacetylase (HDAC) and folate, and upregulated H(2)O(2) and homocysteine. FA, AA, and NAC significantly upregulated SOD, but only AA alone activated GSH. AA and NAC downregulated H(2)O(2), while FA was totally ineffective. All three nutraceutics comparably rescued HDAC with simultaneously suppressed homocysteine accumulation and folate re-elevation, although less effectively by NAC. Based on these data, we conclude VPA possesses "Multiple Point Action Mechanism". In addition to affecting the cited transcription and translation levels, we hypothesize that VPA competitively antagonize the glutamic acid to couple with pteroic acid in biosynthesis of dihydrofolic acid (DHFA). H(2)O(2) directly destroyed the NADPH reducing system at dihydrofolate reductase (DHFR) and methylene tetrahydrofolate reductase (MTHFR) levels, while completely restored by AA, an implication in preservation of intact apoenzymes. In addition, the GSH-GSSG system is sandwiched between the reducing systems NADPH/NADP and DHA-AA, its net balance is highly dependent on in situ in vivo Redox state, hence folic acid transformation is varying. To rescue the VPA-induced teratogenicity, simultaneous multiple prescriptions are suggested.
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Acetilcisteína/farmacología , Anticonvulsivantes/antagonistas & inhibidores , Anticonvulsivantes/toxicidad , Antioxidantes/farmacología , Ácido Ascórbico/farmacología , Ácido Fólico/farmacología , Teratógenos , Ácido Valproico/antagonistas & inhibidores , Ácido Valproico/toxicidad , Vitaminas/farmacología , Acetilcisteína/sangre , Animales , Ácido Ascórbico/sangre , Embrión de Pollo , Cromatografía Líquida de Alta Presión , Ácido Fólico/sangre , Deformidades del Pie/inducido químicamente , Glutatión/metabolismo , Miembro Posterior/anomalías , Histona Desacetilasas/metabolismo , Homocisteína/metabolismo , Peróxido de Hidrógeno/metabolismo , Articulaciones/anomalías , Articulaciones/patología , Músculo Esquelético/anomalías , Músculo Esquelético/patología , Neovascularización Fisiológica/efectos de los fármacos , Superóxido Dismutasa/metabolismo , Adhesión del Tejido , Vitaminas/sangreRESUMEN
CONTEXT: In utilization of Alpinia zerumbet (Pers.) Burtt and Smith (Zingiberaceae) (AZ), usually the angiocarps are discarded without further use. OBJECTIVE: We speculate whether the angiocarps could show hypolipidemic effect. METHODS AND METHODS: Several diets were prepared: Alpinia seed powder (ASP); Alpinia seed powder/husk (ASH): 40/60; and Alpinia seed essential oil (ASO): 0.01-0.10%. Sprague-Dawley rats divided into 11 groups were fed these diets for 8 weeks and tested for the hypolipidemic bioactivity. RESULTS: The fecal neutral cholesterol excretion was increased, and the serum total triglyceride (TG) was significantly reduced from 153.7 mg/dL in the high-fat group (H) to 114.3-119.8 mg/dL by ASO; to 116.3-147.9 mg/dL by ASP; and to 116.2-145.3 mg/dL by ASH. Activity of superoxide dismutase (SOD) and glutathione peroxidase (GPX) were almost unaffected. The high-density lipoprotein (HDL) levels were mostly raised by ASO to 180.3-200.8 mg/dL. The lowdensity lipoprotein (LDL) levels were mostly reduced to 66.8-82.6 mg/dL by ASH. The level of arachidonic acid was mostly raised to 0.50-0.60% by ASO, compared with 0.37% of group H. More importantly, the significant reduction in hepatic TG and total cholesterol (TC) implicated a crucial liver protective effect. DISCUSSION AND CONCLUSION: ASP and ASH consisted of high crude-fiber content, while ASO consisted of seed essential oil. Both the seed essential oil and the whole powder of AZ previously had been reported to possess potent hypolipidemic bioactivity. Conclusively, the hypolipidemic effect can be attributed to the combined effect of the essential oil and the crude fiber.
Asunto(s)
Alpinia/química , Frutas/química , Hipolipemiantes/farmacología , Animales , Enfermedad Hepática Inducida por Sustancias y Drogas/prevención & control , Colesterol/sangre , Colesterol/química , Cricetinae , Dieta , Medicamentos Herbarios Chinos , Ácidos Grasos/metabolismo , Heces/química , Cromatografía de Gases y Espectrometría de Masas , Glutatión Peroxidasa/análisis , Hidrólisis , Metabolismo de los Lípidos/efectos de los fármacos , Lipoproteínas/sangre , Hígado/efectos de los fármacos , Hígado/metabolismo , Masculino , Mesocricetus , Metilación , Aceites Volátiles/aislamiento & purificación , Aceites Volátiles/farmacología , Semillas/química , Superóxido Dismutasa/análisisRESUMEN
Fermented soybean liquid (FSL) has been well cited for its broad spectrum of biological effects, yet its documented gastropeptic ulcer (GPU) ameliorating effect is still lacking. It was hypothesized that to avoid the injury exerted by gastric fluid, HP has to be sheltered in chyme emulsions immediately on infection. The HP urease (HPU) and the acidic proton pump (PP) may act as the "two-point pH modulator" to maintain an optimum pH between 6 and 7, and FSL is able to destroy such a modulating mechanism. FSL exhibited higher contents of isoflavonoids (2.5-17.3-fold) and essential amino acids (1.5-4.0-fold) than the nonfermented. FSL administered at 1 g/20 mL tid for 3 months eradicated Helicobacter pylori (HP) by 82% in 37 volunteers having GPU (p < 0.20); simultaneously, the plasma conjugated diene and TBARs levels were significantly resumed (p < 0.05). Kinetic analysis based on the conventional "urease theory" revealed that a cluster of 2.0 × 10(9) of HP cells is required for a single attack in the gastric lumen at pH 1.0-2.5. To verify the hypothesis, chyme-shelter testing was conducted in artificial gastric fluid (pH 2.4 ± 0.20). Results showed the HP cell viability was time- and size-dependent. At 20 min of contact time, the viability was 100, 4.2, 31.4, 43.3, 57.2, and 82.6%, respectively, in intact, dispersed, and particulate chymes (mesh sizes 80, 60, 40, and 20). The corresponding data became 96.2, 0.0, 14.5, 18.5, 21.3, and 28.6%, respectively, at a contact time of 40 min. Conclusively, the kinetic analysis and the chyme-shelter testing revealed that direct infection by bare HP cells is unlikely in real status. FSL is beneficial to GPU most probably due to its ability to raise blood alkalinity levels, destroying the PP and its ROS suppressing effect.
Asunto(s)
Proteínas Bacterianas/metabolismo , Glycine max/química , Infecciones por Helicobacter/tratamiento farmacológico , Helicobacter pylori/efectos de los fármacos , Úlcera Péptica/tratamiento farmacológico , Preparaciones de Plantas/farmacocinética , Bombas de Protones/metabolismo , Ureasa/metabolismo , Aspergillus oryzae/metabolismo , Regulación hacia Abajo/efectos de los fármacos , Enterococcaceae/metabolismo , Femenino , Fermentación , Infecciones por Helicobacter/microbiología , Helicobacter pylori/enzimología , Helicobacter pylori/metabolismo , Humanos , Cinética , Masculino , Úlcera Péptica/microbiología , Preparaciones de Plantas/administración & dosificación , Glycine max/microbiologíaRESUMEN
Guava [Psidium guajava L. (Myrtaceae)] budding leaf extract (PE) has shown tremendous bioactivities. Previously, we found seven major compounds in PE, i.e., gallic acid, catechin, epicatechin, rutin, quercetin, naringenin, and kaempferol. PE showed a potentially active antiglycative effect in an LDL (low density lipoprotein) mimic biomodel, which can be attributed to its large content of polyphenolics. The glycation and antiglycative reactions showed characteristic distinct four-phase kinetic patterns. In the presence of PE, the kinetic coefficients were 0.000438, 0.000060, 0.000, and -0.0001354 ABS-mL/mg-min, respectively, for phases 1 to 4. Computer simulation evidenced the dose-dependent inhibition model. Conclusively, PE contains a large amount of polyphenolics, whose antiglycative bioactivity fits the inhibition model.
Asunto(s)
Flavonoides/farmacocinética , Lipoproteínas LDL/antagonistas & inhibidores , Modelos Biológicos , Fenoles/farmacocinética , Extractos Vegetales/farmacocinética , Psidium , Agua/metabolismo , Células Cultivadas , Células Epiteliales/efectos de los fármacos , Células Epiteliales/metabolismo , Flavonoides/aislamiento & purificación , Productos Finales de Glicación Avanzada , Glicosilación/efectos de los fármacos , Humanos , Lipoproteínas LDL/metabolismo , Fenoles/aislamiento & purificación , Extractos Vegetales/aislamiento & purificación , Hojas de la Planta , PolifenolesRESUMEN
To find in vivo behaviors of an antioxidant when used as an adjuvant cancer therapy, a more detailed integrated pharmacokinetic scheme is needed. Major reaction parameters associated with the sequential routes from ingestion to decay of an antioxidant were used in mathematical analysis, which included absorption rate coefficient k(a), quenching rate coefficient of the antioxidant k(q1) and tissue quenching rate coefficient k(r). The model was then treated with computer simulation using cited decay rate coefficients and some assumed parameters. When intestinal absorption rate coefficient k(a) becomes larger, retention time of antioxidant in plasma would be prolonged. moreover, k(a) had no effect on either quenching ability of antioxidants or tissue recovering capability. in quenching plasma ROS, the larger the quenching coefficient k(q1), the shorter peak- and the life-times would be for the secondary free radicals that are formed in primary quenching. Conclusively, it is suggestive to prescribe an antioxidant therapy with an appropriate values of k(a) and larger values of k(q1).
Asunto(s)
Antineoplásicos/farmacocinética , Antineoplásicos/uso terapéutico , Antioxidantes/farmacocinética , Antioxidantes/uso terapéutico , Terapias Complementarias , Modelos Biológicos , Neoplasias/tratamiento farmacológico , Animales , Antineoplásicos/sangre , Antineoplásicos/química , Antioxidantes/química , Carotenoides/sangre , Carotenoides/química , Carotenoides/farmacocinética , Carotenoides/uso terapéutico , Simulación por Computador , Suplementos Dietéticos , Semivida , Humanos , Absorción Intestinal , Licopeno , Manitol/sangre , Manitol/química , Manitol/farmacocinética , Manitol/uso terapéutico , Neoplasias/sangre , Especies Reactivas de Oxígeno/sangre , Especies Reactivas de Oxígeno/químicaRESUMEN
In folkloric plant medicines, Alpinia zerumbet (AZ) has been popularly recognized as an exellent hepatoprotector. To search for a good high-density lipoprotein cholesterol (HDL-C) elevating herbal preparation, we examined AZ for its antioxidant and hypolipidaemic bioactivities, especially its HDL-C elevating activity. AZ seeds contain 0.51% essential oils (SO), which are comprised of monoterpenoids, oxygenated monoterpenoids, sesquiterpenoids, oxygenated sesquiterpenoids, aldehydes, acid, and esters. Gas chromatography/mass spectrometry analysis indicated that most of the monoterpenes and sesquiterpenes were recoverable in pentane eluent, whilst the oxygenated monoterpenoids and sesquiterpenoids remained in ether eluent. The high contents of rutin, quercetin, and polyphenolics in ethanolic extract of AZ seeds exhibit moderate antilipoperoxidative but potent DPPH free radical scavenging bioactivities. Conclusively, both seed powder (SP) and SO are effective hypolipidaemics with amazingly potent HDL-C elevating capabilities. On the basis of hepatoprotectivity, SP is a more feasible hypolipidemic agent as well as a promising HDL-C elevating plant medicine.
Asunto(s)
Alpinia/química , HDL-Colesterol/sangre , Extractos Vegetales/farmacología , Animales , LDL-Colesterol/sangre , Cricetinae , Flavonoides/análisis , Peroxidación de Lípido/efectos de los fármacos , Hígado/anatomía & histología , Masculino , Mesocricetus , Aceites Volátiles/análisis , Tamaño de los Órganos/efectos de los fármacos , Fenoles/análisis , Polifenoles , Quercetina/análisis , Rutina/análisis , Terpenos/análisisRESUMEN
Using the low-density lipoprotein (LDL), collagen, and thrombin models, we report here that the rosemary extracts (REs), either the aqueous (REw) or the acetonic (REA), all possessed many antiglycation-related features, and the effective concentrations required were as follows: 0.1 mg/mL for suppressing the relative electrophoretic mobility, 1.3 microg/mL for anticonjugated diene induction, 0.5 mg/mL for inhibition of thiobarbituric acid reactive substances production, 0.1 mg/mL for AGEs (advanced glycation end products) formation, 0.1 mg/mL to block glucose incorporation, and 0.05 mg/mL as an effective anti-antithrombin III. Using high-performance liquid chromatography/mass spectrometry, we identified five major constituents among eight major peaks, including rosmarinic acid, carnosol, 12-methoxycarnosic acid, carnosic acid, and methyl carnosate. In the LDL model, REA was proven to be more efficient than REw; yet, the reverse is true for the collagen and the thrombin III models, the reason of which was ascribed to the higher lipid-soluble antioxidant content (such as rosmarinic acid, carnosol, carnosic acid, 12-methoxycarnosic acid and methyl carnosate) in REA than in REw and the different surface lipid characteristics between LDL and collagen; although to act as anti-AGEs, both extracts were comparable. To assist the evidence, a larger 2,2-diphenyl-1-picrylhydrazyl radical scavenging capability with less total polyphenolic content was found in REA. We conclude that rosemary is an excellent multifunctional therapeutic herb; by looking at its potential potent antiglycative bioactivity, it may become a good adjuvant medicine for the prevention and treatment of diabetic, cardiovascular, and other neurodegenerative diseases.
Asunto(s)
Colágeno/química , Lipoproteínas LDL/química , Extractos Vegetales/farmacología , Rosmarinus/química , Trombina/química , Antioxidantes/análisis , Glicosilación/efectos de los fármacos , Extractos Vegetales/química , Hojas de la Planta/químicaRESUMEN
Experimentation with a physiomimic system and kinetic analysis exhibited four distinct reaction phases in LDL glycation despite of the type of inducer: glucose or glyoxal. LDL glycation was more sensitive to a status of hyperglycemia (such as 400 mg glucose/100 mL) as evidenced by the reaction order of 0.53. Glucose reacted intensively in the Initial Phase (reaction period 0-2h) which was identified to result from a parallel mechanism involving both the direct Schiff's product formation and the auto-oxidative cleavages. In contrast, a physiological level of glyoxal revealed merely a reaction order of only 0.09, implicitly indicating a far less sensitive glycation which can be attributed to a mechanism proceeding simply through a molecular Schiff's reaction. On treatment with Psidium guajava L. aqueous extract (PE) (0.01-0.625 mg/mL), a rather unique and significant inhibitory characteristic on LDL glycation was observed with a dose-dependent manner. We attributed such an effect of PE to its distinct abundance of polyphenolic content (165.61+/-10.39 mggallic acid equivalent (GAE)/g). Conclusively, PE is an excellent anti-LDL glycative agent whose potential therapeutic uses can be extended to the prevention of a variety of cardiovascular and neurodegenerative diseases associated with glycations.
Asunto(s)
Lipoproteínas LDL/metabolismo , Psidium , Glucosa/farmacología , Productos Finales de Glicación Avanzada/metabolismo , Glicosilación/efectos de los fármacos , Glioxal/farmacología , Humanos , Hiperglucemia/metabolismo , Técnicas In Vitro , Cinética , Lipoproteínas LDL/química , Lipoproteínas LDL/efectos de los fármacos , Modelos Biológicos , Extractos Vegetales/farmacología , Biología de SistemasRESUMEN
AIM: To study the change of lipid metabolism by antiandrogen therapy in patients with prostate cancer. MATERIALS AND METHODS: We studied with a 2.5 years follow-up the changes in plasma cholesterols (C), triglycerides (TG), lipoproteins (LP), and apolipoproteins (Apo) B-100, A-I, and A-II pro fi les in 24 patients of mean age 60 years with low risk prostate cancer (stage: T1cN0M0, Gleason score: 2-5) during treatment with cyproterone acetate (CPA) without surgical management or radiation therapy. RESULTS: Significant decreases of HDL-C, Apo A-I and Apo A-II and an increase of triglyceride levels in VLDL were induced by CPA. After a period of 2.5 years on CPA treatment, four patients out of twenty-four were found to be affected by coronary heart disease. CONCLUSIONS: Ischaemic coronary arteriosclerosis with an incidence rate of 16.6% as caused by prolonged CPA therapy is mediated through changes in HDL cholesterol, Apo A-I and Apo A-II pro fi les, other than the well-known hyperglyceridemic effect caused by estrogen.