Abelmoschus esculentus fractions potently inhibited the pathogenic targets associated with diabetic renal epithelial to mesenchymal transition.

Although Abelmoschus esculentus (AE) is known for anti-hyperglycemia, few reports have addressed its target. Our recent studies have focused on diabetic renal epithelial to mesenchymal transition (EMT), which plays a critical role in fibrosis that accompanies increasing vimentin and suggested signals DPP-4/AT-1/TGF-ß1. This study aimed to investigate whether AE is useful for preventing diabetic renal EMT. We used a succession of extractions and obtained the corresponding fractions F1-F5, each with its own individual properties: F1 inhibits high glucose-stimulated vimentin, AT-1, TGF-ß1, and DPP-4, and recovers E-cadherin in tubular cells; F2 decreases high glucose-induced vimentin, AT-1 and DPP-4; F3-F5 do not reduce the expression of vimentin. Chemical analysis revealed that F1 is rich of flavonoid glycosides especially quercetin glucosides, and pentacyclic triterpene ester. F2 contains a large amount of carbohydrates and polysaccharides composed of uronic acid, galactose, glucose, myo-inositol etc. In conclusion, AE has the potential to serve as an adjuvant for diabetic nephropathy, with F1 and F2 especially deserving further investigation and development.

Schisandra chinensis peptidoglycan-assisted transmembrane transport of lignans uniquely altered the pharmacokinetic and pharmacodynamic mechanisms in human HepG2 cell model.

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".

Selected nutraceutic screening by therapeutic effects on doxorubicin-induced chronic kidney disease.

SCOPE: The number of patients with chronic kidney disease (CKD) are increasing. Interventions such as controlling hypertension and specific pharmacologic options are recommended. Some nutraceutics may have benefits in this regard. METHODS AND RESULTS: Naringenin (a flavanon), catechin (a flavanol), and quercetin (a flavonol) and rutin (a flavonol rutinoside) were tried on CKD in a Sprague Dawley rat model. Results indicated quercetin to be the most effective therapeutic candidate with respect to renal edema, hypertension, serum creatinine, hematocrit, cardiopathy, aorta calcification, glomerular amyloidosis, erythrocyte depletion in bone marrow, collagen deposition, expressions of TNF-α, cleaved caspase-3, IκBα, PPARα, and serum insulin. But quercetin was only partially effective in restoring glomerular filtration rate, albuminuria, serum cholesterol, triglyceride, blood urea nitrogen (BUN), uric acid, malondialdehyde, superoxide dismutase; urinary BUN and urinary creatinine. As for signaling, quercetin was completely effective in alleviating the cleaved caspase-3, being only partially effective in suppressing Bax and Bad, restoring Bcl-2, and rescuing DNA damage. CONCLUSION: The CKD status cannot to be ameliorated by naringenin, rutin, and catechin. Comparatively, quercetin may be a better therapeutic candidate.

Structural Characteristics and Antioxidative Capability of the Soluble Polysaccharides Present in Dictyophora indusiata (Vent. Ex Pers.) Fish Phallaceae.

Dictyophora indusiata (Vent. ex Pers.) Fish Phallaceae (Chinese name Zhu-Sun, the bamboo fungi) has been used as a medicinal mushroom to treat many inflammatory, gastric and neural diseases since 618 AD in China. We hypothesize that the soluble polysaccharides (SP) present in D. indusiata and their monosaccharide profiles can act as an important role affecting the antioxidative capability, which in turn would influence the biological activity involving anti-inflammatory, immune enhancing and anticancer. We obtained six SP fractions and designated them as D1, a galactoglucan; D2, a galactan; D3, the isoelectrically precipitated riboglucan from 2% NaOH; D4, a myoinositol; D5 and D6, the mannogalactans. The total SP accounted for 37.44% w/w, their molecular weight (MW) ranged within 801-4656 kDa. D3, having the smallest MW 801 kDa, exhibited the most potent scavenging effect against the α,α-diphenyl-ß-picrylhydrazyl, •OH(-), and •O(2) (-) radicals, yielding IC(50) values 0.11, 1.02 and 0.64 mg mL(-1), respectively. Thus we have confirmed our hypothesis that the bioactivity of D. indusiata is related in majority, if not entirely, to its soluble polysaccharide type regarding the MW and monosaccharide profiles.

Fermented soybean liquid alleviated peptic ulcer through the destruction of acidic proton pump rather than suppression of urease of Helicobacter pylori: a kinetic analysis.

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.

Arabinogalactan present in the mountain celery seed extract potentiated hypolipidemic bioactivity of coexisting polyphenols in hamsters.

CONTEXT: Previously, we showed the essential oils (EO) of the mountain celery [Cryptotaenia japonica Hass (Umbelliferae)] seeds (MCS) to be a prominent hypolipidemic agent. OBJECTIVE: We hypothesized the aqueous extract (AE) of its seeds could also exhibit a comparable nutritional effect. MATERIALS AND METHODS: Experiments were carried out for compositional analysis, antioxidant assay, and hypolipidaemic assay with AE in hamsters. RESULTS: AE contained soluble arabinogalactan (AGal) with molecular weight (MW) 878 kDa. AE also was enriched in polyphenolics and flavonoids, reaching 30.4 and 2.20 mg/100 g, respectively. AGal consisted of eight monosaccharides (in mols %), galactose (28.75), arabinose (24.84), glucose (17.91), mannose (6.93), ribose (6.03), fucose (5.83), xylose (5.30), and rhamnose (4.41), with average MW 878 kDa. In vitro, AE showed potent ferrous chelating and DPPH scavenging effects but only moderate H2O2 scavenging capability. In hamsters, AE exhibited promising hypolipidemic bioactivity, in particular, the HDL-C and hepatic unsaturated fatty acid (UFA) biosynthesis regarding oleic, linoleic, and arachidonic acids. DISCUSSION AND CONCLUSION: The presence of AGal enhanced the hypolipidemic and antioxidative bioactivity of MCS. MCS is feasibly beneficial to the hepatic de novo UFA synthesis and the hypolipidemics as evidenced by hamster model.

Chemical synthesis of 9(Z)-octadecenamide and its hypolipidemic effect: a bioactive agent found in the essential oil of mountain celery seeds.

The unusual hypolipidemic activity of the methanolic fractionate of the essential oil (EOM) obtained from the mountain celery seed was previously reported. The most enriched 9(Z)-octadecenamide (oleamide) was speculated to be responsible for the relevant bioactivity. Chemically syntheized oleamide (CSO) yielded 85.1% with a purity of 98.6% when identified by RP-HPLC, FTIR, HREIMS, (1)H NMR, and (13)C NMR. CSO was tested for its antioxidative and hypolipidemic bioactivities. Results indicated CSO was potently hypolipidemic with regard to serum TG, TC, LDL-C, LDL-C/HDL-C, and hepatic TG (p < 0.05), but not for serum HDL-C and hepatic TC. In addition, CSO exhibited only poor antioxidative activity, implicating the possibility that the hypolipidemic and antioxidative bioactivity of original EOM was due to another coexisting constituent, probably gamma-selinene. Conclusively, oleamide is a potent hypolipidemic agent as regarding its effects on decreasing serum TG, TC, LDL-C and hepatic TG.

Insulin secretagogue bioactivity of finger citron fruit (Citrus medica L. var. Sarcodactylis Hort, Rutaceae).

Finger citron [Citrus medica L. var. Sarcodactylis Hort, Rutaceae] (FC) fruits, widely cultivated in Japan, the southern provinces of China and Taiwan, are commonly used as functional vegetables and preserved as sweetmeats. Previously we identified the major compounds in essential oils (% in EO) of FC fruits to be d-limonene (51.24), gamma-terpenene (33.71), alpha-pinene (3.40), and beta-pinene (2.88). Documented evidence on its insulin secretion characteristics is still lacking. In parallel to compositional analysis, we performed in vivo the safety, hypoglycemic, and antidiabetic tests in Sprague-Dawley-SPF rats and Wistar DIO rats respectively. By kinetic analysis on the hypoglycemic patterns of the intraperitoneal glucose tolerance (IPGTT) and the insulin-glucose tolerance tests (IGTT), its insulin secretagogue effect was confirmed. In conclusion, FC fruits that concomitantly possess insulin secretagogue and slimming effects would be very beneficial to type 2 diabetes mellitus patients.

Relevance of phenolic diterpene constituents to antioxidant activity of supercritical CO(2) extract from the leaves of rosemary.

Isolation of phenolic diterpene constituents from the freeze-dried leaves of Rosmarinus officinalis has been obtained by supercritical extraction with carbon dioxide. To determine the ideal conditions for the maximum yield of extract, nine different conditions using three levels of pressures (3000, 4000 and 5000 psi) in combination with three temperatures at 40, 60 and 80 degrees C, respectively, in combination with the analyses of the corresponding antioxidant activities and constituents which existed in extracts has been investigated. The antioxidant activity of each obtained extract was determined by using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals test. GC/MS method was used as an alternative to conventional HPLC method for the determination of the principal antioxidant constituents in extract, including phenolic diterpenes carnosic acid (CA) and carnosol (CAL). The confirmation of CA and CAL in extract was forward performed by subjecting HPLC isolates from extract into an ion trap mass spectrometer through an electrospray ionization (ESI) interface for MS/MS analysis. These results indicate that an ideal extraction process was obtained at 5000 psi and 80 degrees C with an extraction yield of 4.27% (w/w) and rich in phenolic antioxidants CA and CAL as contents of 35.23 and 0.46 mg g(-1) in extract, respectively.