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Microbial metabolism of pseudoprotodioscin.

Microbial transformation of the furostanol saponin pseudoprotodioscin ( 1) using Aspergillus fumigatus resulted in the isolation of two new steroidal metabolites, 3- O-[bis- alpha- L-rhamnopyranosyl-(1-->2 and 1-->4)- beta- D-glucopyranosyl]-22 R,25 R-spirost-5-ene-3 beta,20 alpha-diol ( 2) and 3- O-[bis- alpha- L-rhamnopyranosyl-(1-->2 and 1-->4)- beta- D-glucopyranosyl]-25 R-furost-5-ene-3 beta,22 alpha,26-triol ( 3), in addition to the previously reported steroidal saponins: dioscin ( 4) and progenin II ( 5). The structure elucidation of these metabolites was based primarily on 1D and 2D NMR analyses. Metabolites 2 - 5 showed significant cytotoxicity against cancer cell lines A375, L929, and HeLa with IC (50) values ranging from 1.18 microM to 17.88 microM.

Animals↗

Diosgenin, a plant-derived sapogenin, stimulates Ca2+-activated K+ current in human cortical HCN-1A neuronal cells.

The effects of diosgenin (3beta-hydroxy-5-spirostene), a plant-derived sapogenin, on ion currents in human cortical neurons (HCN-1A) were investigated. In the whole-cell configuration, diosgenin (0. -30 microM) increased the amplitude of K+ outward current (I(K)). Diosgenin-stimulated I(K) was sensitive to inhibition by paxilline (1 microM), but not by apamin (200 nM) or glibenclamide (10 muM). In the cell-attached configuration, diosgenin applied to the bath increased the activity of large-conductance Ca2+-activated K+ (BK(Ca)) channels without altering single-channel conductance. Diosgenin enhanced BK(Ca)-channel activity with an EC50 value of 25 microM. However, in inside-out patches, diosgenin applied to the intracellular surface had no effect on BK(Ca)-channel activity, while cilostazol or caffeic acid phenethyl ester increased it. As shown with the aid of intracellular Ca2+ measurements, diosgenin elevated intracellular Ca2+ in HCN-1A cells. Western blotting also revealed the presence of the alpha-subunit of BK (Ca) channels in these cells. The sustained stimulation of I(K) arises primarily from the diosgenin-induced Ca2+ influx across the cell membrane. The effect of diosgenin on these channels may affect the functional activity of cortical neurons. Abbreviations. I(K):K+ outward current I(K(Ca)):Ca2+-activated K+ current BK(Ca) channel:Large-conductance Ca2+-activated K+ channel CAPE:caffeic acid phenethyl ester [Ca2+] (i):intracellular Ca2+ concentration I/V relationship:current/voltage relationship K (ATP) channel:ATP-sensitive K+ channel K(Ca) channel:Ca2+-activated K+ channel.

Calcium Channel Blockers↗

Processing effects on susceptibility of starch to digestion in some dietary starch sources.

Maize flour, potato flour, cocoyam flour, plantain flour, yam flour, and rice flour were assayed for starch digestibility by an established enzymatic procedure. These were either autoclaved, microwaved, or parboiled and then freeze-dried. Freeze-dried samples were stored for 10 days either below freezing or at ambient temperature. Parameters assessed were readily digestible starch (RDS), slowly digestible starch (SDS), and total starch (TS). Data was analyzed by t-test (P < or = 0.05). RDS levels among raw flours ranged from 1.01 g/100g in rice flour to 8.16 g/100 g in cocoyam flour. Autoclaving and parboiling increased RDS levels in most flours, while microwaving significantly reduced RDS compared with raw flour. Ambient temperature storage reduced the RDS content. SDS levels ranged from 4.95 g/100 g in yam flour to 22.2 g/100 g in maize flour. SDS levels were increased by autoclaving and parboling, but significantly reduced by microwaving, compared with the raw flour. Storage at ambient temperature resulted in lower SDS. The TS content in raw flour ranged from 28.0 g/100 g in plantain flour to 68.4 g/100 g in rice flour. Autoclaving resulted in reduced TS levels insome flours. Moist heat processing and the post-process storage temperature therefore result in significant changes in starch susceptibility to enzymic digestion. This information will be useful in developing food processing and storage procedures that modify starch resistance to digestion in order to optimize its nutritional quality and to enhance the physiological benefits.

Dietary Carbohydrates↗

Phytoestrogens: a viable option?

Estrogen replacement therapy is one of the most commonly prescribed medicines in the United States by traditional medical professionals. Over the past decade, the market for complementary/ alternative therapies for hormone replacement has dramatically increased. Women are seeking more "natural" alternatives to treat menopausal symptoms. Well-designed randomized clinical trials are often lacking, as is the information on efficacy and safety. This article will review several popular herbal therapies for menopausal symptoms including phytoestrogens, black cohosh (Cimicifuga racemosa), dong quai (Angelica sinensis), chast tree (Vitex agnus-castus), and wild Mexican yam. Their use, mechanism of action, and adverse effects are outlined.

Angelica sinensis↗

[Complementary and alternative therapies for climacteric symptoms].

OBJECTIVE: Review on complementary and alternative therapies for climacteric symptoms. METHODS: Search for publications about complementary or alternative treatments for climacteric symptoms based on Cochrane Library and Medline (1966-2006) including the references from the identified clinical trials and reviews. RESULTS: Cimicifuga may influence climacteric symptoms, especially hot flushes. Results for phytoestrogens, hop and Salvia seem promising but are less convincing. St. John's wort is an option for the treatment of moderate depressive symptoms. Phytoestrogens seem to have some potential for the prevention of osteoporosis and cardiovascular diseases. Results for the influence of lifestyle on hot flushes are conflicting, but interventions have demonstrated their use for the prevention of osteoporosis and cardiovascular diseases. CONCLUSIONS: Lifestyle modifications, Cimicifuga and phytoestrogens may relieve climacteric symptoms. Phytoestrogens and Cimicifuga should not be given to breast cancer survivors.

Acupuncture↗

An estrogen replacement therapy containing nine synthetic plant-based conjugated estrogens promotes neuronal survival.

Epidemiological data from retrospective and case-control studies have indicated that estrogen replacement therapy can decrease the risk of developing Alzheimer's disease. In addition, estrogen replacement therapy has been found to promote neuronal survival both in vivo and in vitro. We have shown that conjugated equine estrogens (CEE), containing 238 different molecules composed of estrogens, progestins, and androgens, exerted neurotrophic and neuroprotective effects in cultured neurons. In the current study, we sought to determine whether a steroidal formulation of nine synthetic conjugated estrogens (SCE) chemically derived from soybean and yam extracts is as effective as the complex multisteroidal formulation of CEE. Analyses of the neuroprotective efficacy indicate that SCE exhibited significant neuroprotection against beta amyloid, hydrogen peroxide, and glutamate-induced toxicity in cultured hippocampal neurons. Indices of neuroprotection included an increase in neuronal survival, a decrease in neurotoxin-induced lactate dehydrogenase release, and a reduction in neurotoxin-induced apoptotic cell death. Furthermore, SCE was found to attenuate excitotoxic glutamate-induced [Ca2+]i rise. Quantitative analyses indicate that the neuroprotective efficacy of SCE was comparable to that of the multisteroidal CEE formulation. Data derived from these investigations predict that SCE could exert neuroprotective effects comparable to CEE in vivo and therefore could reduce the risk of Alzheimer's disease in postmenopausal women.

Amyloid beta-Peptides↗

[Experimental study on the hypoglycemic effect of tangniaole capsule].

OBJECTIVE: To study on the hypoglycemic effect of Tangniaole Capsule. METHOD: The effects of Tangniaole Capsule were proved through experiments on both normal and diabetic animals. RESULTS: Tangniaole Capsule was able to decrease the blood-sugar content in normal mice and rats, heighten the level of serum insulin and the content of liver glycogen in normal rats, decrease the blood-sugar content and increase the content of liver glycogen in hyperglycemina rats induced by adrenalin, inhibit the alloxan-induced hyperglycemia of mice and rats and improve the glucose tolerance of rats. CONCLUSION: Tangniaole Capsule have obvious hypoglycemic effect.

Alloxan↗

[The antitumor activity of Diosgenin in vivo and in vitro].

OBJECTIVE: To investigate the antitumor activity of Diosgenin in vivo and in vitro. METHOD: S-180, HepA, U14 and EAC transplant mice were given Diosgenin ig or i.p. everyday for 10 days, from the next day when they were inoculated in axilla. Tumor growth inhibit rates were calculated. Four kinds of cells, MCF, L929, A375-S2 and HeLa, were incubated respectively with Diosgenin in vitro. Tumor growth inhibit rates were also calculated. RESULT: In vivo, both ig and i.p., Diosgenin inhibited S-180, HepA, U 14 mice transplant tumor, the inhibit rates being 30%-50%, but it did not inhibit the EAC mice transplant tumor. In vitro, Diosgenin inhibited L929, HeLa, MCF cell growth, and IC50 were 1.2, 18.2, 19.8 micrograms.mL-1 respectively, but it did not significantly affect A375-S2 cells. CONCLUSION: Diosgenin has an obvious antitumor activity on S-180, HepA, U14 transplant mice in vivo and L929, HeLa, MCF cells in vitro.

Animals↗

[Determination of glycosides in traditional Chinese medicine liu-wei di-huang by RP-HPLC].

OBJECTIVE: To establish a RP-HPLC method for determination of glycosides in Traditional Chinese Medicine Liu-wei Di-huang. METHOD: The samples were analyzed on an ODS column at 30 degrees C, with mobile phase of methanol/water (33:67) at flow rate 1.0 mL.min and detection at wavelength of 236 nm. RESULT: Three major components reached base-line separation and were identified to be mononiside, loganin, paeoniflorin. Respectively for the three components, linear correlations were found between peak areas and concentrations in the ranges of 7.4-60, 7.7-62 mg.L-1 and 8.5-68 mg.L-1, and the recoveries were 98.8%, 98.3%, 99.6%. CONCLUSION: The established method is proved to be suitable for simultaneous quantification of three major glycosidic components in Liuwei Dihuang decoction and can be used for evaluation of the quality of Liuwei Dihuang preparations.

Benzoates↗