Sunday, September 23, 2012

High-linoleic Safflower Oil Diet (Safslim) - High Adiponectin and Low Belly Fat

Belly fat, the scourge of every middle aged American. Many have tried to defeat it and many have failed. I myself am currently fighting the good fight. Well another weapon has emerged in the battle and oddly enough it's a fat.

Safflower (Carthamus tinctorius) is a thistle like plant whose seeds are high in both oleic acid and linoleic acid. Linoleic acid has been linked to higher adiponectin levels. Adiponectin is a protein hormone that controls glucose regulation and fatty acid metabolism. When adiponectin levels are high body fat percentages are low in adults and visa versa.

I found two products of note containing the proper amounts of linoleic acids in them.

  1. Safslim found in local health stores selling for about $25 for 15 days worth.

  2. Spring Valley Safflower Oil found at Walmart selling for $15 for 15 days worth.

They both say 30 serving but that does not account for taking it twice per day as directed.

I am going to try the Spring Valley version first.

I did get a sample of the Safslim version and it is very pleasant tasting.



The below information can be found on the Re-Body website along with coupons for Safslim.

The Science of SAFActive78™ High-Linoleic Safflower Oil

Found in our SafSlim™ Belly Fat Supplements
Never heard of high-linoleic safflower oil? SafSlim™’s expeller-pressed, high-linoleic (78 percent) emulsified safflower oil (SAF) is a very effective way to target and reduce belly fat. In a 16-week study, Ohio State University researchers compared it with conjugated linoleic acid (CLA) by studying post-menopausal women who had high blood sugar and wanted to lose weight.
Highlights of this study:
  • These participants showed an average reduction of 6.3 percent belly fat and an average of 20.3 percent increase in adiponectin, an important belly fat hormone.
  • SAF outperformed CLA in measurements of trunk adipose (belly fat) and adiponectin levels. There was no significant change in adiponectin or in trunk adipose loss with CLA.
  • The study participants achieved results with no modifications to their exercise or diet regimens. However, SafSlim is intended to be used in addition to any reduced-calorie diet and exercise program.

Gout, B., Bourges, C., & Paineau-Dubreuil, S. (2010). Satiereal, a Crocus sativus L extract, reduces snacking and increases satiety in a randomized placebo-controlled study of mildly overweight, healthy women. Nutrition Research, 30, 305 – 313.
Leigh E Norris, Angela L Collene, Michelle L Asp, Jason C Hsu, Li-Fen Liu, Julia R Richardson, Dongmei Li, Doris Bell, Kwame Osei, Rebecca D Jackson, and Martha A Belury. Comparison of dietary conjugated linoleic acid with safflower oil on body composition in obese postmenopausal women with type 2 diabetes mellitus1–4. Am J Clin Nutr 2009;90:468–76.


Mahler's Aggressive Strength - MikeMahler.com




Saturday, September 8, 2012

Raspberry Ketone Fat Burner Explained.


Raspberry ketones are found in red raspberries and is the primary compound responsible for the aroma. The compound regulates a protein called adiponectin used by the body to regulate metabolism. Raspberry ketone helps your body burn fat faster by causing the fat within your cells to get broken up more effectively. The recommended dose is 100mg per day. To get the same benefit from the whole raspberries, you would have to consume 90 pounds of raspberries.


 
Here are a few products that you can consider.

References:
Koeduka T, Watanabe B, Suzuki S, Hiratake J, Mano J, Yazaki K. Characterization of raspberry ketone/zingerone synthase, catalyzing the alpha, beta-hydrogenation of phenylbutenones in raspberry fruits. Biochem Biophys Res Commun. 2011;412(1):104-8.

Tateiwa J I, Horiuchi H, Hashimoto K, Yamauchi T, Uemura S. Cation-exchanged montmorillonite-catalyzed facile Friedel-crafts alkylation of hydroxy and methoxy aromatics with 4-hydroxybutan-2-one to produce raspberry ketone and some pharmaceutically active compounds. J Org Chem 1994; 59: 5901-5904.

Kawada T, Hagihara K I, Iwai K. Effects of capsaicin on lipid metabolism in rats fed a high fat diet. J Nutr 1986; 116: 1272-1278.

Carpene C, Galitzky J, Fontana E, Atgie C, Lafontan M, Berlan M. Selective activation of β3-adrenoceptors by octamine: comparative studies in mammalian fat cells. Naunyn Schmiedebergs Arch Pharmacol 1999; 359: 310-321.

Morimoto C, Satoh Y, Hara M, Inoue S, Tsujita T, Okuda H. Anti-obese action of raspberry ketone. Life Sci. 2005;77(2):194-204.

Shin, K. O. and Moritani, T. Alterations of autonomic nervous activity and energy metabolism by capsaicin ingestion during aerobic exercise in healthy men. J.Nutr.Sci.Vitaminol.(Tokyo) 2007;53(2):124-132.

Inoue, N., Matsunaga, Y., Satoh, H., and Takahashi, M. Enhanced energy expenditure and fat oxidation in humans with high BMI scores by the ingestion of novel and non-pungent capsaicin analogues (capsinoids). Biosci.Biotechnol.Biochem. 2007;71(2):380-389.

Lejeune, M. P., Kovacs, E. M., and Westerterp-Plantenga, M. S. Effect of capsaicin on substrate oxidation and weight maintenance after modest body-weight loss in human subjects. Br.J.Nutr. 2003;90(3):651-659.

Martin B, Ji S, Maudsley S, Mattson MP. "Control" laboratory rodents are metabolically morbid: why it matters. Proc Natl Acad Sci USA. 2010;107(14):6127-33.

Thursday, September 6, 2012

My Weight is Up to 204lbs. I'm instituting a walk/run policy.

I'm going to start slow. Here's my plan. Cardio Monday through Friday. Lower body weight training on Saturday and upper body on Sunday.

 
I'm going to start Primaforce Yohimbe HCL as my preworkout for cardio and rub on some Ab-Solution.


I am also going to give intermittent fasting a shot.  For me that will mean black coffee until 1 p.m.. I will eat for an 8 hour window from 1 p.m. to 9 p.m..

My cardio will start as a walk/run program. Walking 7 minutes and running 3 minutes for three rounds with a cool down walk of at least 5 minutes. My Gymboss timer will keep track of the time.


Green Coffee Extract pre-meals will hopefully keep my insulin response in check.
 


 
This is going to be a tough task. The first Duncan's Donut in Kansas City just opened on my route to work.
 
Keep fighting the good fight! 


Tuesday, September 4, 2012

Muscletech Hydroxycut Hardcore Elite‏: The Perfect Fatburner?

Has Muscletech done it again? Is this the industries new best fatburner? Maybe....only time will tell.

I have not tried it yet but will. It has the combination of stuff that could make it the best. A synergistic combination of ingredients that should speed you on your way to rip city.

Let's break it down.

CAFFEINE

Frees up fat and boosts your metabolism to burn that freed fat.

FORSKOLIN

Activates the enzyme adenylate cyclase that allows fat cells to be broken down and used as fuel. Forskolin also increases testosterone production at the source.

GREEN-COFFEE EXTRACT

Contains chlorogenic acid which has been shown in several clinical studies to lead to significant fat loss. It works with caffeine to do this while also lowering the impact of post meal blood sugars. 

COCOA EXTRACT

Cocoa provides theobromine, an active metabolite of caffeine that provides fat-burning effects similar to caffeine.

YOHIMBE

Yohimbine and rauwolscine bind to fat cells removing limits to the amount of fat burned.

Source Citation (MLA 7th Edition)


Stoppani, Jim. "Muscletech hydroxycut hardcore elite: an up-close look at muscletech's clinically supported fat burner." Joe Weider's Muscle & Fitness May 2012: 76. Academic OneFile. Web. 4 Sep. 2012.
 


 


Sunday, September 2, 2012

Weight Trainers Cutting Stack: BPI Sports A-HD and Solid


I did this stack sometime before I started this blog and was surprised with the results. I started taking it and found that I was leaning out. I hadn't changed my diet and had friends keep telling me that my face was getting leaner. The weird thing was that my weight was not changing but my face and body was looking leaner.

Cool huh.

My favorite BPI Sports products are still Blox and Super Pro but as far as visual results this combo beats them both.

A-HD by itself did nothing for me but I've met guys that love it stand alone. I will probably try A50 in acouple of months.

BPI Sports calls it the Get Hard Stack and it seems to work. I have no idea how because I've searched and searched and can't find anything as far as studies goes.

This is all anecdotal or "Bro Science". Give it a try.


I am always afraid of long-term use of anything that hasn't been used or tested with human subjects. So be cautious.

BPI recommends that you take 1 Solid in the morning and 1 A-HD in the afternoon. I think most days that I took both in the morning.

Here's what's in it.

A-HD (the give a bunch of chemical names but it's really common stuff)

Safflower Seed Extract or Carthamus tinctorius CHEMICAL NAME: (3s,4s)-4-[(3,4-dimethoxyphenyl)methyl]-3-hydroxy-3-[[3-methoxy-4-[(2s,3r,4s,5r,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-phenyl]methyl]oxolan-2-one

Flax Seed Lignan CHEMICAL NAME: (2r,3r)-2,3-bis[(4-hydroxy-3-methoxyphenyl)methyl]butane-1,4-diol;(2r,3r,4s,5s,6r)-6-(hydroxymethyl)oxane-2,3,4,5-tetrol

Pterostilbene - Similiar to Resveratrol CHEMICAL NAME: 4-[(e)-2-(3,5-dimethoxyphenyl)ethenyl]phenol

Gingerol CHEMICAL NAME: s)-5-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-3-decanone

Caffeate (beehive propolis) CHEMICAL NAME: phenethyl(e)-3-(3,4-dihydroxyphenyl)prop-2-enoate

For a really good treatment of this goto What’s In BPI Arimedex? or BPI Sports A-HD (Arimedex) Ingredients: Snake Oil or TheReal Deal? .

Why not just call it these? Instead of giving names that make you think it's a prohormone combination. Whatever, it did give me results when combined with SOLID.

The below study references was found on www.bodybuilding.com product page.

1] Biosci Biotechnol Biochem. 2006 Nov;70(11):2783-5.


  • [2] J Toxicol Environ Health A. 1999 Apr 23;56(8):555-70.



  • [3] J Vet Med Sci. 2002 Sep;64(9):761-5.



  • [4] J Nutr. 2006 Jun;136(6):1545-51.



  • [5] Exp Biol Med. 2007 Sep;232(8):1071-80.



  • [6] Curr Clin Pharmacol. 2006 Jan;1(1):81-101.



  • [7] Mol Nutr Food Res. 2010 Mar;54(3):335-44.



  • [8] Ir J Reprod Med. 2009 Winter;7(1):7-12.



  • [9] Ann NY Acad Sci. 2004 Dec;1030:501-7.



  • [10] J Steroid Biochem Mol Biol. 2009 Jan;113(1-2):65-74.

  • SOLID™
    Proprietary Blend 100mg
    Borassus Aethiopum (Germinating Shoot) *
    Tulbaghia Violacea Harv. (Leaf And Rhizome) *
    Cynodon Dactylon (Aerial) *

    Found the below on a forum at www.supplementreviews.com .

    SOLID™'s dual Anabolic and Androgenic activity results from the fact that it's formulated with a novel class of naturally-occurring compounds...* Compounds which appear to effectively bind to androgen receptors, and modulate protein synthesis and help decrease protein breakdown.* 1 The anabolic actions of androgens are demonstrated through changes in body, plasma amino acid level, and plasma urea level, among other indicators. 4-7

    The physiological (regulation, metabolism, and mechanisms) importance of this dual anabolic and androgenic activity simply cannot be understated.* It is T-H-E key. The key to SOLID™, the key to getting the hardening, definition, strength, and vascular effects you want... and, need, to be contest ready! †*


    † When combined with a proper exercise and nutrition regimen.

    The below study references was found on www.bodybuilding.com product page.

    REFERENCES:
    [1] J Sci Res. 2010; 2(2): 362-8.
    [2] J Young Pharm. 2011 Jan-Mar; (3)1: 26-35.
    [3] J Ethnopharmacol. 2010; 132: 359-61.
    [4] J Appl Physiol. 1989 Jan;66(1):498-503.
    [5] J Appl Physiol. 1991 Mar;70(3):1038-43.
    [6] Metabolism. 1985 Jun;34(6):571-3.
    [7] Endocr Rev. 1987 Feb;8(1):1-28.


    Mahler's Aggressive Strength - MikeMahler.com






    Green Coffee Bean Extract - Starting Tomorrow - Featured on the Dr. Oz Show


    There are lots of green coffee bean products out there. Life Extension, Top Secret, Futurebiotics, Resverage, Biogenetic Laboratories to name a few. I recently met a guy who lost 20 pounds over the past month taking one capsule (400mg) before each meal. He also said he has more energy without the drained feeling in the afternoon.

    I like the theory behind green coffee bean extract because it is based on sugar control. Slowing the insulin response to high blood sugar levels seem to be key. From what I've read, excess sugars are either shuttled into muscle or fat by insulin and if you haven't used up all the sugars in muscle by working out, it has no where to go but into fat. If you aren't always low or slow carb you will have considerable fat accumulation.

    I bought some today and will start it tomorrow. It appears that everyone else in town is buying it too because I there was only one bottle left of each of the brands above when I went to get it. I bought the Life Extension Coffeegenic brand. Why because they always back up their products with study references. I will update you when the bottle is empty.

    Dr. Oz recommends 800mg twice per day. I'm going to do 400mg with each of my meals because I'm not made of money.



    The below study references are from Life Extension Magazine February 2012 edition.

    Green Coffee Bean Extract

    The effect of chlorogenic acid enriched coffee on glucose absorption in healthy volunteers and its effect on body mass when used long-term in overweight and obese people.

    The results from a clinical study performed in 12 healthy volunteers with different coffee products containing glucose show that instant coffee enriched with chlorogenic acid induced a reduction in the absorption of glucose of 6.9% compared with the control. No such effects were seen with normal or decaffeinated instant coffee. In a second, comparative, randomized, double-blind, 12-week study we investigated the effect on the body mass of 30 overweight people, compared with normal instant coffee. The average losses in mass in the chlorogenic acid enriched and normal instant coffee groups were 5.4 and 1.7 kg, respectively. We conclude that chlorogenic acid enriched instant coffee appears to have a significant effect on the absorption and utilization of glucose from the diet. This effect, if the coffee is used for an extended time, may result in reduced body mass and body fat when compared with the use of normal instant coffee.
    J Int Med Res. 2007 Nov-Dec;35(6):900-8

    Acute effects of decaffeinated coffee and the major coffee components chlorogenic acid and trigonelline on glucose tolerance.

    OBJECTIVE: Coffee consumption has been associated with lower risk of type 2 diabetes. We evaluated the acute effects of decaffeinated coffee and the major coffee components chlorogenic acid and trigonelline on glucose tolerance. RESEARCH DESIGN AND METHODS: We conducted a randomized crossover trial of the effects of 12 g decaffeinated coffee, 1 g chlorogenic acid, 500 mg trigonelline, and placebo (1 g mannitol) on glucose and insulin concentrations during a 2-h oral glucose tolerance test (OGTT) in 15 overweight men. RESULTS: Chlorogenic acid and trigonelline ingestion significantly reduced glucose (-0.7 mmol/l, P = 0.007, and -0.5 mmol/l, P = 0.024, respectively) and insulin (-73 pmol/l, P = 0.038, and -117 pmol/l, P = 0.007) concentrations 15 min following an OGTT compared with placebo. None of the treatments affected insulin or glucose area under the curve values during the OGTT compared with placebo. CONCLUSIONS: Chlorogenic acid and trigonelline reduced early glucose and insulin responses during an OGTT.
    Diabetes Care. 2009 Jun;32(6):1023-5

    Inhibitory effect of green coffee bean extract on fat accumulation and body weight gain in mice.

    BACKGROUND: An epidemiological study conducted in Italy indicated that coffee has the greatest antioxidant capacity among the commonly consumed beverages. Green coffee bean is rich in chlorogenic acid and its related compounds. The effect of green coffee bean extract (GCBE) on fat accumulation and body weight in mice was assessed with the objective of investigating the effect of GCBE on mild obesity. METHODS: Male ddy mice were fed a standard diet containing GCBE and its principal constituents, namely, caffeine and chlorogenic acid, for 14 days. Further, hepatic triglyceride (TG) level was also investigated after consecutive administration (13 days) of GCBE and its constituents. To examine the effect of GCBE and its constituents on fat absorption, serum TG changes were evaluated in olive oil-loaded mice. In addition, to investigate the effect on hepatic TG metabolism, carnitine palmitoyltransferase (CPT) activity in mice was evaluated after consecutive ingestion (6 days) of GCBE and its constituents (caffeine, chlorogenic acid, neochlorogenic acid and feruloylquinic acid mixture). RESULTS: It was found that 0.5% and 1% GCBE reduced visceral fat content and body weight. Caffeine and chlorogenic acid showed a tendency to reduce visceral fat and body weight. Oral administration of GCBE (100 and 200 mg/kg. day) for 13 days showed a tendency to reduce hepatic TG in mice. In the same model, chlorogenic acid (60 mg/kg. day) reduced hepatic TG level. In mice loaded with olive oil (5 mL/kg), GCBE (200 and 400 mg/kg) and caffeine (20 and 40 mg/kg) reduced serum TG level. GCBE (1%), neochlorogenic acid (0.028% and 0.055%) and feruloylquinic acid mixture (0.081%) significantly enhanced hepatic CPT activity in mice. However, neither caffeine nor chlorogenic acid alone was found to enhance CPT activity. CONCLUSION: These results suggest that GCBE is possibly effective against weight gain and fat accumulation by inhibition of fat absorption and activation of fat metabolism in the liver. Caffeine was found to be a suppressor of fat absorption, while chlorogenic acid was found to be partially involved in the suppressive effect of GCBE that resulted in the reduction of hepatic TG level. Phenolic compounds such as neochlorogenic acid and feruloylquinic acid mixture, except chlorogenic acid, can enhance hepatic CPT activity.
    BMC Complement Altern Med. 2006 Mar 17;6:9

    Coffee polyphenols suppress diet-induced body fat accumulation by downregulating SREBP-1c and related molecules in C57BL/6J mice.

    The prevalence of obesity is increasing globally, and obesity is a major risk factor for type 2 diabetes and cardiovascular disease. We investigated the effects of coffee polyphenols (CPP), which are abundant in coffee and consumed worldwide, on diet-induced body fat accumulation. C57BL/6J mice were fed either a control diet, a high-fat diet, or a high-fat diet supplemented with 0.5 to 1.0% CPP for 2-15 wk. Supplementation with CPP significantly reduced body weight gain, abdominal and liver fat accumulation, and infiltration of macrophages into adipose tissues. Energy expenditure evaluated by indirect calorimetry was significantly increased in CPP-fed mice. The mRNA levels of sterol regulatory element-binding protein (SREBP)-1c, acetyl-CoA carboxylase-1 and -2, stearoyl-CoA desaturase-1, and pyruvate dehydrogenase kinase-4 in the liver were significantly lower in CPP-fed mice than in high-fat control mice. Similarly, CPP suppressed the expression of these molecules in Hepa 1-6 cells, concomitant with an increase in microRNA-122. Structure-activity relationship studies of nine quinic acid derivatives isolated from CPP in Hepa 1-6 cells suggested that mono- or di-caffeoyl quinic acids (CQA) are active substances in the beneficial effects of CPP. Furthermore, CPP and 5-CQA decreased the nuclear active form of SREBP-1, acetyl-CoA carboxylase activity, and cellular malonyl-CoA levels. These findings indicate that CPP enhances energy metabolism and reduces lipogenesis by downregulating SREBP-1c and related molecules, which leads to the suppression of body fat accumulation.
    Am J Physiol Endocrinol Metab. 2011 Jan;300(1):E122-33

    National, regional, and global trends in fasting plasma glucose and diabetes prevalence since 1980: systematic analysis of health examination surveys and epidemiological studies with 370 country-years and 2•7 million participants.

    BACKGROUND: Data for trends in glycaemia and diabetes prevalence are needed to understand the effects of diet and lifestyle within populations, assess the performance of interventions, and plan health services. No consistent and comparable global analysis of trends has been done. We estimated trends and their uncertainties in mean fasting plasma glucose (FPG) and diabetes prevalence for adults aged 25 years and older in 199 countries and territories. METHODS: We obtained data from health examination surveys and epidemiological studies (370 country-years and 2•7 million participants). We converted systematically between different glycaemic metrics. For each sex, we used a Bayesian hierarchical model to estimate mean FPG and its uncertainty by age, country, and year, accounting for whether a study was nationally, subnationally, or community representative. FINDINGS: In 2008, global age-standardised mean FPG was 5•50 mmol/L (95% uncertainty interval 5•37-5•63) for men and 5•42 mmol/L (5•29-5•54) for women, having risen by 0•07 mmol/L and 0•09 mmol/L per decade, respectively. Age-standardised adult diabetes prevalence was 9•8% (8•6-11•2) in men and 9•2% (8•0-10•5) in women in 2008, up from 8•3% (6•5-10•4) and 7•5% (5•8-9•6) in 1980. The number of people with diabetes increased from 153 (127-182) million in 1980, to 347 (314-382) million in 2008. We recorded almost no change in mean FPG in east and southeast Asia and central and eastern Europe. Oceania had the largest rise, and the highest mean FPG (6•09 mmol/L, 5•73-6•49 for men; 6•08 mmol/L, 5•72-6•46 for women) and diabetes prevalence (15•5%, 11•6-20•1 for men; and 15•9%, 12•1-20•5 for women) in 2008. Mean FPG and diabetes prevalence in 2008 were also high in south Asia, Latin America and the Caribbean, and central Asia, north Africa, and the Middle East. Mean FPG in 2008 was lowest in sub-Saharan Africa, east and southeast Asia, and high-income Asia-Pacific. In high-income subregions, western Europe had the smallest rise, 0•07 mmol/L per decade for men and 0•03 mmol/L per decade for women; North America had the largest rise, 0•18 mmol/L per decade for men and 0•14 mmol/L per decade for women. INTERPRETATION: Glycaemia and diabetes are rising globally, driven both by population growth and ageing and by increasing age-specific prevalences. Effective preventive interventions are needed, and health systems should prepare to detect and manage diabetes and its sequelae.
    Lancet. 2011 Jul 2;378(9785):31-40

    A large proportion of prediabetes and diabetes goes undiagnosed when only fasting plasma glucose and/or HbA1c are measured in overweight or obese patients.

    AIMS: The purposes of the study were to determine the prevalence of unrecognized dysglycaemia in overweight (body mass index [BMI] 25-29.9 kg/m(2)) and obese (BMI ≥30 kg/m(2)) patients, to assess the extent to which measures of fasting plasma glucose (FPG) and/or HbA(1c), compared with oral glucose tolerance tests (OGTTs), misdiagnose dysglycaemia, and to determine the factors associated with an isolated abnormal post-OGTT glucose value. METHODS: OGTT was performed and HbA(1c) was measured in 1283 inpatients with BMI scores ≥ 25 kg/m(2) and no history of dysglycaemia. RESULTS: Prediabetes was found in 257 (20.0%) subjects (197 with impaired glucose tolerance, 29 with impaired fasting glucose, 31 with both) and diabetes in 77 (6.0%), including 22 with FPG ≥ 7 mmol/L (WHO definition). The sensitivity of FPG >6 mmol/L, FPG >5.5 mmol/L, HbA(1c) ≥ 6% and the recommendations of the French National Agency of Accreditation and Evaluation in Health Care (ANAES) to identify patients with abnormal OGTTs was 29.9, 41.3, 36.8 and 15.6%, respectively. The factors that were independently associated with diabetes in obese women with FPG <7 mmol/L were age (per 10 years: OR 1.54 [1.00-2.11]; P=0.049) and FPG (OR 6.1 [1.4-30.0]; P=0.014), whereas age (OR 1.26 [1.09-1.44]; P<0.01) and waist circumference (per 10 cm: OR 1.17 [1.01-1.33]; P<0.05) were independently associated with dysglycaemia in obese women with FPG <6.1 mmol/L. CONCLUSION: In overweight and obese patients: dysglycaemia is commonly seen; FPG alone, compared with OGTT, failed to diagnose 70% of dysglycaemia cases; FPG >5.5 mmol/L and HbA(1c) ≥ 6.0% are not necessarily substitutes for OGTT; and older age and larger waist circumference should be used to select those obese women with normal FPG who might further benefit from OGTTs to diagnose dysglycaemia.
    Diabetes Metab. 2010 Sep;36(4):312-8

    Chlorogenic acid reduces the plasma glucose peak in the oral glucose tolerance test: effects on hepatic glucose release and glycaemia.

    The effects of chlorogenic acid (CA) on hepatic glucose output, blood glucose levels and on glucose tolerance were analysed. Hepatic uptake of CA and its effects on hepatic catabolism of L-alanine and glucose-6-phosphatase (G-6-Pase) activity were also evaluated. CA (1 mM) inhibited about 40% of G-6-Pase activity (p < 0.05) in the microsomal fraction of hepatocytes, but no effect was observed on production of glucose from gluconeogenesis or on L-alanine catabolism, at various concentrations of CA (0.33, 0.5 and 1 mM), in liver perfusion experiments. Since there were indications of a lack of uptake of CA by the liver, it is possible that this compound did not reach sufficiently high intracellular levels to inhibit the target enzyme. Accordingly, intravenous administration of CA also failed to provoke a reduction in blood glucose levels. However, CA did promote a significant reduction (p < 0.05) in the plasma glucose peak at 10 and 15 min during the oral glucose tolerance test, probably by attenuating intestinal glucose absorption, suggesting a possible role for it as a glycaemic index lowering agent and highlighting it as a compound of interest for reducing the risk of developing type 2 diabetes.
    Cell Biochem Funct. 2008 Apr;26(3):320-8

    Characterization of inhibitors of postprandial hyperglycemia from the leaves of Nerium indicum.

    Nerium indicum is an India-Pakistan-originated shrub belonging to the oleander family. The ingestion of leaves of N. indicum before a meal is known to effect the lowering of postprandial glucose levels in type II diabetic patients and this plant is now used as a folk remedy for type II diabetes in some regions of Pakistan. In the present study, the hot-water extract of N. indicum leaves was found to reduce the postprandial rise in the blood glucose when maltose or sucrose was loaded in rats. It was also found that the extract strongly inhibited alpha-glucosidase, suggesting that the suppression of the postprandial rise in the blood glucose is due to the occurrence of some inhibitors of alpha-glucosidase in the leaves. We, therefore, tried to isolate the active principles from the leaf extract, using alpha-glucosidase-inhibitory activity as the index. Employing Sephadex G-15, silica gel and reversed-phase HPLC, we isolated two active compounds. The UV, mass and NMR spectrometric analyses established that the chemical structures of these compounds are 3-O-caffeoylquinic acid (chlorogenic acid) and its structural isomer, 5-O-caffeoylquinic acid. Both compounds were shown to inhibit alpha-glucosidases in a non-competitive manner. The authentic chlorogenic acid was found to suppress the postprandial rise in the blood glucose in rats and also inhibited the absorption of the glucose moiety from maltose and glucose in the everted gut sac system prepared from rat intestine. These results demonstrate that chlorogenic acid is one of the major anti-hyperglycemic principles present in the leaves of N. indicum. Furthermore, among polyphenol compounds tested, quercetin and catechins were shown to have strong inhibitory activity against alpha-glucosidase.
    J Nutr Sci Vitaminol (Tokyo).2007 Apr;53(2):166-73