Glucose disposal agents / Insulino mimetics / Nutrient partitioners

[conv999]

quindi che prodotti consigli e in che modalità di assunzione ???
grazie!!

..probabilmente non hai letto tutte le pagine del post.

badlinus87 ha elencato una serie di prodotti e i suoi feedback (grazie)
IO ho deciso di prenderne due di questi.

..e il saggio menphisdaemon ha chiesto a utenti/tester che siano affidabili se tali prodotti potessero o meno garantire un surplus di carbo nell'ordine dei 100g di cho.

QUindi io ho detto di essere ( credo a ragione) un tester affidabile e che una volta provati potrei dare un feedback attendibile.

Quindi in sostanza ( ai fini della discussione " Glucose disposal agents / Insulino mimetics / Nutrient partitioners " ) ora non posso dare alcun giudizio ne di modalità d'assunzione ne tantomeno di dosi.
-Bepi-

[badlinus87]

L'altro ieri mi è arrivato recompadrol.
Per adesso ne sto usando 1 cap 3 volte al dì (questo prodotto va dosato in base alla quantità di cho ovvero 1 cap per pasti fino ad una 60 di cho e 2 per oltre) e come prima impressione, ho notato soltanto la classica eliminazione del senso di gonfiore dopo un pasto, nient'altro.
Sò che è molto presto per trarre conclusioni, ma alla fine per adesso la corona per me la detiene SLIN SANE, che già alla prima assunzione mi diede un pump ed una vascolarizzazione non indifferenti, oltre al suddetto effetto.
Più avanti vi farò sapere

[PrinceRiky]

la cannella già è un blandissimo mimetico in estratto superconcentrato. l'aceto di mele non saprei.

[conv999]

porca miseria.... appena arrivato il Slin Sane (anche il Recompadrol) e desideroso di provarlo e mi arriva una mail adesso che hanno fatto il Slin-Sane V2 (new version).
Ora... spesso le nuove versioni non sono meglio delle precedenti (anzi spesso è vero il contrario..) .. ma cavoli vedo che hanno completamente cambiato gli ingredienti e aggiunto anche K-R-Ala.....

[mastino83]

L'altro ieri mi è arrivato recompadrol.
Per adesso ne sto usando 1 cap 3 volte al dì (questo prodotto va dosato in base alla quantità di cho ovvero 1 cap per pasti fino ad una 60 di cho e 2 per oltre) e come prima impressione, ho notato soltanto la classica eliminazione del senso di gonfiore dopo un pasto, nient'altro.
Sò che è molto presto per trarre conclusioni, ma alla fine per adesso la corona per me la detiene SLIN SANE, che già alla prima assunzione mi diede un pump ed una vascolarizzazione non indifferenti, oltre al suddetto effetto.
Più avanti vi farò sapere

secondo te si potrebbero associare: slin sane + hemavol + cho come pre wo??
scusa l'ignoranza , ma slin sane è un partitore di nutrienti ???
grazie mille

[mr oat]

Io usero' anabeta...slin sane pero sembra ottimo... Poi la v2 con k-r-ala e' veramente interessante....

[badlinus87]

secondo te si potrebbero associare: slin sane + hemavol + cho come pre wo??
scusa l'ignoranza , ma slin sane è un partitore di nutrienti ???
grazie mille

Si slinsane è un partitore di nutrienti, ma cmq da un pump non indifferente.(e superiore a molti NO products, ma nn so se è il caso dell'hemavol).
Io non li abbinerei, perrchè potresti usarli separatamente e ottenere benefici sul lungo termine, ma cmq si può fare, dovresti prendere prima l'hemavol a stomako vuoto, aspettare una 40 di minuti poi prendere slin sane e dopo 15-20 minuti i cho.

Io usero' anabeta...slin sane pero sembra ottimo... Poi la v2 con k-r-ala e' veramente interessante....

Mi ha sempre stuzzicato fin dalla sua presentazione, il problema è che in rete, a parte i log sponsorizzati, non si trovano molte recensioni positive, e per quello che costa non voglio rischiare

[dave07]

ragazzi per capirci qualcosa ho ricercato un po i vari ingredienti di need2slin, recompadrol, anabolic pump, p-slin, slin sane v2 e slin sane, anche per avere una idea sul quale provare eventualmente. vi riporto quello che ho trovato.


need2slin: l'ingrediente principale sembra essere l'acido gimnemico che ha un importante ruolo sia nel bloccare reversibilmente il recettore per il glucosio che alterare la percezione del sapore dolce. la banaba contenuta nel composto ha proprietà ipoglicemizzanti mentre ALC, l-norvalina, colues forskoli, NaRala, sinefrina hcl sappiamo tutti che ruoli hanno.


recompadrol: è composto da garcinia cambogia (blocca la produzione di acetilCoA (substrato energetico utilizzato per la sintesi di cortisolo) e riduce la sintesi degli acidi grassi), berberine hcl aumenta la sensibilità all'insulina e aumenta il processo di glicolisi (trasformazione glucosio -> piruvato), salacia reticulata (di cui non ho trovato info apprezzabili), vanadyl Sulfate sembra essere una sostanza insulino-mimetica, ma da quello che ho capito non vi sono studi certi che ne attestino l'effettiva attività, anche l'aminoguanidina migliora la sensibilità all'insulina e tende a ridurre il tasso di gluciosio ematico e per finire ci sono acido gimnemico e banaba.


anabolic pump: phellodendron (dovrebbe essere berberine hcl da quel che ho capito) e laghestremia speciosa (banaba) e chetoni del cissus


p-slin: banaba, acido gimnemico


slin sane v2: ingrediente principale jiaogulan. è un erba di origine asiatica cono sciuta come un adattogeno. fra le tante funzioni che ho trovato sembra mantenga in range normali la pressione, migliori la cardiovascolarizzazione, abbia una riduzione del colesterolo e ipoglicemizzante perchè riduce il glucosio nel sangue. gli altri ingredienti sono NaRala, norvalina e banaba


slin sane: norvalina, acido gimnemico e banaba

glycobol: NaRala, berberine, trigonella (dovrebbe abbassare anch'essa il tasso di zuccheri nel sangue), estratto di cannella e 'Bis-Malto-Oxovanadium' (di cui non ho reperito abbastanza info)

[Tony07]

ci sarebbe anche il Glycobol ben valutato oltreoceano

[dave07]

ci sarebbe anche il Glycobol ben valutato oltreoceano

aggiornato ,

comunque vedendo le varie composizioni sembra che le componenti influenti come insulino-mimetiche siano : acido gimnemico, banaba, berberine contornate poi da NaRala e l-norvalina.
bisognerebbe però sapere i dosaggi dei vari composti (alcuni blend quindi impossibile) e studiare quale di queste sostanze esplichi il lavoro maggiore o comunque sia la componente più 'forte' e fondamentale.

[brosgym]

Magari partire da come agiscono, almeno in teoria......

[badlinus87]

glycobol però in molte recensioni sembra dare problemi di natura glicemica e intestinale

[Tony07]

glycobol però in molte recensioni sembra dare problemi di natura glicemica e intestinale

hai ragione, molti accusano problemi di defecazione immediatamente dopo . Ma secondo me perchè non sanno dosare adeguatamente il prodotto.. poi non so non lo ho provato..

[blindevil7]

Magari partire da come agiscono, almeno in teoria......

iniziamo con la gimnema

Mechanism of Action of Gymnemic Acids

Gymnemic acid formulations have also been found useful against obesity, according to recent reports [10]. This is attributed to the ability of gymnemic acids to delay the glucose absorption in the blood. The atomic arrangement of gymnemic acid molecules is similar to that of glucose molecules. These molecules fill the receptor locations on the taste buds thereby preventing its activation by sugar molecules present in the food, thereby curbing the sugar craving. Similarly, Gymnemic acid molecules fill the receptor location in the absorptive external layers of the intestine thereby preventing the sugar molecules absorption by the intestine, which results in low blood sugar level [11].
G. sylvestre leaves have been found to cause hypoglycemia in laboratory animals and have found a use in herbal medicine to help treat adult onset diabetes mellitus (NIDDM). When Gymnema leaf extract is administered to a diabetic patient, there is stimulation of the pancreas by virtue of which there is an increase in insulin release [12]. These compounds have also been found to increase fecal excretion of cholesterol [13], but further studies to prove clinical significance in treating hypercholesterolemia (high serum cholesterol) are required. Other uses for Gymnema leaf extract are its ability to act as a laxative, diuretic, and cough suppressant. These other actions would be considered adverse reactions whenGymnema is used for its glucose lowering effect in diabetes.
Gymnema leaf extract, notably the peptide ‘Gurmarin’, has been found to interfere with the ability of the taste buds on the tongue to taste sweet and bitter. Gymnemic acid has a similar effect. It is believed that by inhibiting the sweet taste sensation, people taking it will limit their intake of sweet foods, and this activity may be partially responsible for its hypoglycemic effect [14].
There are some possible mechanisms by which the leaves and especially Gymnemic acids from G. sylvestre exert its hypoglycemic effects are: 1) it increases secretion of insulin, 2) it promotes regeneration of islet cells, 3) it increases utilization of glucose: it is shown to increase the activities of enzymes responsible for utilization of glucose by insulin-dependant pathways, an increase in phosphorylase activity, decrease in gluconeogenic enzymes and sorbitol dehydrogenase, and 4) it causes inhibition of glucose absorption from intestine.
The gymnemic acid components are believed to block the absorption of glucose in the small intestine, the exact action being unknown. It could be involve one or more mechanisms [14].
One of the mechanisms responsible for adult onset diabetes mellitus is a form of insulin resistance, which is attributed to the inability of insulin to enter cells via the insulin receptor. Gymnema may overcome this resistance, but require further studies to confirm its validity and also whether the effect is clinically relevant. Should this effect be proven, Gymnema may prove useful in both adult onset (NIDDM) and juvenile onset diabetes mellitus (IDDM) to help insulin enter cells. In the case of IDDM, the insulin is injected by syringe and is not secreted from the pancreas [15].
The leaves are also noted for lowering serum cholesterol and triglycerides. The primary chemical constituents of Gymnema include gymnemic acid, tartaric acid, gurmarin, calcium oxalate, glucose, stigmasterol, betaine, and choline. While the water-soluble acidic fractions reportedly provide the hypoglycemic action, it is not yet clear what specific constituent in the leaves is responsible for the same. Some researchers have suggested gymnemic acid as one possible candidate, although further research is needed [16]. Both gurmarin (another constituent of the leaves) and gymnemic acid have been shown to block sweet taste in humans. The major constituents of the plant material 3B glucuronides of different acetylated gymnemagenins, gymnemic acid a complex mixture of at least 9 closely related acidic glucosides [17–19].
The following figure could provide a diagrammatic representation for explaining the action of gymnemic acids on the intestinal receptors. The basic function of the acids is to bind to the receptor on the intestine, and stop the glucose molecule from binding to the receptor. Thus, gymnemic acids prevent the absorption of excess glucose.

---------- Post added at 17:59:01 ---------- Previous post was at 17:57:18 ----------



---------- Post added at 18:08:30 ---------- Previous post was at 17:59:01 ----------
References

1. The Wealth of India. Raw materials, vol. IV. Council of Scientific and Industrial Research; New Delhi: 1956. A Dictionary of Indian Raw materials and Industrial products; pp. 276–277.
2. Komalavalli N., Rao M.V. In vitro micropropagation of Gymnema sylvestre: multipurpose medicinal plant. Plant Cell, Tissue and Organ Culture. 2000;61:97–105.
3. Dateo G.P., Long L. Gymnemic acid, the antisaccharine principle of Gymnema sylvestre. Studies on isolation and heterogenesity of gymnemic acid A₁. J. Agric. Food Chem. 1973;21:899–903. [PubMed]
4. Liu H.M., Kiuchi F., Tsuda Y. Isolation and structure elucidation of Gymnemic acids, antisweet principles of Gymnema sylvestre. Chem. Pharm. Bull. 1992;40:1366–1375. [PubMed]
5. Sinsheimer J.E., Manni P.E. Constituents from Gymnema sylvestre leaves. J. Pharm. Sci.1965;54:1541–1544. [PubMed]
6. Sinsheimer J.E., Subbarao G. Constituents from Gymnema sylvestre leaves VIII: Isolation, chemistry and derivatives of gymnemagenin and gymnestrogenin. J. Pharm. Sci. 1971;60:190–193.[PubMed]
7. Sinsheimer J.E., Subba R.G., Mc Ilhenny H.M. Constituents from Gymnema sylvestre Leaves V: Isolation and preliminary characterization of Gymnemic acids. J. Pharm. Sci. 1970;59:622–628.[PubMed]
8. Yoshikawa K., Amimoto K., Arihara S., Matsuura K. Structure studies of new antisweet constituents from Gymnema sylvestre. Tetr. Lett. 1989;30:1103–1106.
9. Yoshikawa K., Nakagawa M., Yamamoto R., Arihara S., Matsuura K. Antisweet natural products V structures of gymnemic acids VIII-XII from Gymnema sylvestre R. Br. Chem. Pharm. Bull.1992;40:1779–1782.
10. Yoshikawa K., Kondo Y., Arihara S., Matsuura K. Antisweet natural products IX structures of gymnemic acids XV-XVIII from Gymnema sylvestre R. Br. Chem. Pharm. Bull. 1993;41:1730–1732.
11. Sahu N., Mahato S.B., Sarkar S.K., Poddar G. Triterpenoid Saponins from Gymnema sylvestre.Phytochem. 1996;41:1181–1185.
12. Kanetkar P.V., Laddha K.S., Kamat M.Y. Poster presented at the 16^th ICFOST meet organized by CFTRI and DFRL. Mysore, India: 2004. Gymnemic acids: A molecular perspective of its action on carbohydrate metabolism.
13. Persaud S.J., Al-Majed H., Raman A., Jones P.M. Gymnema sylvestre stimulates insulin release in vitro by increased membrane permeability. J. Endocrinol. 1999;163:207–212. [PubMed]
14. Nakamura Y., Tsumura Y., Tonogai Y., Shibata T. Fecal steroid excretion is increased in rats by oral administration of gymnemic acids contained in Gymnema sylvestre leaves. J. Nutr. 1999; 129:1214–1222. [PubMed]
15. Agarwal S.K., Singh S.S., Verma S., Lakshmi V., Sharma A. Chemistry and medicinal uses ofGymnema sylvestre (gur-mar) Leaves: A Review. Indian Drugs. 2000;37:354–360.
16. Khare A.K., Tondon R.N., Tewari J.P. Hypoglycemic activity of an indigenous drug Gymnema sylvestre in normal and diabetic persons. Ind. J. Physiol. Pharmacol. 1983;27:257–261.
17. Maeda M., Iwashita T., Kurihara Y. Studies on taste modifiers II: Purification and structure determination of gymnemic acids, antisweet active principle from Gymnema sylvestre leaves. Tetr. Lett.1989;30:1547–1550.
18. Manni P.E., Sinsheimer J.E. Constituents from Gymnema sylvestre leaves. J. Pharm. Sci.1965;54:1541–1544. [PubMed]
19. Sinsheimer J.E., Subbarao G. Constituents from Gymnema sylvestre leaves VIII: Isolation, chemistry and derivatives of gymnemagenin and gymnestrogenin. J. Pharm. Sci. 1971;60:190–193.[PubMed]
20. Dahanukar S.A., Kulkarni R.A., Rege N.N. Pharmacology of medicinal plants and natural products.Indian J. Pharmacol. 2000;32:S81–S118.
21. Ramachandran A., Snehalatha C., Satvavani K., Sivasankari S., Vijav V. Type 2 diabetes in Asian-Indian urban children. Diabetes Care. 2003;26:1022–1025. [PubMed]
22. Jachak S.M. Herbal drugs as antidiabetic: an overview. CRIPS. 2002;3:9–13.
23. Flier J.S. Prevention of obesity reduces the risk of a wide range of health problems. The missing link with obesity? Nature. 2001;409:292–293. [PubMed]
24. Claire S. The hormone resistin links obesity to diabetes. Nature. 2001:307.


Berberina

Berberine’s Probable and Possible Mechanisms of ActionThe studies encompassed by the review that is the central topic of the article “Berberine is Superior to Metformin” (of which this sidebar is a part) have found that berberine is beneficial for glucose metabolism and insulin activity through a number of distinct mechanisms: Mimicking insulin action1 Berberine mimics insulin action by increasing glucose uptake ability by 3T3-L1 adipocytes (fat cells) and L6 myocytes (muscle cells) in an insulin-independent manner. Furthering this mimicking process, berberine inhibits activity of protein tyrosine phosphatase 1B (an important negative regulator of insulin and leptin signaling in vivo). It also increases phosphorylation in 3T3-L1 adipocytes. In diabetic mice, berberine lowers hyperglycemia and improves impaired glucose tolerance, but does not increase insulin release and synthesis. The results suggest that berberine represents a different class of anti-hyperglycemic agents. Improving insulin action by activating AMPK2-5 AMPK (AMP-activated protein kinase) is an enzyme that plays a role in cellular energy homeostasis. Principally, the effect of AMPK activation is stimulation of hepatic fatty acid oxidation and ketogenesis,* inhibition of cholesterol synthesis, lipogenesis (the formation of fat), and triglyceride synthesis, inhibition of adipocyte lipolysis and lipogenesis, stimulation of skeletal muscle fatty acid oxidation and muscle glucose uptake, and modulation of insulin secretion by pancreatic beta-cells.6 AMPK is expressed in a number of tissues, including the liver, brain, and skeletal muscle, where it acts as a “metabolic master switch” that regulates several intracellular systems, including the cellular uptake of glucose, the beta-oxidation of fatty acids, and the biogenesis of glucose transporter 4 (GLUT4).7 * Ketogenesis is the process by which ketone bodies are produced as a result of fatty acid breakdown. Glucose is usually used by cells for energy. But, when there’s no insulin to help it transport out of the blood and into the cells, the body has an “energy crisis” and starts to break down body fat into ketones as an alternative fuel source. This is called ketosis. Reducing insulin resistance through protein kinase C (PKC)-dependent up-regulation of insulin receptor (InsR) expression8,9 Berberine induced InsR gene expression through a PKC-dependent activation of its promoter. Inhibition of PKC abolished berberine-caused InsR promoter activation and InsR mRNA transcription. In animal models, treatment of type 2 diabetes mellitus rats with berberine lowered fasting blood glucose and fasting serum insulin, increased insulin sensitivity, and elevated InsR mRNA as well as PKC activity in the liver. Inducing glycolysis10 Berberine has recently been reported to activate AMPK and increase its phosphorylation, which was associated with persistent elevation in AMP/ATP ratio and reduction in oxygen consumption. An increase in glycolysis was observed with a rise in lactic acid production. The results of this suggest that berberine enhances glucose metabolism by stimulation of glycolysis, which is related to inhibition of glucose oxidation in mitochondria. Berberine-induced AMPK activation is likely a consequence of mitochondria inhibition that increases the AMP/ATP ratio. Promoting GLP-1 secretion and modulating its release11,12 Glucagon-like peptide (GLP)-1 is a potent glucose-dependent insulinotropic gut hormone released from intestinal L cells. GLP-1 is one of the incretins, a group of gastrointestinal hormones that cause a short-term increase in the amount of insulin released from the beta cells of the Islets of Langerhans (which also produce insulin in the pancreas) after eating (see above image). Several approved drugs act on incretins, but there are many side effects, a significant number of which are gastrointestinal. This is ironic because berberine has been used to treat gastrointestinal problems. Berberine increased GLP-1 secretion in streptozotocin-induced diabetic rats. In vivo, 5-week treatment of berberine enhanced GLP-1 secretion induced by glucose load and promoted proglucagon mRNA expression as well as L cell proliferation in intestine. In vitro, berberine concentration-dependently stimulated GLP-1 release in NCI-H716 cells. Berberine also promoted both prohormone convertase 3 and proglucagon mRNA expression. This demonstrates that berberine showed its modulation on GLP-1 via promoting GLP-1 secretion and GLP-1 biosynthesis. Inhibition of DPP-413 Berberine was investigated as an inhibitor of human dipeptidyl peptidase IV (DPP IV) in an attempt to explain its anti-hyperglycemic activities. The investigation included simulated docking experiments to fit berberine within the binding pocket of DPP IV. Berberine was found to readily fit within the binding pocket of DPP IV in a low energy orientation characterized with optimal electrostatic attractive interactions bridging the isoquinolinium positively charged nitrogen atom (berberine) and the negatively charged acidic residue of glutamic acid-205 (GLU205) of DPP IV. Experimentally, berberine was found to inhibit human recombinant DPP IV in vitro with IC(50) = 13.3 microM. These findings suggest that DPP IV inhibition is, at least, one of the mechanisms that explain the anti-hyperglycemic activity of berberine. The fact that berberine was recently reported to potently inhibit the pro-diabetic target human protein tyrosine phosphatase 1B (h-PTP 1B) discloses a novel dual natural h-PTP 1B/DPP IV inhibitor. Inhibition of hepatic gluconeogenesis14 Berberine is a compound originally identified in a Chinese herbal medicine Huanglian (Coptis chinensis French). It improves glucose metabolism in type 2 diabetic patients. The mechanisms involve in activation of adenosine monophosphate activated protein kinase (AMPK) and improvement of insulin sensitivity. However, it is not clear if berberine reduces blood glucose through other mechanism. In this study, we addressed this issue by examining liver response to berberine in diabetic rats, in which hyperglycemia was induced in Sprague-Dawley rats by high fat diet. We observed that berberine decreased fasting glucose significantly. Gluconeogenic genes, Phosphoenolpyruvate carboxykinase (PEPCK) and Glucose-6-phosphatase (G6Pase), were decreased in liver by berberine. Hepatic steatosis was also reduced by berberine and expression of fatty acid synthase (FAS) was inhibited in liver. Activities of transcription factors including Forkhead transcription factor O1 (FoxO1), sterol regulatory element-binding protein 1c (SREBP1) and carbohydrate responsive element-binding protein (ChREBP) were decreased. Insulin signaling pathway was not altered in the liver. In cultured hepatocytes, berberine inhibited oxygen consumption and reduced intracellular adenosine triphosphate (ATP) level. The data suggest that berberine improves fasting blood glucose by direct inhibition of gluconeogenesis in liver. This activity is not dependent on insulin action. The gluconeogenic inhibition is likely a result of mitochondria inhibition by BBR. The observation supports that berberine improves glucose metabolism through an insulin-independent pathway. References Chen C, Zhang Y, Huang C. Berberine inhibits PTP1B activity and mimics insulin action. Biochem Biophys Res Commun Jul 2 2010;397(3):543-7. Turner N, Li JY, Gosby A, et al. Berberine and its more biologically available derivative, dihydroberberine, inhibit mitochondrial respiratory complex I: a mechanism for the action of berberine to activate AMP-activated protein kinase and improve insulin action. Diabetes May 2008;57(5):1414-8. Lee YS, Kim WS, Kim KH, et al. Berberine, a natural plant product, activates AMP-activated protein kinase with beneficial metabolic effects in diabetic and insulin-resistant states. Diabetes Aug 2006;55(8):2256-64. Ma X, Egawa T, Kimura H, et al. Berberine-induced activation of 5’-adenosine monophosphate-activated protein kinase and glucose transport in rat skeletal muscles. Metabolism 2010 Nov;59(11):1619-27. Hwang JT, Kwon DY, Yoon SH. AMP-activated protein kinase: a potential target for the diseases prevention by natural occurring polyphenols. N Biotechnol Oct 1 2009;26(1-2):17-22. Winder WW, Hardie DG. AMP-activated protein kinase, a metabolic master switch: possible roles in type 2 diabetes. Am J Physiol Jul 1999;277(1 Pt 1):E1-10. Viollet B, Mounier R, Leclerc J, Yazigi A, Foretz M, Andreelli F. Targeting AMP-activated protein kinase as a novel therapeutic approach for the treatment of metabolic disorders. Diabetes Metab Dec 2007;33(6):395-402. Zhang H, Wei J, Xue R, et al. Berberine lowers blood glucose in type 2 diabetes mellitus patients through increasing insulin receptor expression. Metabolism Feb 2009;59(2):285-92. Kong WJ, Zhang H, Song DQ, et al. Berberine reduces insulin resistance through protein kinase C-dependent up-regulation of insulin receptor expression.Metabolism Jan 2009;58(1):109-19. Yin J, Gao Z, Liu D, Liu Z, Ye J. Berberine improves glucose metabolism through induction of glycolysis. Am J Physiol Endocrinol Metab Jan 2008;294(1):E148-56. Lu SS, Yu YL, Zhu HJ, et al. Berberine promotes glucagon-like peptide-1(7-36) amide secretion in streptozotocin-induced diabetic rats. J Endocrinol Feb 2009;200(2):159-65. Yu Y, Liu L, Wang X, Liu X, Xie L, Wang G. Modulation of glucagon-like peptide-1 release by berberine: in vivo and in vitro studies. Biochem Pharmacol Apr 1 2009;79(7):1000-6. Al-masri IM, Mohammad MK, Tahaa MO. Inhibition of dipeptidyl peptidase IV (DPP IV) is one of the mechanisms explaining the hypoglycemic effect of berberine. J Enzyme Inhib Med Chem Oct 2009;24(5):1061-6 Xia X, Yan J, Shen Y, Tang K, Yin J, Zhang Y, Yang D, Liang H, Ye J, Weng J. Berberine improves glucose metabolism in diabetic rats by inhibition of hepatic gluconeogenesis. PLoS One 2011 Feb 3;6(2):e16556.

[brosgym]

iniziamo con la gimnema

Mechanism of Action of Gymnemic Acids

Gymnemic acid formulations have also been found useful against obesity, according to recent reports [10]. This is attributed to the ability of gymnemic acids to delay the glucose absorption in the blood. The atomic arrangement of gymnemic acid molecules is similar to that of glucose molecules. These molecules fill the receptor locations on the taste buds thereby preventing its activation by sugar molecules present in the food, thereby curbing the sugar craving. Similarly, Gymnemic acid molecules fill the receptor location in the absorptive external layers of the intestine thereby preventing the sugar molecules absorption by the intestine, which results in low blood sugar level [11].
G. sylvestre leaves have been found to cause hypoglycemia in laboratory animals and have found a use in herbal medicine to help treat adult onset diabetes mellitus (NIDDM). When Gymnema leaf extract is administered to a diabetic patient, there is stimulation of the pancreas by virtue of which there is an increase in insulin release [12]. These compounds have also been found to increase fecal excretion of cholesterol [13], but further studies to prove clinical significance in treating hypercholesterolemia (high serum cholesterol) are required. Other uses for Gymnema leaf extract are its ability to act as a laxative, diuretic, and cough suppressant. These other actions would be considered adverse reactions whenGymnema is used for its glucose lowering effect in diabetes.
Gymnema leaf extract, notably the peptide ‘Gurmarin’, has been found to interfere with the ability of the taste buds on the tongue to taste sweet and bitter. Gymnemic acid has a similar effect. It is believed that by inhibiting the sweet taste sensation, people taking it will limit their intake of sweet foods, and this activity may be partially responsible for its hypoglycemic effect [14].
There are some possible mechanisms by which the leaves and especially Gymnemic acids from G. sylvestre exert its hypoglycemic effects are: 1) it increases secretion of insulin, 2) it promotes regeneration of islet cells, 3) it increases utilization of glucose: it is shown to increase the activities of enzymes responsible for utilization of glucose by insulin-dependant pathways, an increase in phosphorylase activity, decrease in gluconeogenic enzymes and sorbitol dehydrogenase, and 4) it causes inhibition of glucose absorption from intestine.
The gymnemic acid components are believed to block the absorption of glucose in the small intestine, the exact action being unknown. It could be involve one or more mechanisms [14].
One of the mechanisms responsible for adult onset diabetes mellitus is a form of insulin resistance, which is attributed to the inability of insulin to enter cells via the insulin receptor. Gymnema may overcome this resistance, but require further studies to confirm its validity and also whether the effect is clinically relevant. Should this effect be proven, Gymnema may prove useful in both adult onset (NIDDM) and juvenile onset diabetes mellitus (IDDM) to help insulin enter cells. In the case of IDDM, the insulin is injected by syringe and is not secreted from the pancreas [15].
The leaves are also noted for lowering serum cholesterol and triglycerides. The primary chemical constituents of Gymnema include gymnemic acid, tartaric acid, gurmarin, calcium oxalate, glucose, stigmasterol, betaine, and choline. While the water-soluble acidic fractions reportedly provide the hypoglycemic action, it is not yet clear what specific constituent in the leaves is responsible for the same. Some researchers have suggested gymnemic acid as one possible candidate, although further research is needed [16]. Both gurmarin (another constituent of the leaves) and gymnemic acid have been shown to block sweet taste in humans. The major constituents of the plant material 3B glucuronides of different acetylated gymnemagenins, gymnemic acid a complex mixture of at least 9 closely related acidic glucosides [17–19].
The following figure could provide a diagrammatic representation for explaining the action of gymnemic acids on the intestinal receptors. The basic function of the acids is to bind to the receptor on the intestine, and stop the glucose molecule from binding to the receptor. Thus, gymnemic acids prevent the absorption of excess glucose.

---------- Post added at 17:59:01 ---------- Previous post was at 17:57:18 ----------

Innanzitutto buon contributo però.....

Dei 4 meccanismi proposti
1) alquanto improbabile, al tal proposito leggere la referenza 10 sarebbe utile....
2) possibile ma nel nostro caso serve a poco..
3) possibile ma da provare, mi sembra un pò un giro contorto e basato su un meccanismo patologico
4) forse la più probabile, ma non ci serve....anzi!

Edit leggendo l'abstract della 10, c'è un'attivazione dell'AMPK, anche se sugli amici roditori....certo sono meccanismi che andrebbero valutati....anche per possibili sides...che non conosciamo