The effect of Korean pine nut oil (PinnoThin™) on food intake, feeding behaviour and appetite: A double-blind placebo-controlled trial

Certain free fatty acids have been shown to have potent effects on food intake and self-reported changes in appetite; effects associated with increases in the release of endogenous cholecystokinin (CCK) and glucagon like peptide-1 (GLP-1). In the current study, the effects of a Korean pine nut oil product, PinnoThin™, at doses 2 g, 4 g and 6 g triglyceride (TG) and 2 g free fatty acid (FFA), on food intake and appetite were examined in a cross-over double-blind placebo-controlled randomised counter-balanced design in 42 overweight female volunteers. 2 g FFA PinnoThin™, given 30 minutes prior to an ad-libitum buffet test lunch, significantly reduced food intake (gram) by 9% (F(4,164) = 2.637, p = 0.036) compared to olive oil control. No significant effect of PinnoThin™ on macronutrient intake or ratings of appetite were observed. Given the recent data showing that the TG form of PinnoThin™ may also reduce appetite by increasing CCK release, the lack of any effect of the TG form found in this study could be attributed to the timing of the dosing regime. Collectively, these data suggest that PinnoThin™ may exert satiating effects consistent with its known action on CCK and GLP-1 release, and previously observed effects on self-reported appetite ratings

Newly published studies on satiety benefits of Korean pine nut oil (PinnoThin™)

A Korean pine nut oil product, PinnoThin™, has been shown to trigger the release of the satiety gut hormone cholecystokinin (CCK) in vitro. Recently published randomized, placebo-controlled double-blind crossover clinical trials have investigated the effects of PinnoThin™ on satiety markers. A clinical trial in 18 overweight postmenopausal women, studied the effects of PinnoThin™ free fatty acid (FFA) and triglyceride (TG) versus placebo (olive oil) on CCK and glucagon peptide-1 (GLP-1) release and appetite sensations. PinnoThin™ FFA and TG were shown to have significant effects on CCK release, while PinnoThin™ FFA had significant effects on GLP-1. Prospective food intake assessed by visual analogue scale (VAS) was significantly reduced 30 minutes after PinnoThin™ FFA intake. Another study on 42 overweight young women investigated the effects of PinnoThin™ FFA and different doses of PinnoThin™ TG versus placebo (olive oil) on food intake, feeding behaviour and appetite. Pinno- Thin™ FFA given 30 minutes prior to ad libitum buffet lunch significantly reduced food intake (grams) and tended to decrease energy intake (kcal) compared to placebo, while no compensation for the reduced intake was observed at ad libitum dinner. Since it was previously shown that PinnoThin™ TG is normally hydrolyzed to PinnoThin™ FFA, the differential results seen in the case of PinnoThin™ FFA and TG are consistent with a delay in TG conversion to FFA. These studies suggest that PinnoThin™ has satiating effects corresponding to increased release of satiety hormones CCK and GLP-1 and decrease in subsequent food intake

Newly published studies on satiety benefits of Korean pine nut oil (PinnoThin™)

A Korean pine nut oil product, PinnoThin™, has been shown to trigger the release of the satiety gut hormone cholecystokinin (CCK) in vitro. Recently published randomized, placebo-controlled double-blind crossover clinical trials have investigated the effects of PinnoThin™ on satiety markers. A clinical trial in 18 overweight postmenopausal women, studied the effects of PinnoThin™ free fatty acid (FFA) and triglyceride (TG) versus placebo (olive oil) on CCK and glucagon peptide-1 (GLP-1) release and appetite sensations. PinnoThin™ FFA and TG were shown to have significant effects on CCK release, while PinnoThin™ FFA had significant effects on GLP-1. Prospective food intake assessed by visual analogue scale (VAS) was significantly reduced 30 minutes after PinnoThin™ FFA intake. Another study on 42 overweight young women investigated the effects of PinnoThin™ FFA and different doses of PinnoThin™ TG versus placebo (olive oil) on food intake, feeding behaviour and appetite. Pinno- Thin™ FFA given 30 minutes prior to ad libitum buffet lunch significantly reduced food intake (grams) and tended to decrease energy intake (kcal) compared to placebo, while no compensation for the reduced intake was observed at ad libitum dinner. Since it was previously shown that PinnoThin™ TG is normally hydrolyzed to PinnoThin™ FFA, the differential results seen in the case of PinnoThin™ FFA and TG are consistent with a delay in TG conversion to FFA. These studies suggest that PinnoThin™ has satiating effects corresponding to increased release of satiety hormones CCK and GLP-1 and decrease in subsequent food intake

The effect of Korean pine nut oil on in vitro CCK release, on appetite sensations and on gut hormones in post-menopausal overweight women

Abstract Appetite suppressants may be one strategy in the fight against obesity. This study evaluated whether Korean pine nut free fatty acids (FFA) and triglycerides (TG) work as an appetite suppressant. Korean pine nut FFA were evaluated in STC-1 cell culture for their ability to increase cholecystokinin (CCK-8) secretion vs. several other dietary fatty acids from Italian stone pine nut fatty acids, oleic acid, linoleic acid, alpha-linolenic acid, and capric acid used as a control. At 50 μM concentration, Korean pine nut FFA produced the greatest amount of CCK-8 release (493 pg/ml) relative to the other fatty acids and control (46 pg/ml). A randomized, placebo-controlled, double-blind cross-over trial including 18 overweight post-menopausal women was performed. Subjects received capsules with 3 g Korean pine (Pinus koraiensis) nut FFA, 3 g pine nut TG or 3 g placebo (olive oil) in combination with a light breakfast. At 0, 30, 60, 90, 120, 180 and 240 minutes the gut hormones cholecystokinin (CCK-8), glucagon like peptide-1 (GLP-1), peptide YY (PYY) and ghrelin, and appetite sensations were measured. A wash-out period of one week separated each intervention day. CCK-8 was higher 30 min after pine nut FFA and 60 min after pine nut TG when compared to placebo (p This study suggests that Korean pine nut may work as an appetite suppressant through an increasing effect on satiety hormones and a reduced prospective food intake.</p

(closed circles) Pine nut FFA, (closed triangles) pine nut TG, (open squares) placebo

Significant differences (p < 0.05) indicated by a: pine nut FFA versus placebo, b: pine nut TG versus placebo.<p><b>Copyright information:</b></p><p>Taken from "The effect of Korean pine nut oil on in vitro CCK release, on appetite sensations and on gut hormones in post-menopausal overweight women"</p><p>http://www.lipidworld.com/content/7/1/10</p><p>Lipids in Health and Disease 2008;7():10-10.</p><p>Published online 20 Mar 2008</p><p>PMCID:PMC2322999.</p><p></p

<i>N</i>′-(Arylsulfonyl)pyrazoline-1-carboxamidines as Novel, Neutral 5-Hydroxytryptamine 6 Receptor (5-HT₆R) Antagonists with Unique Structural Features

The 5-HT₆ receptor (5-HT₆R) has been in the spotlight for several years regarding CNS-related diseases. We set out to discover novel, neutral 5-HT₆R antagonists to improve off-target selectivity compared to basic amine-containing scaffolds dominating the field. High-throughput screening identified the <i>N</i>′-(sulfonyl)pyrazoline-1-carboxamidine scaffold as a promising neutral core for starting hit-to-lead. Medicinal chemistry, molecular modeling, small molecule NMR and X-ray crystallography were subsequently applied to optimize the leads into antagonists (compounds <b>1</b>–<b>49</b>) displaying high 5-HT₆R affinity with optimal off-target selectivity. Unique structural features include a pseudoaromatic system and an internal hydrogen bond freezing the bioactive conformation. While physicochemical properties and CNS availability were generally favorable, significant efforts had to be made to improve metabolic stability. The optimized structure <b>42</b> is an extremely selective, hERG-free, high-affinity 5-HT₆R antagonist showing good human in vitro metabolic stability. Rat pharmacokinetic data were sufficiently good to enable further in vivo profiling