Hypophagic and weight reducing effect of Momardica charinta fruit by Enhancing 5-HT neurotransmitter in rats brain.

Momardica charint seed as vegetable and folk medicine in Pakistan, India, China, Bangladesh and other Asian countries Momardica charinta also known as Kerala, bittergourd ,balsam pear. It possesses many biological active constituents including glycosides, saponins, phenolic and flavonoids compound, protein, triterpenes, steroid, saponins, alkaloid. It also contain thiamine ,beta carotene, folate, riboflavin, calcium, iron, potassium, zinc and fiber. Several studies have been done to show medicinal importance of its fruit which has different biological functions such as anti-diabetes antihypertension, antiviral, antibacterial and antifungal infection, anti-tumorous as well as anti-carcinogenic effects. The present research is big contribution of Momardicacharinta activity as weight reducing plant through serotonergic neurotransmitter Decrease in body weight and food intake might be due to increased concentration of serotonin in their respective receptors in brain, which produce hypophagic effect in rats treated with water extract of Momardicacharinttia. More animal and human trials needed to confirm, the safety and antiobesity effect of MC and the role of neurotransmitter involve in reduction of body weight.

Characteristics and functionality of appetite-reducing thylakoid powders produced by three different drying processes.

BACKGROUND: Thylakoids, a chloroplast membrane extracted from green leaves, are a promising functional ingredient with appetite-reducing properties via their lipase-inhibiting effect. Thylakoids in powder form have been evaluated in animal and human models, but no comprehensive study has been conducted on powder characteristics. The aim was to investigate the effects of different isolation methods and drying techniques (drum-drying, spray-drying, freeze-drying) on thylakoids' physicochemical and functional properties. RESULTS: Freeze-drying yielded thylakoid powders with the highest lipase-inhibiting capacity. We hypothesize that the specific macromolecular structures involved in lipase inhibition were degraded to different degrees by exposure to heat during spray-drying and drum-drying. We identified lightness (Hunter's L-value), greenness (Hunter's a-value), chlorophyll content and emulsifying capacity to be correlated to lipase-inhibiting capacity. Thus, to optimize the thylakoids functional properties, the internal membrane structure indicated by retained green colour should be preserved. This opens possibilities to use chlorophyll content as a marker for thylakoid functionality in screening processes during process optimization. CONCLUSION: Thylakoids are heat sensitive, and a mild drying technique should be used in industrial production. Strong links between physicochemical parameters and lipase inhibition capacity were found that can be used to predict functionality. The approach from this study can be applied towards production of standardized high-quality functional food ingredients. © 2017 Society of Chemical Industry.

New pregnane glycosides from Brucea javanica and their antifeedant activity.

Three new pregnane glycosides, 3-O-ß-D-glucopyranosyl-(1→2)-α-L-arabinopyranosyl-(20R)-pregn-5-ene-3ß,20-diol (1), 3-O-α-L-arabinopyranosyl-(20R)-pregn-5-ene-3ß,20-diol-20-O-ß-D-glucopyranoside (2), 3-O-α-L-arabinopyranosyl-(20R)-pregn-5-ene-3ß,20-diol-20-O-ß-D-glucopyranosyl-(1→2)-ß-D-glucopyranoside (3) were isolated along with four known compounds, 4-7, from the leaves and stems of Brucea javanica. Their structures were determined by detailed analyses of 1D- and 2D-NMR spectroscopic data. All of the compounds isolated from Brucea javanica were tested for the antifeedant activities against the larva of Pieris rapae. Compounds 1, 3, and 5 showed significant antifeedant activities after 72 h incubation.

Fenugreek Cultivation with Emphasis on Historical Aspects and its uses in Traditional Medicine and Modern Pharmaceutical Science.

Fenugreek (Trigonella foenum-graecum L.) is a native plant found in the parts of Iran to the North of India, and is presently planted also in other regions of the world. Fenugreek is considered a notable multipurpose medicinal and traditional herb in Iran, India, and China for several centuries. The most important components of fenugreek seeds are protein, neutral detergent fiber, gum, lipids, moisture, ash and starch. Fenugreek seeds and leaves are anti-cholesterolemic, anti-tumor, antiinflammatory, carminative, demulcent, deobstruent, emollient, expectorant, galactogogue, febrifuge, laxative, hypoglycaemic, restorative, parasiticide and uterine tonic and useful in burning sensation. Traditionally, fenugreek seeds being used worldwide are beneficial for bone and muscles, respiratory system, gastro-intestinal system, female reproductive system, cardio-vascular system, endocrinology and hepatic. Fenugreek helps reduce cholesterol, reduce cardiovascular risk, control diabetes, a good consolation for sore throats, a remedy for acid reflux, constipation, colon cancer prevention, appropriate for kidney trouble, skin infection, increase milk production, reduce menstrual discomfort, and reduce menopause symptoms. It is also an appetite suppressant that helps in weight loss. Both modern science and traditional medicine integration with novel technologies and discoveries will secure the cultivation of medicinal herbs and promote sustainability in the long-term and a wide-range.

Bioavailability, pharmacokinetics, and tissue distribution of the oxypregnane steroidal glycoside P57AS3 (P57) from Hoodia gordonii in mouse model.

P57AS3 (P57), an oxypregnane steroidal glycoside, is known to be responsible for the appetite suppressing activity of HOODIA GORDONII, a dietary supplement used for weight loss. In this study, bioavailability, pharmacokinetics, and tissue distribution of P57 were determined in CD1 female mice after administration of a single dose of enriched methanolic extract of HOODIA GORDONII (equivalent to a dose of 25 mg of P57/kg) by oral gavage or a single dose of purified P57 (25 mg/kg) intravenously. The level of P57 in plasma and tissues (brain, liver, kidney, and intestine) was determined by UPLC-MS. After oral administration of HOODIA extract, the peak plasma level of P57 was achieved in 0.6 h. Upon intravenous administration, the plasma clearance rate of P57 was 1.09 L/h/kg. P57 was rapidly distributed and eliminated from the tissues within 4 hours. The level of tissue distribution was highest in the kidney followed by liver and brain. Upon oral administration, P57 was not detected in the brain and a very low concentration was seen in the intestine, kidney, and liver. Tissue/plasma ratio was 0.33 for brain, 0.57 for liver, and 0.75 for kidney with IV route and 0.11 for intestine, 0.02 for liver, and 0.04 for kidney with oral route. The half-life of the elimination phase was similar with both routes. The oral bioavailability was 47.5 % and the half-life of the absorption phase was 0.13 h. In conclusion, P57 showed moderate bioavailability and was eliminated rapidly.

Antifeedant activity of anticopalic acid isolated from Vitex hemsleyi.

The known labdane-type diterpenoids anticopalic acid (1) and 3 beta-hydroxyanticopalic acid (2) were isolated from extracts of the aerial parts of Vitex hemsleyi Briq. (Labiatae). The acid 1 showed an antifeedant, dose-dependent activity against Spodoptera frugiperda (J. E. Smith) (Lepidoptera: Noctuidae). To our knowledge this is the first report on the antifeedant activity of a labdane-type diterpene against S. frugiperda.

[Bryophytes, a potent source of drugs for tomorrow's medicine?]. / Les Bryophytes, source potentielle de médicaments de demain?

Although secondary plant metabolites provided numerous leads for the development of a wide array of therapeutic drugs, the discovery of new drugs with novel structures has declined in the past few years. Indeed higher plants have a similar evolutionary history and so produce similar metabolites. Search for novel sources of new therapeutic compounds within unexplored parts of biodiversity is thus an attractive challenge. Bryophytes, a group of small terrestrial plants remain relatively untouched in the drug discovery process whereas some have been used as medicinal plants. Studies of their secondary metabolites are recent but reveal original compounds, some of which not synthesized by higher plants. However investigations often meet difficulties during harvest or isolation of active compounds. In consequence, small quantities of substances obtained may be the main reason for the lack of biological tests. Strategies to overcome those troubles may exist and then lead to innovative medicinal applications.

Preparation of Pinolenic Acid Concentrates from Pine Nut Oil Fatty Acids by Solvent Fractionation.

Pinolenic acid (PLA), which is a fatty acid (FA) exclusively found in the oils of edible pine nuts, has an appetite-suppression effect, thereby being effective to reduce body weight in humans. PLA concentrates would be suitable for use in functional foods and nutraceuticals due to the health benefits of PLA. PLA concentrates were prepared from free FA (FFA) obtained from pine nut oil using solvent fractionation. Siberian pine nut oil containing 18.3 wt% PLA was used as the starting material for the fractionation. The fractionation was performed in n-hexane at ultra-low temperatures down to -85°C. The PLA concentrates produced under the optimal conditions established in this study (temperature, -85°C; n-hexane-to-FFA ratio (v/w), 30:1; fractionation time, 36 h) contained 69.8 wt% PLA. The yield of PLA was 77.4 wt% of the initial PLA weight in the FFA. These results suggest that solvent fractionation is a more effective approach to prepare PLA concentrates with higher PLA contents at a particular yield of PLA than published methods using urea crystallization (e.g., PLA content = ~47 wt%, yield of PLA = ~77 wt%, Woo et al. (2016)) or lipase-catalyzed reactions (e.g., PLA content = ~30 wt%, yield of PLA = ~61 wt%, Lee et al. (2011)). The resulting PLA concentrates contained 11 of the 12 different species of FA present in the FFA, thereby indicating that the PLA concentrates prepared by solvent fractionation have more diverse FA profiles than those prepared by urea crystallization (e.g., 7 species of FA, Woo et al. (2016)).

Satietogenic Protein from Tamarind Seeds Decreases Food Intake, Leptin Plasma and CCK-1r Gene Expression in Obese Wistar Rats.

OBJECTIVE: This study evaluated the effect of a protein, the isolated Trypsin Inhibitor (TTI) from Tamarindus indica L. seed, as a CCK secretagogue and its action upon food intake and leptin in obese Wistar rats. METHODS: Three groups of obese rats were fed 10 days one of the following diets: Standard diet (Labina®) + water; High Glycemic Index and Load (HGLI) diet + water or HGLI diet + TTI. Lean animals were fed the standard diet for the 10 days. Food intake, zoometric measurements, plasma CCK, plasma leptin, relative mRNA expression of intestinal CCK-related genes, and expression of the ob gene in subcutaneous adipose tissue were assessed. RESULTS: TTI decreased food intake but did not increase plasma CCK in obese animals. On the other hand, TTI treatment decreased CCK-1R gene expression in obese animals compared with the obese group with no treatment (p = 0.027). Obese animals treated with TTI presented lower plasma leptin than the non-treated obese animals. CONCLUSION: We suggest that TTI by decreasing plasma leptin may improve CCK action, regardless of its increase in plasma from obese rats, since food intake was lowest.

An appetite suppressant from Hoodia species.

Studies conducted at the Council for Scientific and Industrial Research (CSIR, South Africa) identified extracts from Hoodia species, in particular Hoodia pilifera and Hoodia gordonii, as possessing appetite suppressing properties. Two pregnane glycosides were isolated by fractionation of the dried stems of H. gordonii. Their structures were determined as 3beta-[beta-D-thevetopyranosyl-(1-->4)-beta-D- cymaropyranosyl-(1-->4)-beta-D-cymaropyranosyloxy]-12beta-tigloyloxy-14beta-hydroxypregn-5-en-20-one (1) and 3beta-[beta-D-cymaropyranosyl-(1-->4)-beta-D-6-thevetopyranosyl-(1-->4)-beta-D-cymaropyranosyl-(1-->4)-beta-D-cymaropyranosyloxy]-12beta-tigloyloxy-14beta-hydroxypregn-5-en-20-one (2) on the basis of spectroscopic studies and conversion to known compounds. Compounds 1 and 2 were also isolated from H. pilifera. Compound 1 was tested for its appetite suppressant properties in rats by oral gavage at 6.25-50 mg/kg and the results showed that all doses resulted in a decrease of food consumption over an eight day period and a body mass decrease when compared to the control sample receiving only the vehicle. In a comparative study against a fenfluramine control sample, compound 1 resulted in a reduction in food intake over the study period, with a concomitant overall decrease in body weight while fenfluramine resulted in a small decrease in food intake, but an increase in body weight (though less than control group) over the same period of time.

Determination of the appetite suppressant P57 in Hoodia gordonii plant extracts and dietary supplements by liquid chromatography/electrospray ionization mass spectrometry (LC-MSD-TOF) and LC-UV methods.

Hoodia gordonii is traditionally used in South Africa for its appetite suppressant properties. P57AS3 (P57), an oxypregnane steroidal glycoside, is the only reported active constituent from this plant as an appetite suppressant. Effective quality control of these extracts or products requires rapid methods to determine P57 content. New methods of liquid chromatography/mass spectrometry (LC/MS) and LC-UV for analysis of P57 from H. gordonii have been developed. The quantitative determination of P57 was achieved with a Phenomenex Gemini (Torrance, CA) reversed-phase column using gradient mobile phase of water and acetonitrile, both containing 0.1% acetic acid. The method was validated for linearity, repeatability, and limits of detection and quantification. Good results were obtained in terms of repeatability (relative standard deviation <5.0%) and recovery (98.5-103.5%). The developed methods were applied to the determination of P57 for H. gordonii plant samples, one related genus (Opuntia ficus-indica), and dietary supplements that claim to contain H. gordonii.

Hydroxamic acids in Secale cereale L. and the relationship with their antifeedant and allelopathic properties.

Contents of the hydroxamic acids 2,4-dihydroxy-1,4-benzoxazin-3-one (DIBOA), and 2,4-dihydroxy-7-methoxy-1,4-benzoxazin-3-one (DIMBOA) in leaves and roots of 14 cultivars of rye, Secale cereale L., were determined. Dynamics of accumulation in three cultivars were evaluated. DIBOA was the main cyclic hydroxamic acid in leaves but the contents differed significantly between the cultivars. Both DIBOA and DIMBOA were present in the roots. Maximum concentration of DIBOA in leaves and DIMBOA in roots was reached between 48-54 h and 54-72 h after germination, respectively. Antifeedant activity of DIBOA towards the aphid Rhopalosiphum padi and the feeding behavior were studied by electronic recording in barley leaves treated with different contents of DIBOA. The deleterious activity of DIBOA could arise by starvation and/or a toxic effect. Additionally, allelopathic potential of pure DIBOA and aqueous extracts of leaves and roots of rye (Tetra-Baer) on the germination of lettuce (Lactuca sativa) and rye (Tetra-Baer) seeds was evaluated. A high percentage of germination inhibition of pure DIBOA and the extracts of leaves and roots was observed. The activity is in agreement with the contents of hydroxamic acids in the plants. The substrates had no allelopathic effect on rye seeds.

A 50000-dalton anorexigenic protein from urine.

A potent, homogeneous, 50 kDa protein which transiently depresses food intake of rats up to 24 h after injection was isolated from rat urine. It was prepared from an ethanolic benzoic acid precipitate of urine. The material was subjected to DEAE-Sephacel chromatography, whereupon four fractions (DEAE pools a, b, c, and d) were obtained. The latter three contained anorexigenic activity. DEAE pools b and c were subjected to further purification on columns of Sephacryl S-300 eluted with buffer containing 8 M urea. One of the subfractions of DEAE pool b contained only one protein as judged by polyacrylamide gel electrophoresis in sodium dodecyl sulfate. This protein had a molecular weight of 50,000 and was active in reducing 24 h food intake at a dose of 130 micrograms/100 g bodyweight.

A lectin from an edible mushroom Pleurotus ostreatus as a food intake-suppressing substance.

In an experiment in which rats were allowed free access to food and water, the rats did not eat the diet containing a mushroom Pleurotus ostreatus even if they were emaciated. A P. ostreatus lectin (POL) was isolated from the mushroom as the food intake-suppression principle. In hemagglutination inhibition assays, Me-alphaGalNAc was the most potent inhibitor among the monosaccharides tested. Among all the sugars tested, 2'-fucosyllactose (Fucalpha1-->2Galbeta1-->4Glc) was the strongest inhibitor and its inhibitory potency was five times greater than that of Me-alphaGalNAc. POL exhibited a binding ability to bovine submaxillary mucin (BSM) and asialo-BSM and the other glycoproteins were inert to the binding. The food intake-suppressing activity of POL was dependent on the dose. The diet containing 0.1% POL caused a 50% decrease in the food intake of rats against the control.

Pyrrolizidine alkaloids from Anchusa strigosa and their antifeedant activity.

The pyrrolizidine alkaloid (PA) content of flowers, leaves, and roots of Anchusa strigosa (Boraginaceae) was analysed by ESI-LC-MS. Six PAs, including two new natural compounds, were detected, characterized by NMR spectroscopy, and quantified in each plant organ. The results indicated that the highest total concentration of PAs was in the leaves (23.63 mg/g of dried part), followed by the flowers (19.77 mg/g), and finally by the roots (1.80 mg/g). All PAs isolated were subjected to Spodoptera exigua and Pieris brassicae larvae. Feeding activity by both herbivore species using a bioassay was inhibited up to circa 75% depending on PA and applied concentration.

The effects of semi- and HPLC-purified human satietin and alpha-1-glycoprotein on ingestion and body weight.

Satietin is thought to be an endogenous glycoprotein that can suppress food intake (FI) and body weight (b.wt.). In Experiment 1, rats were ICV infused with either a-CSF or with 50 micrograms/rat of human satietin. FI was suppressed (p less than 0.05) for 2 days after infusion, whereas b.wt. was attenuated (p less than 0.05) for 14 days. In Experiment 2, the previously thought homogenous human satietin was further purified by HPLC and this yielded two peaks (A and B). Rats were ICV infused with either a-CSF or 50 micrograms/rat of Peak A, Peak B or the semipurified parent human satietin (sph-SAT) from which the peaks were derived. All three treatments suppressed (p less than 0.05) FI on day 1 after infusion and on day 2 in the groups that received Peak A and sph-SAT. Body weight was attenuated (p less than 0.01) in all the experimental groups on day 1 and for 2 and 10 days, respectively, in the Peak A and sph-SAT-treated groups. Immunostaining revealed Peak A contained both albumin and alpha-1-glycoprotein (A1G), whereas Peak B contained neither. In the last experiment rats were ICV infused with either a-CSF or 50 micrograms/rat of A1G or A1G that was put through the sph-SAT extraction procedure. FI was suppressed (p less than 0.01) and b.wt. attenuated in both experimental groups only on the first day postinfusion. These data suggest that some, but possibly not all, of the previously found biological activity attributed to sph-SAT might be due to contaminants of the preparation.

Food intake suppression in rats by a substance isolated from human feces.

A substance which suppresses food intake was isolated from human feces. This substance was extracted and partially purified using Sephacryl S-200 column chromatography and a DEAE-Sephadex A-25 column chromatography. To assess the biological activity, rats were subjected to various applications. The intraperitoneal administration and the intracerebroventricular microinfusion of this substance suppresses short- and long-term food intake. The central infusion suppresses feeding with a potency over 1000 times that the peripheral administration. The central infusion of the heat-treated substance was without effect. These results suggest that a substance present in human feces (probably of a proteic nature) suppresses food intake in rats, at the level of the central nervous system.

Purification of the anorectic agent satietin from bovine serum.

Purification and properties of an endogenous anorexigenic substance extracted from the bovine serum has recently been reported. The semipurified and HPLC-purified substances have shown similar biological effect in ad lib-fed or fasted rats, as was found in the case of human satietin. This substance purified from bovine serum or plasma suppressed food intake following intracerebroventricular (ICV) or peripheral administration in rats. A similar purification procedure as was used for the preparation of human serum satietin resulted in semipurified bovine material. This preparation was further purified by HPLC reversed-phase column and yielded two peaks (peak 1 and peak 2). The retention time of peak 2 revealed by HPLC (peak addition method) and the molecular weight measurements carried out by polyacrylamide gel electrophoresis in the presence of sodium dodecyl sulfate (SDS-PAGE) and high performance size-exclusion chromatography (SE-HPLC) proved that peak 2 contains bovine serum albumin mostly. Rats were injected with 20 micrograms/rat of peak 1 and peak 2. Peak 1 can be considered as a putative satiety agent. Preliminary chemical and biochemical studies showed that the semipurified active agent contained 20-22% protein, 28-30% lipids, and an undetermined amount of carbohydrate. The molecular size of anorectic bovine serum preparation was 38-40 kDa, determined by means of SE-HPLC and SDS-PAGE. Based upon the similarity of chemical and biological nature to human serum satietin we named this new material bovine serum satietin (BS-SAT).

HPLC-purified bovine satietin suppresses food intake and weight without causing conditioned taste aversion.

Satietin (SAT) is a putative satiety agent found in a variety of species including man and the rat. In the present study, satietin was extracted from bovine plasma (b-SAT) and further high-pressure liquid chromatography (HPLC)-purified. Rats were given chronic third ventricle cannulas and patency was verified. In experiment 1, rats were divided into three groups and ICV infused with artificial cerebrospinal fluid (a-CSF) or b-SAT: group 1, a-CSF (n = 11); group 2, 20 micrograms/rat, b-SAT (n = 11); and group 3, 40 micrograms/rat, b-SAT (n = 9). Infusions were repeated thrice three days apart. Compared to a-CSF, the high b-SAT dose suppressed food intake for 24-h after each successive infusion. The low dose significantly decreased food intake only after the first infusion. Water intake was suppressed only after the first injection of the high dose. Body weight was decreased after the first and second infusions of both doses and following the third infusion of the high dose. In experiment 2, rats were trained to drink fluid for 1 h/day while food was ad lib. On day 1, both groups received no infusions and were given tap water. On day 2, the groups were ICV infused with a-CSF, but group 1 (n = 12) was given banana-flavored fluid (BFF) and group 2 (n = 12) almond-flavored fluid (AFF). On day 3, group 1 was again a-CSF-infused but given AFF, whereas group 2 received 40 micrograms/rat b-SAT and was given BFF.(ABSTRACT TRUNCATED AT 250 WORDS)

Experimental anorexigenic effect of a membrane proteoglycan isolated from plants.

The cessation of eating under normal physiological conditions is a voluntary act induced by a conscious sensation known as satiety. In pathological situations there is loss of appetite or anorexia. We have been able to isolate and characterize a proteoglycan from membranes of mono- and dicotyledonous plant sprouts which reduced the food intake significantly when injected into murine model systems without any rebound. Due to its membrane origin, it has been termed 'satiomem'. The plant proteoglycan (50 kDa) consisted of 70-85% carbohydrates and 15-30% proteins.