Evaluation of in vitro lipid-lowering properties of ‘Saba’ banana [Musa acuminata x balbisiana (BBB group) ‘Saba’] peel pectin from different extraction methods

@#Introduction: This study was conducted to investigate the in-vitro lipid-lowering properties of ‘Saba’ banana peel pectin (SBP) extracted using three methods for its possible use as a dietary fibre ingredient. Methods: Pectin from ‘Saba’ banana peels were extracted using acid extraction (citric acid), enzymatic extraction (cellulase), and microwave-assisted extraction. In-vitro lipid-lowering assays were performed using spectrophotometry for pancreatic lipase inhibition and cholesterol binding, while liquid chromatography was used for bile acid-binding capacity. Results: Results revealed that all SBPs were not able to inhibit pancreatic lipase activity. However, all SBPs can notably bind to cholesterol and bile acids, taurocholate, and glycocholate. Acid-extracted pectin had the highest binding capacity to cholesterol (51.36%–55.07%) and glycocholate (27.37%), whereas all SBPs were similarly bound to taurocholate. Conclusion: The results of this study showed that acidextracted SBPs can significantly bind to cholesterol and bile acids, glycocholate and taurocholate, thereby indicating a possible reduction in lipid metabolism.

Discovery of human pancreatic lipase inhibitors from root of Rhodiola crenulata via integrating bioactivity-guided fractionation,chemical profiling and biochemical assay / 药物分析学报

Although herbal medicines(HMs)are widely used in the prevention and treatment of obesity and obesity-associated disorders,the key constituents exhibiting anti-obesity activity and their molecular mechanisms are poorly understood.Recently,we assessed the inhibitory potentials of several HMs against human pancreatic lipase(hPL,a key therapeutic target for human obesity),among which the root-extract of Rhodiola crenulata(ERC)showed the most potent anti-hPL activity.In this study,we adopted an integrated strategy,involving bioactivity-guided fractionation techniques,chemical profiling,and biochemical assays,to identify the key anti-hPL constituents in ERC.Nine ERC fractions(retention time=12.5-35 min),obtained using reverse-phase liquid chromatography,showed strong anti-hPL activity,while the major constituents in these bioactive fractions were subsequently identified using liquid chromatography-quadrupole time-of-flight mass spectrometry(LC-Q-TOF-MS/MS).Among the identified ERC constituents,1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose(PGG)and catechin gallate(CG)showed the most potent anti-hPL activity,with pIC50 values of 7.59±0.03 and 7.68±0.23,respectively.Further investigations revealed that PGG and CG potently inhibited hPL in a non-competitive manner,with inhibition constant(Ki)values of 0.012 and 0.082 μM,respectively.Collectively,our integrative analyses enabled us to efficiently identify and characterize the key anti-obesity constituents in ERC,as well as to elucidate their anti-hPL mechanisms.These findings provide convincing evidence in support of the anti-obesity and lipid-lowering properties of ERC.

Inhibition of α-glucosidase, pancreatic lipase, and antioxidant property of Myrcia hatschbachii D. Legrand containing gallic and ellagic acids / Inhibición de la α-glucosidasa, la lipasa pancreática y la propiedad antioxidante de Myrcia hatschbachii D. Legrand que contiene ácidos gálico y elágico

Several species of the Myrcia genus have been used in folk medicine to treat diabetes. Therefore, the aim of this work was to investigate the inhibitory activity of α-glucosidase and pancreatic lipase in the crude extract (EBF) and in the ethyl acetate fraction (FFA) of Myrcia hatschbachii, as well as to identify isolated phenolic compounds and to evaluate the antioxidant property and preliminary in vitro toxicity against Artemia salina. EBF (IC50: 3.21 µg/mL) and FFA (IC50: 1.14 µg/mL) showed inhibitory activity superior to acarbose (IC50: 193.65 µg/mL). In addition, they showed inhibitory effects of pancreatic lipase (IC50: 556.58 µg/mL for EBF and 532.68 µg/mL for FFA), antioxidant potential, absence of preliminary toxicity and presence of gallic andellagic acids in FFA. The relevant results in the inhibition of α-glucosidase and pancreatic lipase motivate new studies for the development of herbal medicines that assist in the treatment of diabetic patients.

Varias especies del género Myrcia se han utilizado en la medicina popular para tratar la diabetes. Por lo tanto, el objetivo de este trabajo fue investigar la actividad inhibitoria de la α-glucosidasa y la lipasa pancreática en el extracto crudo (EBF) y en la fracción de acetato de etilo (FFA) de Myrcia hatschbachii, así como identificar compuestos fenólicos aislados y evaluar la propiedad antioxidante y toxicidad in vitro preliminar contra Artemia salina. EBF (IC50: 3.21 µg/mL) y FFA (IC50: 1.14 µg/mL) mostraron una actividad inhibitoria superior a la acarbosa (IC50: 193.65 µg/mL). Además, mostraron efectos inhibitorios de la lipasa pancreática (IC50: 556.58 µg/mL para EBF y 532.68 µg/mL para FFA), potencial antioxidante, ausencia de toxicidad preliminar y presencia de ácidos gálico y elágico en FFA. Los resultados relevantes en la inhibición de la α-glucosidasa y la lipasa pancreática motivan nuevos estudios para el desarrollo de medicamentos a base de hierbas que ayudan en el tratamiento de pacientes diabéticos.

Predisposition to acute pancreatitis in dogs with severe acute renal failure / Predisposição à pancreatite aguda em cães com insuficiência renal aguda grave

Patients with acute renal failure often have a negative energy balance, which promotes metabolic changes predisposing to complications. The objective of this study was to evaluate laboratory parameters of 30 dogs with severe acute renal failure, to assess their relationship with the possibility of developing acute pancreatitis due to the negative energy balance, and to correlate these findings with the degree of renal failure. Serum concentrations of urea, creatinine, beta-hydroxybutyrate, triglycerides, amylase, total lipase, and canine pancreatic lipase were compared between healthy dogs and dogs with severe acute renal failure. A greater serum concentration of beta-hydroxybutyrate and greater activity of pancreatic enzymes, particularly canine pancreatic lipase, as well as a stronger correlation between the latter and serum creatinine concentrations, were related to the occurrence of acute pancreatitis in patients with severe acute renal failure. A greater degree of renal failure implied a greater predisposition to acute pancreatitis.(AU)

O portador de insuficiência renal aguda é um paciente que, muitas vezes, encontra-se sob importante condição de balanço energético negativo, gerando alterações metabólicas que predispõem a complicações. O objetivo deste estudo foi avaliar parâmetros laboratoriais de trinta cães com insuficiência renal aguda grave, quanto a possibilidade de desenvolvimento de pancreatite aguda em função do balanço energético negativo, e relacioná-los ao grau de gravidade da insuficiência renal. As concentrações séricas de ureia, creatinina, betahidroxibutirato, triglicérides, amilase, lipase total e lipase pancreática canina foram comparadas entre o grupo de cães hígidos e o de cães doentes. Observou-se maior concentração sérica de betahidroxibutirato e maior atividade das enzimas pancreáticas, especialmente da lipase pancreática canina, além de forte correlação entre esta última e a concentração sérica de creatinina, demonstrando a ocorrência de pancreatite aguda em pacientes com insuficiência renal aguda grave. Verificou-se também que quanto mais grave é a insuficiência renal, maior é a predisposição à pancreatite aguda.(AU)

Predisposition to acute pancreatitis in dogs with severe acute renal failure

ABSTRACT: Patients with acute renal failure often have a negative energy balance, which promotes metabolic changes predisposing to complications. The objective of this study was to evaluate laboratory parameters of 30 dogs with severe acute renal failure, to assess their relationship with the possibility of developing acute pancreatitis due to the negative energy balance, and to correlate these findings with the degree of renal failure. Serum concentrations of urea, creatinine, beta-hydroxybutyrate, triglycerides, amylase, total lipase, and canine pancreatic lipase were compared between healthy dogs and dogs with severe acute renal failure. A greater serum concentration of beta-hydroxybutyrate and greater activity of pancreatic enzymes, particularly canine pancreatic lipase, as well as a stronger correlation between the latter and serum creatinine concentrations, were related to the occurrence of acute pancreatitis in patients with severe acute renal failure. A greater degree of renal failure implied a greater predisposition to acute pancreatitis.

RESUMO: O portador de insuficiência renal aguda é um paciente que, muitas vezes, encontra-se sob importante condição de balanço energético negativo, gerando alterações metabólicas que predispõem a complicações. O objetivo deste estudo foi avaliar parâmetros laboratoriais de trinta cães com insuficiência renal aguda grave, quanto a possibilidade de desenvolvimento de pancreatite aguda em função do balanço energético negativo, e relacioná-los ao grau de gravidade da insuficiência renal. As concentrações séricas de ureia, creatinina, betahidroxibutirato, triglicérides, amilase, lipase total e lipase pancreática canina foram comparadas entre o grupo de cães hígidos e o de cães doentes. Observou-se maior concentração sérica de betahidroxibutirato e maior atividade das enzimas pancreáticas, especialmente da lipase pancreática canina, além de forte correlação entre esta última e a concentração sérica de creatinina, demonstrando a ocorrência de pancreatite aguda em pacientes com insuficiência renal aguda grave. Verificou-se também que quanto mais grave é a insuficiência renal, maior é a predisposição à pancreatite aguda.

Phytochemical Analysis & In-Vitro Anti Obesity Activity Of Different Fractions Of Methanolic Extract Of Fagonia Cretica L.

Obesity is one of the most prevalent health concerns among all age groups & populations worldwide, resulting into a significant increase in mortality and morbidity related to metabolic disorders. Targeting one or more enzymes involved in lipid metabolism can be selective for evaluation of anti obesity action of drug. The present study was aimed to evaluate in vitro anti obesity action by inhibiting pancreatic lipase & ᾳ amylase enzyme by various fractions of methanolic extract of aerial parts Fagonia cretica L. along with their phytochemical analysis. The n- hexane (HFFC), Chloroform (CFFC), Ethyl acetate (EAFFC), n-butanol (BFFC) & aqueous fractions (AQFFC) were prepared from methanolic extracts of F. cretica L & were analyzed for qualitative as well as quantitative phytochemical study using reported methods. The qualitative phytochemical studies of prepared extract & fractions showed presence of flavonoids, saponins, phenolics, alkaloids & carbohydrates. All the fractions were then examined for their in-vitro lipase inhibitory & ᾳ amylase inhibitory activities at a concentration level of 50, 100, 150 & 200µg/ml and their percentage inhibitory effects were reported. Among the analyzed samples, BFFC showed highest lipase inhibitory action i.e. 83.02 ± 2.47% as compared to other fractions. EAFFC showed significantly higher ᾳ amylase inhibitory action i.e. 80.22 ± 1.18% as compared to other fractions.

Three new polyoxygenated bergamotanes from the endophytic fungus Penicillium purpurogenum IMM 003 and their inhibitory activity against pancreatic lipase / 中国天然药物

Purpurolides D-F (1-3), three new polyoxygenated bergamotanes bearing a 6/4/5/5 tetracyclic ring system, were isolated from the endophytic fungus Penicillium purpurogenum IMM 003. Their structures were unambiguously elucidated based on extensive spectroscopic data analyses, C NMR chemical shifts calculations coupled with the DP4+ probability method, and the calculated and experimental electronic circular dichroism (ECD) spectra. Compounds 1-3 showed significant inhibitory activity against pancreatic lipase (PL). The result highlights that the presence of 3-hydroxylated decanoic acid moiety at C-14 is important for increasing the inhibition potency against PL.

Pancreatic lipase inhibitory constituents from Fructus Psoraleae / 中国天然药物

Pancreatic lipase (PL), a crucial enzyme in the digestive system of mammals, has been proven as a therapeutic target to prevent and treat obesity. The purpose of this study is to evaluate and characterize the PL inhibition activities of the major constituents from Fructus Psoraleae (FP), one of the most frequently used Chinese herbs with lipid-lowering activity. To this end, a total of eleven major constituents isolated from Fructus Psoraleae have been obtained and their inhibition potentials against PL have been assayed by a fluorescence-based assay. Among all tested compounds, isobavachalcone, bavachalcone and corylifol A displayed strong inhibition on PL (IC < 10 μmol·L). Inhibition kinetic analyses demonstrated that isobavachalcone, bavachalcone and corylifol A acted as mixed inhibitors against PL-mediated 4-methylumbelliferyl oleate (4-MUO) hydrolysis, with the K values of 1.61, 3.77 and 10.16 μmol·L, respectively. Furthermore, docking simulations indicated that two chalcones (isobavachalcone and bavachalcone) could interact with the key residues located in the catalytic cavity of PL via hydrogen binding and hydrophobic interactions. Collectively, these finding provided solid evidence to support that Fructus Psoraleae contained bioactive compounds with lipid-lowering effects via targeting PL, and also suggested that the chalcones in Fructus Psoraleae could be used as ideal leading compounds to develop novel PL inhibitors.

Recent advances on pancreatic lipase inhibitors from Chinese herbs / 药学学报

Obesity is an important cause of a panel of metabolic diseases, such as hypertension, hyperlipidemia, arteriosclerosis, type 2 diabetes and various cancers. Discovery of anti-obesity agents has always been a hot spot in the field of new drug research and development. Pancreatic lipase (PL, also named triacylglycerol acyl hydrolase), a key enzyme responsible for the hydrolysis of 50%-70% dietary fats in the gastrointestinal system, which has been recognized as a crucial target for the prevention and treatment of obesity. PL inhibitors can reduce the decomposition and absorption of dietary fat in the digestive organs by decreasing the hydrolytic activity of this key enzyme, which can alleviate the symptoms of metabolic diseases such as obesity and hyperlipidemia. Although a potent PL inhibitor (orlistat) has been marketed, it may trigger gastrointestinal side effects after long-term use. Therefore, it is necessary to develop more new PL inhibitors with strong inhibition potency and safety. In recent years, a large number of studies have found that some Chinese herbal extracts and their constituents can regulate lipid metabolism and treat obesity via inhibiting PL. In this paper, the research progress in the field pancreatic lipase inhibitors, as well as the extracts of Chinese herbs and their constituents with pancreatic lipase inhibitory effects were summarized. Meanwhile, the PL inhibition activities and inhibitory mechanisms of herbal constitutes were also summarized systematically. In addition, the authors also highlight the challenges in this field and the future research directions. All information and knowledge presented in this review will be very helpful for the medicinal chemists to find more potent PL inhibitors from herbs or to develop next generation anti-obesity drugs, as well as helpful for the prevention and treatment of obesity and other related metabolic diseases using herba medicines or related products.

Characterization of ethyl acetate and methanol extracts of Commiphora myrrha and evaluating in vitro anti-diabetic and anti-obesity activities

Diabetes mellitus is a clinical disease categorized by hyperglycemia. Reduction of gastrointestinal glucose absorptionthrough the inhibition of carbohydrate digesting enzymes is one of in vitro anti-diabetic therapeutic approach. Thisinvestigation aimed to estimate the in vitro anti-diabetic and anti-obesity activities for ethyl acetate and methanolextracts of Commiphora myrrha oleo-gum as well as the identification of the bioactive compounds. Commiphoramyrrha was extracted with methanol and ethyl acetate. The two extracts were used to evaluate their α-glucosidase,α-amylase, and pancreatic lipase inhibitory activities. Identification of the bioactive compounds of ethyl acetate wasanalyzed by GC-MS (gas chromatography-mass spectrometry). The results showed that the ethyl acetate extract hada stronger inhibition activity on α-amylase (IC50 = 54.60 µg/ml) and α-glucosidase (IC50 = 58.7 µg/ml) than methanolextract on α-amylase (IC50 = 124.01 µg/ml) and α-glucosidase (IC50 = 191.2 µg/ml). Also, ethyl acetate extract hada promising inhibitory effect on pancreatic lipase (IC50 = 107.8 µg/ml) than methanol extract (IC50 = 498.1 µg/ml).GC-MS analysis of ethyl acetate extract identified 31 compounds. Among them nobiletin (50.26%), metaproterenol(orciprenaline) (14.99%), morantel (8.86%), and tricetin (3.38%) were the main compounds. These findings provedthat C. myrrha has anti-diabetic and anti-obesity inhibition activity may be due to the bioactive compounds withinteresting medicinal properties.

Screening, identification and activity evaluation of pancreatic lipase inhibition in Prunella vulgaris / 中国中药杂志

Pancreatic lipase (PL) inhibitors were firstly screened from Prunella vulgaris with PL immobilized on carboxylic acid-terminated magnetic nanoparticles, then these possible inhibitors were identified by LC-MS/MS and mixed standards. Finally, their inhibitory effects and types on PL were tested by p-nitrophenol method. The results showed that four PL inhibitors were screened out from P. vulgaris and confirmed by LC-MS/MS and mixed standards. The IC₅₈ and inhibition types were as follows: caffeic acid [(252.3±3.6) mg·L⁻¹, anti-competitive inhibition], rutin [(91.2±1.6)mg·L⁻¹, competitive inhibition], hesperidin [(31.5±4.4) mg·L⁻¹, competitive inhibition] and ursolic acid [(41.3±2.2) mg·L⁻¹, competitive inhibition]. Their inhibitive types and abilities on PL were related to their molecular size, hydrophobicity and the number of hydrogen bond with PL triplet.

Platycodi radix beverage ameliorates postprandial lipemia response through lipid clearance of triglyceride-rich lipoprotein: A randomized controlled study in healthy subjects with a high-fat load

BACKGROUND/OBJECTIVES: Elevation of postprandial lipemia characterized by a rise in triglyceride (TG)-rich lipoproteins can increase the risk of atherogenesis. The objective of this study was to investigate postprandial lipemia response to a single dietary fat/sugar load test and monitor beneficial changes induced by the consumption of Platycodi radix (AP) beverage in healthy subjects. SUBJECTS/METHODS: A total of 52 subjects were randomly assigned to either placebo or AP beverage group with a high-fat shake in a randomized controlled crossover trial. Postprandial blood was collected at 0, 1, 2, 4, and 6 h and analyzed for TG and lipoprotein lipase mass. Inhibition of pancreatic lipase was determined in vitro. RESULTS: AP inhibited pancreatic lipase activity in vitro (IC₅₀ = 5 mg/mL). Compared to placebo beverage, AP beverage consumption with a high-fat shake induced significant increase of plasma lipoprotein lipase mass (P = 0.0111, β estimate = 4.2948) with significant reduction in very low-density lipoprotein (VLDL) TG concentration (P = 0.038, β estimate = −52.69) at 6 h. Based on significant correlation between high-fat dietary scores MEDFICTS and postprandial TG responses in VLDL (P = 0.0395, r = 0.2127), subgroup analysis revealed that 6 h-postprandial VLDL TG response was significantly decreased by AP consumption in subjects with MEDFICTS ≥ 40 (P = 0.0291, β estimate = −7214). CONCLUSIONS: AP beverage might have potential to alleviate postprandial lipemia through inhibiting pancreatic lipase activity and elevating lipoprotein lipase mass. Subgroup analysis revealed that subjects with high-fat dietary pattern could be classified as responders to AP beverage among all subjects.

Bioactivity and Chemical Constituents of Different Polar Parts from Blueberry Leaves / 中国药学杂志

OBJECTIVE: To study the bioactivity and chemical constituents of different polar parts from blueberry leaves. METHODS: Blueberry leaves were extracted by ethanol and then the extract was sequentially partitioned into five fractions. Silicagel and Sephadex LH-20 chromatographic methods were applied to isolate and purify compounds. Their structures were elucidated by physiochemical properties and spectral analysis.The DPPH• radical scavenging activity, α-glycosidase and pancreatic lipase inhibition activity of different polar parts and partial compounds were determined. RESULTS: The n-butyl alcohol fraction(BF) showed the highest DPPH• radical scavenging activity and α-glycosidase inhibition activity. The ethyl acetate fraction(EAF) showed the strongest pancreatic lipase inhibition activity. A total of five compounds were isolated from the EAF, and their structures were identified as β-sitosterol(1), quercetin-3-O-α-L-arabinofuranoside(2), quercetin(3), quercetin-3-O-β-D-glucopyranoside(4) and 1-O-caffeoylquinic acid(5). A total of two compounds were isolated from the BF, and their structures were identified as quercetin-3-O-α-L-arabinoside(6) and quercetin-3-O-β-D-glucuronide(7). The results showed that compounds 3 and 5 had very good DPPH• radical scavenging and pancreatic lipase inhibitory activity, and compounds 1 and 3 had good α-glucosidase inhibitory activity. CONCLUSION: The different polar parts and compounds of blueberry leaves show strong DPPH• radical scavenging activity, α-glycosidase and pancreatic lipase inhibition activity. Compounds 1, 2, 5 and 6 are isolated from blueberry leaves for the first time.

α-Glucosidase and pancreatic lipase inhibitory activities and glucose uptake stimulatory effect of phenolic compounds from Dendrobium formosum

ABSTRACT A methanol extract from the whole plant of Dendrobium formosum Roxb. ex Lindl., Orchidaceae, showed inhibitory potential against α-glucosidase and pancreatic lipase enzymes. Chromatographic separation of the extract resulted in the isolation of twelve phenolic compounds. The structures of these compounds were determined through analysis of NMR and HR-ESI-MS data. All of the isolates were evaluated for their α-glucosidase and pancreatic lipase inhibitory activities, as well as glucose uptake stimulatory effect. Among the isolates, 5-methoxy-7-hydroxy-9,10-dihydro-1,4-phenanthrenequinone (12) showed the highest α-glucosidase and pancreatic lipase inhibitory effects with an IC50 values of 126.88 ± 0.66 µM and 69.45 ± 10.14 µM, respectively. An enzyme kinetics study was conducted by the Lineweaver-Burk plot method. The kinetics studies revealed that compound 12 was a non-competitive inhibitor of α-glucosidase and pancreatic lipase enzymes. Moreover, lusianthridin at 1 and 10 µg/ml and moscatilin at 100 µg/ml showed glucose uptake stimulatory effect without toxicity on L6 myotubes. This study is the first report on the phytochemical constituents and anti-diabetic and anti-obesity activities of D. formosum.

Pancreatic Lipase Inhibitor from Food Plant: Potential Molecule for Development of Safe Anti-obesity Drug.

Obesity is a global health concern, widely recognized as the largest and fastest growing public health problem in the developed and developing countries associated with high morbidity and mortality. It is a multifactorial disease resulting in significant impairment of health. The strategies used for the treatment of obesity generally comprise of prescription of drugs and surgery. Number of basic mechanisms has been considered for obesity management but these entail serious complexities. In recent year’s pancreatic lipase, a principal lipolytic enzyme secreted by the pancreas has gained importance as -obesity target. As the PL acts in the duodenum it has least involvement with the blood or brain, avoiding a lot of drug related side effects. Although PL has been considered as good target for obesity management, the drug discovery and development in this section is not abundantly explored. Numerous natural molecules have been established for pancreatic lipase inhibitory activity but only orlistat (tetrahydrolipstatin), a saturated derivative of lipstatin designed to inhibit the action of gastrointestinal lipase approved by Food and Drug Administration (FDA) for longterm usage. However, it has severe side effects. Therefore, the possible treatment of obesity using natural products is an extensive field to be explored. Several plant derived molecules including medicinal plants have been reported for their pancreatic lipase inhibitory activity. In particular pancreatic lipase inhibitor from food plants can be considered as a good source for the discovery of a safe anti-obesity agent due to possible active principle as edible component. Present review mainly focuses on the pancreatic lipase inhibitor from food plants and its potential in the development of safe anti-obesity drug.

Synthesis and evaluation of benzylisoquinoline derivatives for their inhibition on pancreatic lipase and preadipocyte proliferation / 中国天然药物

The present study was designed to synthesize and evaluate a series of benzylisoquinoline derivatives. These compounds were synthesized by Bischler-Napieralski cyclization to yield 1-benzyl-3,4-dihydroisoquinolines, and the products were obtained by reductions. All these compounds were identified by MS, (1)H NMR and (13)C NMR. The inhibitory activities on pancreatic lipase and preadipocyte proliferation for the synthesized compounds and alkaloids from Nulembo nucifera were assessed in vitro. Most of the compounds showed inhibitory activities on both pancreatic lipase and preadipocyte proliferation. Particularly, compounds 7p-7u and 9d-9f exhibited significant inhibitory activity on pancreatic lipase while compounds 7c, 7d, 7f, 7g, 7i, and 7j potently inhibited the proliferation of 3T3-L1 preadipocytes. Our results provided a basis for future evaluation and development of these compounds as leads for therapeutics for human diseases.

Screening for anti-pancreatic lipase properties of 28 traditional Thai medicinal herbs

Objective: To screen the effect of 28 medicinal plants on inhibition of pancreatic lipase and evaluate the phytochemical contents of extracts. Methods: The ethanolic extracts of 28 traditional Thai herbal medicines were assayed for their in vitro activities against porcine pancreatic lipase using p-nitrophenyl butyrate as a substrate. Quantitative estimation of flavonoids, phenolics, and alkaloids was done. Results: Extracts from four herbs, Memecylon edule Roxb., Garcinia vilersiana Pierre, Cryptolepis elegans Wall. and Phyllanthus chamaepeuce Ridl., at a concentration of 100 mg/mL, strongly inhibited porcine pancreatic lipase by 90.97%, 92.04%, 94.64%and 95.38%, respectively. There was a significant positive correlation between phenolic content and inhibition activity. Inhibition activity was significantly correlated with flavonoid and with alkaloid contents. Conclusions: From this result, it could be concluded that herbs represent a rich of anti-pancreatic lipase compounds, in particular, Cryptolepis elegans Wall. and Phyllanthus chamaepeuce Ridl. It is suggested that the phytochemical compounds from these plants may be applied for the prevention and treatment of obesity or hyperlipidemia.

Screening for anti-pancreatic lipase properties of 28 traditional Thai medicinal herbs

Objective: To screen the effect of 28 medicinal plants on inhibition of pancreatic lipase and evaluate the phytochemical contents of extracts. Methods: The ethanolic extracts of 28 traditional Thai herbal medicines were assayed for their in vitro activities against porcine pancreatic lipase using p-nitrophenyl butyrate as a substrate. Quantitative estimation of flavonoids, phenolics, and alkaloids was done. Results: Extracts from four herbs, Memecylon edule Roxb., Garcinia vilersiana Pierre, Cryptolepis elegans Wall. and Phyllanthus chamaepeuce Ridl., at a concentration of 100 μg/mL, strongly inhibited porcine pancreatic lipase by 90.97%, 92.04%, 94.64% and 95.38%, respectively. There was a significant positive correlation between phenolic content and inhibition activity. Inhibition activity was significantly correlated with flavonoid and with alkaloid contents. Conclusions: From this result, it could be concluded that herbs represent a rich of anti-pancreatic lipase compounds, in particular, Cryptolepis elegans Wall. and Phyllanthus chamaepeuce Ridl. It is suggested that the phytochemical compounds from these plants may be applied for the prevention and treatment of obesity or hyperlipidemia.

Actividad de las Enzimas Tripsina y Lipasa Pancreáticas en Cerdos Alimentados con Harina de Pijiguao (Bactris gasipaes H.B.K.) y Lisina Sintética / Trypsin and Lipase Pancreatic Enzymes Activity in Pigs Fed with Pijiguao Meal (Bactris gasipaes H.B.K.) and Synthetic Lysine

Para determinar la actividad de las enzimas tripsina y lipasa pancreática de cerdos alimentados con harina de pijiguao (Bactris gasipaes H.B.K., HP) y lisina sintética (LS), se diseñó un experimento con 48 cerdos castrados, con peso vivo promedio de 30 ± 0,5 kg, distribuidos al azar en seis diferentes dietas experimentales, con un arreglo factorial 3 x 2, con tres niveles de HP (0, 16 y 32 %), con o sin adición de 0,27% de LS; con cuatro repeticiones por dieta y dos cerdos por unidad experimental. Se sacrificaron cuatro cerdos por dieta en la tercera y sexta semana, para obtener muestras de páncreas. No se observó efecto de dieta (HPxLS) sobre la actividad de las enzimas, pero si hubo efecto (P<0,05) de la interacción dieta x semana sobre la actividad de la tripsina y lipasa. No hubo diferencias significativas en la actividad de la tripsina en la tercera semana después del consumo de las dietas. En la sexta semana todas las dietas, excepto la que contenía 0,27% LS y 16% HP, mostraron menor (P<0,05) actividad de la tripsina que la dieta basal. La actividad de la lipasa pancreática fue mayor (P<0,05) en los cerdos que consumieron la dieta con 32% HP sin LS en la tercera semana; y en la sexta semana, la actividad fue menor (P<0,05) en los cerdos cuyas dietas contenían 16% HP con y sin la adición de 0,27% LS, en comparación con la dieta basal y la que contenía 32% HP sin LS. En conclusión, la HP y/o LS en dietas para cerdos en crecimiento afecta la actividad de las enzimas tripsina y lipasa pancreáticas luego de la sexta semana de consumo.

An experiment was conducted to determine the activities of trypsin and lipase pancreatic enzymes from growing pigs fed peach palm meal (Bactris gasipaes H.B.K.; PPM) and synthetic lysine (SL). Forty-eight barrows, with an average live weight of 30 ± 0 5 kg, were randomly distributed and allotted to six experimental diets in a 3x2 factorial arrangement of treatments, with three levels of PPM (0, 16 and 32 %), with or without the addition of 0.27% SL, with four replications per diet and two pigs per experimental unit. To collect pancreas samples, four pigs per diet were slaughtered at third and sixth weeks. The results of the assay showed no effect of diet (PPM xLS) on the activity of the enzymes. An effect (P <0.05) of the diet x week interaction on trypsin and lipase enzymatic activities was observed. There were no significant differences in the activity of trypsin in the third week, after consumption of diets. In the sixth week, all diets, except that containing 0.27 % of SL and 16 % of PPM, showed lower (P<0.05) trypsin activity than the basal diet. In the third week, the pancreatic lipase activity was greatest (P<0.05) in pigs fed the diet with 16% of PPM without SL; and in the sixth week, the activity was less (P<0.05) in pigs fed diets containing 32% of PPM with and without the addition of 0.27% of SL, when compared with the basal diet and that which contained 32% of PPM and/or SL. In summary, the PPM and/or SL diets affect the trypsin and pancreatic lipase activities after sixth weeks of consumption.

Chemical Composition and In vitro Studies of the Essential Oil and Aqueous Extract of Pelargonium graveolens Growing in Jordan for Hypoglycaemic and Hypolipidemic Properties.

Aims: This study aimed to analyze the chemical composition of essential oil of Pelargonium graveolens L. Her. ex Ait. growing in Jordan and to test the efficacy of the leaves aqueous extract and essential oil against pancreatic triacylglycerol lipase (PL), α- amylase and α-glucosidase. Study Design: GC-MS analysis of the essential oil obtained by hydrodistillation and Solid Phase Microextraction (SPME) methods as well as in vitro enzymatic investigations. Place and Duration of Study: Faculty of Pharmacy, The University of Jordan, between November 2012 and August 2013. Results: The hydrodistilled oil of P. graveolens fresh leaves yielded twenty eight components, accounting for 95.83 % of the total oil content, while thirty seven components were detected from the fresh leaves by SPME (98.86%). Twenty six and thirty one components were identified in the hydrodistilled and SPME oils of the dried leaves amounting to 96.08 % and 97.83 %, respectively. Oxygenated monoterpenes predominated the volatile fractions of the leaves of both methods with citronellol, citronellyl formate and menthone/isomenthone as the major constituents. Similar to orlistat (PL IC50 of 114.0 ± 4.0 ng/mL), P. graveolens extract and volatile oil as well as their purified phyto-constituents inhibited highly substantially in a dose dependent trend PL in vitro (n=3). The P. graveolens extract PL- IC50 was 207.4±15.2 μg/mL. As for their volatile oils’ components, PL- IC50 (%) (V/V) in an ascending order were: menthone; 0.01±0.0 <geraniol; 0.34±0.02 < linalool; 0.7 ± 0.0 < caryophyllene; 1.17±0.12 <P. graveolens oil; 2.93 ± 0.27. Comparable to acarbose, P. graveolens leaves aqueous extracts (AEs) were identified as in vitro potent and efficacious dual inhibitors of α- amylase and α-glucosidase with IC50: 4.6±0.1 mg/mL (p<0.001, n=3). Conclusion: Taken together, P. graveolens leaves, as a nutraceutical modulating gastrointestinal carbohydrate and lipid digestion and absorption, maybe advocated as candidate for obesity-diabetes/metabolic syndrome management.