Inhibitory effects of Piper umbellatum Linn. leaf extracts on α-amylase and α-glucosidase activities

Background@#Alpha-amylase and alpha-glucosidase are essential enzymes in converting food into energy inside the body. However, the proper management of these enzymes is needed to maintain normal blood glucose levels in the body. Thus, inhibiting these carbohydrate-hydrolyzing enzymes is necessary for managing hyperglycemia and alleviating Type 2 Diabetes Mellitus complications. Studies have reported that the Piper species have inhibitory properties on these digestive enzymes. However, the locally cultivated P. umbellatum has not yet been studied. @*Objectives@#The study evaluated the inhibitory potentials of the locally grown P. umbellatum leaf extracts against α-amylase and α-gluiosidase. @*Methodology@#The P. umbellatum leaf extracts were screened for in vitro inhibitory α-amylase and α-glucosidase tests. The most active crude extract was subjected to semi-purification and fractions were subjected to inhibitory enzymatic tests. Qualitative and quantitative phytochemical analyses were conducted. @*Results@#Among all crude extracts, the KMB-HE exhibited the highest activities comparable to that of the acarbose standard (p>0.05). The KMB-HE showed inhibitions of 81.01%±1.66 and 89.51%±3.03 on α-amylase and α-glucosidase at 250 μg/mL, respectively. In addition, it contained the highest phenolic (195.00 ±3.60 GAE mg/gram) and flavonoid (4.55±0.06 QE mg/gram) contents that may be linked to the observed activities. The semi-purification of KMB-HE collected 24 fractions with PF10 demonstrating inhibitions of 68.07%±13.48 and 74.21%±2.22 in α-amylase and α-glucosidase, respectively. Also, the PF10 contained the highest phenolic (204.75±2.42 GAE mg/gram) and flavonoid (4.00±0.07 QE mg/gram) compounds among all the active fractions tested. The PF10 satisfied the recommended criteria for plant natural inhibitors: a moderate-to-low α-amylase and stronger α-glucosidase inhibitory activity. @*Conclusion@#The P. umbellatum exhibited good inhibitory activities on carbohydrate-hydrolyzing enzymes. These may lead to further analysis of the P. umbellatum for future development of a safer, locally available natural remedy in managing Type 2 Diabetes Mellitus.

Anti-inflammatory activity of Piper umbellatum Linn. leaf extracts

Background@#Earlier studies reported the anti-inflammatory activity in several species of Piper, and Piper umbellatum Linn. leaves containing some phytochemicals that are potent anti-inflammatory agents. However, there was no thorough investigation on the anti-inflammatory activity of the locally grown P. umbellatum in the Philippines. @*Objective@#The study aimed to determine the anti-inflammatory activity of Piper umbellatum leaves using in vitro and in vivo assays. @*Methodology@#Crude extracts were obtained from P. umbellatum leaves using polar and non-polar solvents. The anti-inflammatory activities of all crude extracts were determined using the carrageenan-induced paw edema test in mice and phytochemical analysis. The crude extract with the highest activity was partially purified using column chromatography. The fractions with similar TLC profile were pooled and tested for antiinflammatory activity. COX-1 and COX-2 enzyme inhibitory activity were determined in pooled fractions that showed initial activity in animal model. @*Results@#Among the crude extracts of P.umbellatum, the crude ethyl acetate extract exhibited a significant dose-dependent inhibition on paw edema test with doses of 500 mg/kg bw, 1,000 mg/kg bw and 1,500 mg/kg bw (p<0.05). Among the 20 pooled fractions (PF) collected from the ethyl acetate extract, PF58, PF60 and PF64 had the highest COX-2 enzyme inhibitions of 83.12 %, 84.78% and 77.47%, respectively (p<0.05). PF60 also exhibited the highest anti-inflammatory activity on paw edema with inhibitions of 62.45% at low dose (250 mg/kg bw) and 76.10 % at high dose (1,000 mg/kg bw) in mice. @*Conclusion@#The ethyl acetate extract of P. umbellatum leaves and its fraction-PF60 exhibited a significant anti-inflammatory activity in in vitro and in vivo assays and contained high amounts of total phenolic and total flavonoid.

Antidiabetic potential of methanol extracts from leaves of Piper umbellatum L. and Persea americana Mill

Objective: To determine inhibitory activity of methanolic leaf extract of Piper umbellatum and Persea americana (P. americana) (traditionally used in Cameroon against diabetes) on α-glucosidase, β-glucosidase, maltase-glucoamylase, aldose reductase and aldehyde reductase activities, enzymes involved in starch digestion or diabetic complications. Methods: The methanol extracts from Piper umbellatum and P. americana were prepared by maceration. To assess relative efficacy of these extracts, the determination of concentrations that were needed to inhibit 50% of enzyme activity was done, whereas, gas chromatography-mass spectrum was used to identify components from extracts that may be responsible for the activities. Results: The tested extracts strongly inhibited α-glucosidase, maltase-glucoamylase, aldose reductase and aldehyde reductase activities with IC

Antidiabetic potential of methanol extracts from leaves of Piper umbellatum L.and Persea americana Mill

Objective:To determine inhibitory activity of methanolic leaf extract of Piper umbellatum and Persea americana (P.americana) (traditionally used in Cameroon against diabetes) on α-glucosidase,β-glucosidase,maltase-gluconmylase,aldose reductase and aldehyde reductase activities,enzymes involved in starch digestion or diabetic complications.Methods:The methanol extracts from Piper umbellatum and P.americana were prepared by maceration.To assess relative efficacy of these extracts,the determination of concentrations that were needed to inhibit 50％ of enzyme activity was done,whereas,gas chromatography-mass spectrum was used to identify components from extracts that may be responsible for the activities.Resullts The tested extracts strongly inhibited α-glucosidase,maltase-glucoamylase,aldose reductase and aldehyde reductase activities with IC50 ranging from (1.07 ± 0.03) to 01.77 + 1.17) μg/mL.Among the tested extracts,P.americana was the most active against sensitive enzymes (IC50 of 1.07 ± 0.03 to 15.63 ± 1.23).But,none of the extracts showed interesting inhibitory effect against β-glucosidase as their percentage inhibitions were less than 16％.From gas chromatographymass spectrum analysis,10 and 8 compounds were identified in Piper umbellatum and P.americana extracts respectively,using NIST library 2014.Conclusions:Results of this study provide the scientific credential for a prospective usage of these plants to treat diabetes.

Farmacologia e fitoquímica de extratos e formulações de Jacaranda decurrens Cham., Jacaranda caroba (Vell.) DC. e Piper umbellatum L / Pharmacology and phytochemistry of extracts and formulations from Jacaranda decurrens Cham., Jacaranda caroba (Vell.) DC. and Piper umbellatum L

Jacaranda decurrens Cham., Jacaranda caroba (Vell.) DC. e Piper umbellatum L. são plantas nativas do Brasil, presentes no estado de São Paulo, com relatos de uso popular para atividade antiúlcera. Este trabalho teve como objetivo avaliar a atividade antiúlcera de J. caroba, J. decurrens e formulações de nanocápsulas contendo P. umbellatum. Também pretendeu-se caracterizar a fitoquímica de tais formulações e extratos. Adicionalmente, foi avaliada a toxicidade aguda e subaguda de J. caroba. Os extratos de Jacaranda apresentaram compostos fenólicos em seus perfis cromatográficos obtidos por CCD e CLAE, característicos para cada espécie. Os diferentes extratos de J. caroba variaram sua composição química conforme a procedência e idade da planta. As espécies J. decurrens e J. caroba de três diferentes regiões não apresentaram ação antiúlcera aguda em ratos em modelo de indução por etanol acidificado, embora o extrato e as frações de J. caroba apresentaram potencial atividade anti Helicobacter pylori, com CIM variando entre 125 e 1.000 µg/mL. O extrato de J. caroba não promoveu sintomas de toxicidade aguda e subaguda em ratos. A DL50 observada foi maior que 5.000 mg/kg. Não foram relatadas alterações significativas na aparência macroscópica e peso dos órgãos, porém houve indicação de atividade mutagênica em teste de Ames na linhagem TA98 de S. typhimurium, o qual apresentou uma tendência dose-resposta para concentrações entre 7,5 e 15,0 mg/placa após ativação metabólica (S9). A formulação de nanocápsulas de poli-ε- caprolactona com extrato de P. umbellatum apresentou partículas com diâmetro médio de 181,6 ± 0,9 nm e potencial zeta de -31 ± 4 mV. Através de análise por CLAE observou-se maior eficiência de encapsulamento para a porção mais apolar da fração, enquanto que os compostos mais polares ficaram dispersos no meio. As nanocápsulas poliméricas apresentaram atividade gastroprotetora mesmo sem a adição de ativos e tiveram sua atividade aumentada pela fração clorofórmica de P. umbellatum

Jacaranda decurrens Cham., Jacaranda caroba (Vell.) DC. and Piper umbellatum L. are native plants in Brazil, present in the state of São Paulo, with popular usage reports for anti-ulcer activity. This study aimed to evaluate the anti-ulcer activity of J. caroba, J. decurrens and nanocapsules formulations containing P. umbellatum. Also, we intended to characterize the phytochemistry of such formulations and extracts. Additionally, we evaluated the acute and subacute toxicity of J. caroba. Extracts from Jacaranda presented phenolic compounds in their chromatographic profiles obtained by TLC and HPLC, with variations between species. Samples of J. caroba extracts showed different chemical composition according to the origin and age of the plant. The species J. decurrens and J. caroba from three different regions showed no acute anti-ulcer action when tested in rats by acidified ethanol induction model. However, extract and fractions from J. caroba showed potential anti Helicobacter pylori activity, with MIC ranging from 125 and 1,000 ug/mL. J. caroba extract did not cause symptoms of acute and subacute toxicity in rats. The DL50 was determined above 5,000 mg/kg. Also, there were no significant changes to the macroscopic appearance of organs or changes in their weights. Meanwhile, an indication of mutagenic activity was observed in the Ames test. The TA98 strain of S. typhimurium, showed a tendency of dose-response for concentrations between 7.5 and 15.0 mg/plate after metabolic activation (S9). The nanocapsules formulation of poly-ε-caprolactone containing P. umbellatum extract had an average particle diameter of 181.6 ± 0.9 nm and zeta potential of -31 ± 4 mV. HPLC analysis showed better entrapping efficiency for the more apolar portion of the fraction, while the more polar compounds were dispersed in the medium. The polymeric nanocapsules showed gastroprotective activity even without the addition of active molecules and had their activity increased by chloroform fraction of P. umbellatum