Background Brucea javanica (B. javanica) seeds, also known as “Melada pahit” in Indo-Malay region are traditionally used to treat diabetes. The objective of this study was to determine antidiabetic, antioxidant and anti-inflammatory effects of B. javanica seeds on nicotinamide (NA)-streptozotocin (STZ) induced type 2 diabetic (T2D) rats and to analyze its chemical composition that correlate with their pharmacological activities.MethodsA hydroethanolic extract of B. javanica seeds was fractionated with n-hexane, chloroform and ethyl acetate. An active fraction was selected after screening for its ability to inhibit α-glucosidase and glycogen phosphorylase α (GP-α). Isolation and characterization were carried out by using column chromatography, NMR and LCMS/MS. All isolates were assayed for inhibition of GP-α and α-glucosidase. Antidiabetic effect of active fraction was further evaluated in T2D rat model. Blood glucose and body weight were measured weekly. Serum insulin, lipid profile, renal function, liver glycogen and biomarkers of oxidative stress and inflammation were analyzed after 4-week treatment and compared with standard drug glibenclamide.ResultsEthyl acetate fraction (EAF) exerted good inhibitory potential for α-glucosidase and GP-α compared with other fractions. Chromatographic isolation of the EAF led to the identification of seven compounds: vanillic acid (1), bruceine D (2), bruceine E (3), parahydroxybenzoic acid (4), luteolin (5), protocatechuic acid (6), and gallic acid (7). Among them, Compound (5) was identified as the most potent inhibitor of GP-α and α-glucosidase and its GP-α inhibitory activity (IC50 = 45.08 μM) was 10-fold higher than that of caffeine (IC50 = 457.34 μM), and α-glucosidase inhibitory activity (IC50 = 26.41 μM) was 5.5-fold higher than that of acarbose (IC50 = 145.83 μM), respectively. Compounds (4), (6), and (7) inhibited GP-α activity in a concentration-dependent manner with IC50 values of 357.88, 297.37, and 214.38 μM, and their inhibitory effect was higher than that of caffeine. These compounds exhibited weak potency on α-glucosidase compared with acarbose. Compounds (1), (2), and (3) showed no inhibition on both GP-α and α-glucosidase. In vivo study showed that EAF treatment significantly reduced blood glucose level, increased insulin and glycogen contents, decreased markers of oxidative stress and inflammation, and lipid levels in T2D rats compared with untreated group.ConclusionsThe EAF has potential therapeutic value for the treatment of T2D via acting as GP-α and α-glucosidase inhibitors by improving hepatic glucose and carbohydrate metabolism, suppressing oxidative stress, and preventing inflammation in T2D rats. According to the results, the efficacy of EAF could be due to the presence of luteolin along with synergistic effect of multiple compounds such as parahydroxybenzoic acid, protocatechuic acid, and gallic acid in B. javanica seeds.
The purpose of this study was to isolate and identify compounds from the bark of Alseodaphne perakensis (Lauraceae) which commonly known as Medang to validate and evaluate the use of this species in antimalaria activity. The comprising compounds from the dichloromethane crude extract were separated using column chromatography and the structures of the compounds were elucidated using spectroscopic analysis. The identified compounds were aporphine alkaloids; corydine 1 and oxohernagine 2. These isolated compounds show IC 50 values 0.404µg/ml and 0.738µg/ml, respectively against Plasmodium falciparum, K1 isolate (resistant strain).
Studies have been conducted over the last decade to identify secondary metabolites from plants, in particular those from the class of alkaloids, for the development of new anti-Alzheimer’s disease (AD) drugs. The genus Alseodaphne, comprising a wide range of alkaloids, is a promising source for the discovery of new cholinesterase inhibitors, the first-line treatment for AD. With regard to this, a phytochemical investigation of the dichloromethane extract of the bark of A. pendulifolia Gamb. was conducted. Repeated column chromatography and preparative thin-layer chromatography led to the isolation of a new bisbenzylisoquinoline alkaloid, N-methyl costaricine (1), together with costaricine (2), hernagine (3), N-methyl hernagine (4), corydine (5), and oxohernagine (6). Their structures were elucidated by the 1D- and 2D-NMR techniques and LCMS-IT-TOF analysis. Compounds 1 and 2 were more-potent BChE inhibitors than galantamine with IC50 values of 3.51 ± 0.80 µM and 2.90 ± 0.56 µM, respectively. The Lineweaver–Burk plots of compounds 1 and 2 indicated they were mixed-mode inhibitors. Compounds 1 and 2 have the potential to be employed as lead compounds for the development of new drugs or medicinal supplements to treat AD.
Phytochemistry investigation on alkaloids from Alseodaphne pendulifolia Gamb. yielded 3 types of aporphines; Hernagine 1, N-methylhernagine 2, and Oxohernagine 3. Preliminary screening on alkaloids crude extract from this species exhibited an antiplasmodial activity (0.804µg/ml IC 50 ) against Plasmodium falciparum, K1 isolate (resistant strain). Further investigation on isolated compound were found to possess antiplasmodial activity (0.738 -1.814µg/ml IC 50 ). This study involves extraction, separation by using various chromatography methods and structural elucidation by spectroscopic technique such as IR, NMR including 1D, 2D-NMR and MS.
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