ABSTRACT
Alzheimer's disease (AD) is a neurodegenerative disease that causes deterioration in intelligence and psychological activities. Yet, till today, no cure is available for AD. The marine environment is an important sink of bioactive compounds with neuroprotective potential with reduced adverse effects. Recently, we collected the red algae Laurencia snackeyi from Terumbu Island, Malaysia which is known to be rich in halogenated metabolites making it the most sought-after red algae for pharmaceutical studies. The red alga was identified based on basic morphological characteristics, microscopic observation and chemical data from literature. The purplish-brown algae was confirmed a new record. In Malaysia, this species is poorly documented in Peninsular Malaysia as compared to its eastern continent Borneo. Thus, this study intended to investigate the diversity of secondary metabolites present in the alga and its cholinesterase inhibiting potential for AD. The extract inhibited both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with IC50 values of 14.45 ± 0.34 µg mL-1 and 39.59 ± 0.24 µg mL-1, respectively. Subsequently, we isolated the synderanes, palisadin A (1), aplysistatin (2) and 5-acetoxypalisadin B (3) that was not exhibit potential. Mass spectrometry analysis detected at total of 33 additional metabolites. The computational aided molecular docking using the AChE and BChE receptors on all metabolites shortlisted 5,8,11,14-eicosatetraynoic acid (31) and 15-hydroxy-1-[2-(hydroxymethyl)-1-piperidinyl]prost-13-ene-1,9-dione (42) with best inhibitory properties, respectively with the lowest optimal combination of S-score and RMSD values. This study shows the unexplored potential of marine natural resources, however, obtaining sufficient biomass for detailed investigation is an uphill task. Regardless, there is a lot of potential for future prospects with a wide range of marine natural resources to study and the incorporation of synthetic chemistry, in vivo studies in experimental design. Supplementary Information: The online version contains supplementary material available at 10.1007/s13205-023-03725-6.
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Osteoarthritis is a disease associated with articular cartilage degradation, intra-articular area inflammation, and subchondral bone replacement. Cytokine IL-1ß has a prominent function in the inflammations process that passes in the joints. The 70% ethanol extracts of deer antler (250 and 500 mg/kg BW) and glucosamine sulfate (250 kg/BW) were evaluated for four weeks in reducing cytokine IL-1ß to rat model OA-induced Monosodium iodoacetate. Measurements of joint diameter in rat's knee and hyperalgesia were performed on weeks 0, 1, 2, 3, 4, 5, 6, and 7. The presence of a significant difference in the stimulation thermal latency (p = 0.00) and the resulting increase in swelling of joint diameter (p = 0.00) are evidence that MIA has successfully induced the rat modeling of OA. A significant decrease in cytokine IL-Iß levels was shown on week 3 after MIA injection (p = 0.00). Both concentrations of deer extracts significantly reduced knee joint diameter (p = 0.00), latency thermal stimulation (p = 0.00), and cytokine IL-1ß levels (p = 0.00). Based on the results, it can be concluded that the 70% ethanol extract of deer antler is a potential medicine for OA therapy.
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This study aimed to obtain a microbial active compound as a novel antimalarial drug from Indonesian isolates. Target-based assays were used to screen for antimalarial activity against the parasite mitochondrial, Plasmodium falciparum malate:quinone oxidoreductase (PfMQO) enzyme. In total, 1600 crude extracts, composed from 800 fungi and 800 actinomycetes extracts, were screened against PfMQO, yielding six active extracts as primary hits. After several stages of stability tests, one extract produced by Aspergillus sp. BioMCC f.T.8501 demonstrated stable PfMQO inhibitory activity. Several purification stages, including OCC, TLC, and HPLC, were performed to obtain bioactive compounds from this active extract. All purification steps were followed by an assay against PfMQO. We identified the active compound as nornidulin based on its LC-MS and UV spectrum data. Nornidulin inhibited PfMQO activity at IC50 of 51 µM and P. falciparum 3D7 proliferation in vitro at IC50 of 44.6 µM, however, it had no effect on the growth of several mammalian cells. In conclusion, we isolated nornidulin from Indonesian Aspergillus sp. BioMCC f.T.8501 as a novel inhibitor of PfMQO, which showed inhibitory activity against the proliferation of P. falciparum 3D7 in vitro.
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Background: Pternandra galeata belongs to the family Melastomataceae. It is a native flowering plant in Borneo Island that serve as food for monkey habitat. There has been limited study on the medicinal and chemical properties of this plant. Objectives: We investigated the acetylcholinesterase inhibitory activity and evaluated the antioxidant activity of the ethanolic extract of Pternandra galeata stem. The total phenolic content in the sample was also determined. Methods: The acetylcholinesterase inhibitory assays were performed using Ellman's method. Two different methods were used to evaluate the antioxidant activity of the extract by 2,2-diphenyl-1-picryl hydrazyl (DPPH) and 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays. The total phenolic content was determined by the Folin-Ciocalteu method by employing gallic acid as a reference. Results: The ethanolic extract of the P. galeata stems inhibited the AChE enzyme with an IC50 value of 74.62 ± 0.89 µg/mL.The sample exhibited antioxidant activity in the DPPH assay with an IC50 value of 20.21 ± 0.08 µg/mL and 7.68 ± 0.09 µg/mL in the ABTS scavenging assay. The total phenolic content was 164.71 ± 3.33 mg GAE/g extract. Conclusion: The ethanolic extract of the P. galeata stem can be a promising cholinesterase inhibitor and antioxidant for treating Alzheimer's disease
Antecedentes: Pternandra galeata pertenece a la familia Melastomataceae. Se trata de una planta con flores nativa de la isla de Borneo que sirve de alimento para el hábitat de los monos. Se han realizado pocos estudios sobre las propiedades medicinales y químicas de esta planta. Objetivos: Se investigó la actividad inhibidora de la acetilcolinesterasa y se evaluó la actividad antioxidante del extracto etanólico del tallo de Pternandra galeata. También se determinó el contenido fenólico total de la muestra. Métodos: Los ensayos de inhibición de la acetilcolinesterasa (AChE) se realizaron mediante el método de Ellman. Se utilizaron dos métodos diferentes para evaluar la actividad antioxidante de los ensayos de 2,2-difenil-1-picril hidrazilo (DPPH) y 2,2'-azinobis-(ácido 3-etilbenzotiazolina-6-sulfónico) (ABTS). El contenido fenólico total se determinó por el método de Folin-Ciocalteu empleando el ácido gálico como referencia. Resultados: El extracto etanólico de los tallos de P. galeata inhibió la enzima AChE con un valor IC50 de 74.62 ± 0.89 µg/mL. La muestra mostró actividad antioxidante en el ensayo DPPH con un valor IC50 de 20.21 ± 0.08 µg/mL y 7.68 ± 0.09 µg/mL en el ensayo de barrido ABTS. El contenido fenólico total fue de 164.71 ± 3.33 mg GAE/g de extracto. Conclusión: El extracto etanólico del tallo de P. galeata puede ser un prometedor inhibidor de la colinesterasa y antioxidante para el tratamiento de la enfermedad de Alzheimer.
Subject(s)
Humans , Alzheimer Disease , Cholinesterase Inhibitors , Phenolic Compounds , AntioxidantsABSTRACT
OBJECTIVES: Glucocorticoid-induced osteoporosis (dexamethasone) is a primary cause of secondary osteoporosis by the decreasing formation and increasing resorption activities. Previously, the in vitro study showed that 70% ethanol and aqueous extract of deer antler have increased alkaline phosphatase in osteoblast cell that known as marker of bone formation. The mind of this study is to analyze the effect of deer antlers in increasing the bone trabecular density of osteoporosis-induced male mice. METHODS: This study used a post-test control group design. A total of 54 healthy male mice were randomly divided to nine groups, i.e., healthy control, osteoporotic, positive control, 70% ethanol (4, 8, and 12 mg/kg BW), and aqueous extracts (4, 8, and 12 mg/kg BW) of deer antler groups. All of the interventions were given 1 mL of test sample for 4 weeks orally. The bone densities were determined using histomorphometry by Image J and Adobe Photoshop. The statistical data were performed using SPSS 23 and statistical significance was set at p<0.05. RESULTS: The results showed that alendronate group, 70% ethanol, and aqueous extract groups increased bone density and calcium levels in serum (p<0.05) compared to osteoporotic group in dose dependent manner. It indicated that 70% ethanol and aqueous extract of deer antler stimulating bone turnover and aqueous extract showed the highest. CONCLUSIONS: Dexamethasone induction for 4 weeks caused osteoporotic mice and the administration of 70% ethanol and aqueous extracts of deer antler from East Kalimantan increased trabecular bone density and calcium levels in dose dependent manner.
Subject(s)
Antlers , Deer , Animals , Bone Density , Calcium , Cancellous Bone , Male , MiceABSTRACT
OBJECTIVES: Osteoporosis is a condition characterized by skeletal degradation of osseous tissue resulting in an escalated chance of broken bones. Traditionally, Rusa unicolor horn from East Kalimantan is used to treat many diseases, including conditions associated with bone turnover. The aim of the present research was to analyze the effects of 70% ethanol and aqueous extracts of R. unicolor antler's horn from East Kalimantan on nitric oxide inhibition, osteoblast differentiation, and mineralization related to bone turnover. MATERIALS AND METHODS: Nitric oxide inhibition of the extracts in lipopolysaccharide-stimulated RAW 264.7 macrophages was evaluated by Griess reagent, while the effects of extracts on osteoblast differentiations were measured by alkaline phosphatase in p-nitrophenyl phosphate. Their effects on mineralization was determined using alizarin red staining. RESULTS: The 70% ethanol and aqueous extracts inhibited cell inflammation (40% and 80%, respectively) and stimulated osteoblast differentiation (65% and 52%, respectively). In the mineralization test, the aqueous extract showed an effect two times higher than that of 70% ethanol extract. CONCLUSION: The extracts can effectively degrade inflammatory marker expression and preserve osteoblast functions.
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Cocos nucifera Linn., which contain lauric acid has been known had antibacterial activity against Propionibacterium acnes that usually improve severe of pimple. Current study investigated optimum formula of emulgel mask based on the C. nucifera L. Extract from Kopyor coconut. Extract were tested for antibacterial against P. acnes ATCC 11827. In this research, C. nucifera L. extract of 1 and 5% were formulated as an active agent of peel off antiacne emulgel mask-containing carbomer 940 in various concentration (1% and 1.5%). The peel-off emulgel mask of C. nucifera L extract was then evaluated in terms of viscosity, pH, drying time, spreadability, and antibacterial activity. The selected formula was formula containing 5% of extract and 1% of carbomer 940. This formula had pH that suitable with skin pH 4.5-6.5, had good spreadability, and also produced highest antibacterial activity against P. acnes.
