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TLC of Peganum harmala in comparison with authentic alkaloids. 1, Peganum harmala (DCM extract); 2, Peganum harmala (MeOH extract); 3, harmaline; 4, harmine;. (A) Bioautography assay. (B) Detection with Dragendorff reagent. Mobile phase: chloroform–ethylacetate–methanol (90 + 7 + 3). This figure is available in colour online at wileyonlinelibrary.com/journal/ptr
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To find new herbal compounds with an acetylcholinesterase (AChE) inhibitory effect, this study focused on herbal drugs and resins which have been used in Iranian traditional medicine for the treatment of cognitive disorders. Forty drugs were selected from authoritative written documents of Iranian traditional medicine. Each drug was extracted by ac...
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... the TLC bioautography assay the alkaloids harmaline and harmine were identified as the most active compounds (Fig. 2). The AChE inhibitory effect of these alkaloids has recently been deduced ( Zheng et al., 2009) in a study of another Peganum species, namely Peganum nigesllastrum Bunge, from a TLC bioautography assay, only. The IC 50 values of the extracts or the isolated alkaloids were not determined this investigation. In our study, the seeds of P. ...
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... Two more compounds; deoxyvasicine and vasicine, isolatedfrom it also exhibited strong BChE inhibitory activity(Yang et al., 2015). In another study seeds of this plant were isolated ten compounds in which harmol, harmaline, and harmine showed AChE inhibitory activity comparable to galanthamine(Zheng et al., 2009;Adhami et al., 2011;Zheng et al., 2011). In the present study, the results show that the crude hydro-methanolic extract of the seeds of P. harmala exhibits 52.8% AChE inhibition, which is significantly greater than the AChE inhibitory activity reported for the aerial parts of the same plant(Gholamhoseinian et al., 2009).3.1.4 ...
Objective: The principal aim of the current study was to estimate the Acetylcholinesterase (AChE) inhibition activity of crude hydro-methanolic extracts of fifty selected local medicinal plants; traditionally known for therapeutic properties. The top four plant extracts that showed promising AChE inhibition activity were further analyzed for antioxidant activity and phytochemical composition (total phenolic, total flavonoid, total tannins, total terpenoids, and total alkaloids). Methods: All the plant extracts were made in 80% methanol. The AChE inhibition activity was determined by a micro-plate assay and the antioxidant potential was calculated by DPPH free radical scavenging assay. Plant extracts having ≥50% ACHE inhibitory activity were further analyzed for phytochemicals, total phenols, total tannins, total flavonoids, total terpenoids, total alkaloids. Results: The results highlighted that out of all fifty selected plants only four possess >50% AChE inhibition potential, that are Quercus infectoria (87.6%), Flacourtia jangomas (66.6%), Peganum harmala (52.8%) and Solanum pseudocapsicum (50.3%) The P. harmala have the least (37.9%) and Q. infectoria possess the highest (90.6%) antioxidant activity, which is justified by the amount of phenolics and flavonoids compounds present in these plants. Phytochemicals study revealed that Q. infectoria possess higher flavonoid and alkaloid content. Whereas, S. pseudocapsicum possess higher phenolic and terpenoid content. Additionally, P. harmala possess high amount of tannins. On the contrary, this plant possess low content of phenolics, terpenoids, flavonoids, and alkaloids. Conclusion: This study concludes Q. infectoria induced significant AChE inhibitory activity as well as phytochemical properties. Thus, this plant could be promising for the development of new therapeutic agents. Additionally, Flacourtia jangomas was reported as new potent AChE inhibitor that encourage further studies that can lead to the development of new agents that might be used in the treatment of Alzheimer’s disease.
... Europe, Asia and southern Russia (Bourogaa et al., 2015), and it is known to have antibacterial, antifungal, antiviral, antidiabetic, antitumor, antileishmania, insecticidal and cytotoxic activities (Jinous and Fereshteh, 2012), and, even, anticancer activity (Boeira et al., 2001;Adhami et al., 2011). ...
Medicinal plants are an inexhaustible source of molecules with several biological activities. The main objective of this research was the evaluation of the antimitotic and genotoxic effect by the Allium cepa test of the methanolic extract of the leaves of Peganum harmala, a spontaneous plant from the arid zones of Algeria (Timzerth, Laghouat). Different concentrations (1, 4, 10, and 16 mg∙mL-1) of the extract, as well as two standards (colchicine and quercetin) at 1 mg∙mL-1 concentration were tested. Mitotic index (MI), limit value for cytotoxicity (LVC), phase index (PI), and aberration indexes (AI) were calculated, and different aberrations were identified in treated meristematic onion cells. Statistical analyses by ANOVA and Newman-Keuls test were performed. The results confirmed our previous findings that the methanolic extract has an anti-mitotic effect similar to that of the standards. The increase in extract concentrations was accompanied by a decrease in the various indexes calculated. The extracts blocked mitosis in prophase which was predominantly present, and caused increase in abnormalities, represented by dominant rates of agglutinations, chromosomal fragmentations and binuclear cells. confirmed that the effect was independent of concentrations, though to varying degrees.
... [123] It is characterized by psychopathological signs such as language deterioration, memory loss, visuospatial impairment, and poor judgment. [124] Alzheimer's disease is also linked with acetylcholine (Ach) deficiency in the synaptic cleft of the cerebral cortex that causes memory disturbance. Acetyl cholinesterase, also known as AChE or acetyl hydrolase, hydrolyzes the neurotransmitter acetylcholine. ...
Globalization witnessed changing trends in consumer markets. However, their long-term impacts include lifestyle and dietary changes. Although research in the pharmaceutical and chemical sciences led to the discovery and development of drugs saving millions of lives, their persistent use led to safety and toxicological issues. The plants previously used in Chinese and Ayurveda medicines received attention of the researchers to validate their traditional therapeutic applications. As a result, the reliance of communities on complementary and alternative medicines started to recover in the last few decades. The myrobalan (Terminalia chebula) is one such example that was renowned as the king of medicinal plants in Ayurveda due to its wide range of utilization in herbal decoctions to treat various health disparities. The current review showed phytochemical profile, that includes phenolic acids, casuarinin, chebulagic acid, chebulinic acid, rutin, and corilagin. Phytochemistry is linked with its medicinal applications and several research studies validated its antioxidant, antimicrobial, anti-inflammatory, hypoglycemic, and digestive tonic. The facts presented in the current article are derived from cell culture, animal, and human studies. Moreover, conceptualized framework regarding the effectiveness against cardiovascular disorders, immune dysfunction, cancer insurgence, and neurological disorders is in the limelight of the article. In last, a comprehensive discussion regarding its potential inclusion in the modern-day functional food market and presents its future applications.
... [123] It is characterized by psychopathological signs such as language deterioration, memory loss, visuospatial impairment, and poor judgment. [124] Alzheimer's disease is also linked with acetylcholine (Ach) deficiency in the synaptic cleft of the cerebral cortex that causes memory disturbance. Acetyl cholinesterase, also known as AChE or acetyl hydrolase, hydrolyzes the neurotransmitter acetylcholine. ...
Globalization witnessed changing trends in consumer markets. However, their long-term impacts include lifestyle and dietary changes. Although research in the pharmaceutical and chemical sciences led to the discovery and development of drugs saving millions of lives, their persistent use led to safety and toxicological issues. The plants previously used in Chinese and Ayurveda medicines received attention of the researchers to validate their traditional therapeutic applications. As a result, the reliance of communities on complementary and alternative medicines started to recover in the last few decades. The myrobalan (Terminalia chebula) is one such example that was renowned as the king of medicinal plants in Ayurveda due to its wide range of utilization in herbal decoctions to treat various health disparities. The current review showed phytochemical profile, that includes phenolic acids, casuarinin, chebulagic acid, chebulinic acid, rutin, and corilagin. Phytochemistry is linked with its medicinal applications and several research studies validated its antioxidant, antimicrobial, anti-inflammatory, hypoglycemic, and digestive tonic. The facts presented in the current article are derived from cell culture, animal, and human studies. Moreover, conceptualized framework regarding the effectiveness against cardiovascular disorders, immune dysfunction, cancer insurgence, and neurological disorders is in the limelight of the article. In last, a comprehensive discussion regarding its potential inclusion in the modern-day functional food market and presents its future applications.
... The inhibitory activities of the extract of SA on AChE enzyme were measured by Ellman's method and as described previously (Adhami et al., 2011). To preparation rat erythrocytes membrane, the blood (2.5-3 ml) was drawn from the rat and transferred to 50 ml de-ionized chilled water. ...
Alzheimer's disease (AD) is a progressive neurological ailment that manifests as difficulties in completing everyday activities, disorientation, and memory loss. Several innovative drug therapies have failed in clinical trials because they cannot stop or encourage the regeneration of injured brain cells. Furthermore, many medications only give symptomatic alleviation. As a result, a better knowledge of stem cell therapy's process might lead to new and effective treatments for this severe disease. Recent preclinical evidence suggests that stem cells can be used to treat or model AD. The mechanisms of stem cell based therapies for AD include stem cell mediated neuroprotection and trophic actions, antiamyloidogenesis, beneficial immune modulation, and the replacement of the lost neurons. This study examined the present status of many Mesenchymal stem cell-based therapeutics in AD pathogenesis. Furthermore, we have emphasized current clinical research that may be useful in treating Alzheimer's disease.
... The inhibitory activities of the extract of SA on AChE enzyme were measured by Ellman's method and as described previously (Adhami et al., 2011). To preparation rat erythrocytes membrane, the blood (2.5-3 ml) was drawn from the rat and transferred to 50 ml de-ionized chilled water. ...
Bhilawanol (Bh) and anacardic acid (AA) are two lipid-soluble compounds mostly found in the nut of Semecarpus anacardium (SA). This herb has many medicinal properties including enhancing learning and memory, yet its active compounds have not been studied for neuroprotective effects. We investigated the neuroprotective effects of Bh and AA against glutamate induced cell death in the adrenal pheochromocytoma cell line of rats (PC12 cells). Cell viability, toxicity and calcium influx were determined by MTT assay, LDH release assay and Fluo-3 imaging while apoptosis was assayed by caspase-3 and Bcl-2 gene expression. Our results showed that Bh and AA treatments significantly increased cell viability, reduced cell toxicity and calcium influx in PC12 cells in addition to suppressing the reactive oxygen species. Furthermore, AA treatment decreased caspase-3 expression level whereas both Bh and AA enhanced the expression of anti-apoptotic gene Bcl-2 in PC12 cells. Both compounds potently inhibited acetylcholinesterase enzyme (AChE) in a dose and time dependent manner. These findings suggest that the traditional use of SA may be explained on the basis of both Bh and AA showing neuroprotective potential due to their effects on enhancing cell viability, reducing cell toxicity most probably by reducing excessive calcium influx and suppression of ROS as well as by decreasing the expression of proapoptotic caspase 3 gene and increasing the expression of antiapoptotic gene Bcl2. Traditional use in enhancing learning and memory was justified in part by inhibition of AChE.
... Study performed by De Silva [43] on industrial utilization of medicinal plants in developing countries showed that the value of trade in herbal medicines has a yearly growth of 12-15%. In fact, the world's population (about 80%) still relies on their traditional medicines to cure the important and common ailments like digestive system diseases [44][45][46][47][48], liver disease [49,50], urinary system disorders [51], skin disorders and rash [45,52], diabetes [53], psychiatric disorders [54], lung diseases [41], pain relief [55], malaria [55] etc. [3,28,30,57] for their everyday health care needs. ...
... The aqueous extract of its leaves and the ethanolic extract of its oleoresin also possessed AChE inhibitory activity with IC 50 values around 10 µg/mL [188]. Moreover, its dichloromethane extract oleoresin has also shown AChE inhibitory activity in vitro [189]. The methanolic extract could reduce Aβmediated cellular toxicity in SH-SY5Y cells [182]. ...
Alzheimer’s disease (AD) is the number one neurovegetative disease, but its treatment options are relatively few and ineffective. In efforts to discover new strategies for AD therapy, natural products have aroused interest in the research community and in the pharmaceutical industry for their neuroprotective activity, targeting different pathological mechanisms associated with AD. A wide variety of natural products from different origins have been evaluated preclinically and clinically for their neuroprotective mechanisms in preventing and attenuating the multifactorial pathologies of AD. This review mainly focuses on the possible neuroprotective mechanisms from natural products that may be beneficial in AD treatment and the natural product mixtures or extracts from different sources that have demonstrated neuroprotective activity in preclinical and/or clinical studies. It is believed that natural product mixtures or extracts containing multiple bioactive compounds that can work additively or synergistically to exhibit multiple neuroprotective mechanisms might be an effective approach in AD drug discovery.
... This method is used to detect AChE inhibitors in various plants. [77,[109][110][111][112][113][114][115][116] If the mixture is better separated on the RP-18 plate, its use in the Marston method [86] is problematic thanks to the weak response of inhibitory active compounds. To accelerate the identification of AChE inhibitors, Ramallo et al. [117] developed agar version of the Marston method [86] combined with high resolution mass spectrometry. ...
Microorganisms and plants can be important sources of many compounds with potential pharmaceutical applications. Extraction of these matrices is one of the ways of identifying the presence of inhibitory active substances against enzymes whose high activity leads to serious human diseases including cancer, Parkinson's or Crohn's diseases. The isolation and purification of inhibitors are time-consuming and expensive steps in the analysis of the crude extract and therefore, it is necessary to find a fast, efficient, and inexpensive method for screening extracts of interest. TLC-Bioautography combines the separation of the extract on a thin layer with its subsequent biological analysis. TLC-Bioautography methods have been developed for several classes of enzymes including oxidoreductases, hydrolases and isomerases, and there is a potential for developing functional methods for other classes of enzymes. This review summarizes known TLC-Bioautography methods and their applications for determining the presence of enzyme inhibitors in extracts and compares the effectiveness of different methodological approaches. It also indicates the current state and perspective of the development of TLC-Bioautography and its possible future applications.
... Alzheimer's disease (AD) is a chronic neurodegenerative disorder which is created via multiple mechanisms in the brain including reduction of acetylcholine (ACh) [1], Res J Pharmacogn 7(3): [25][26][27][28][29][30][31][32][33] intracellular hyper-phosphorylated tau neurofibrillary tangles [2], accumulation of extracellular beta amyloid (Aβ42) plaques [3], β-site APP-cleaving enzyme 1 or beta secretase (BACE 1) [4], redox metal dysregulation [5], and oxidative stress caused by mitochondrial dysfunction [6]. AD is usually described by the reduction or loss of cognitive functions and intelligence in patients, which finally leads to dementia. ...
... Moreover, it has been used for the treatment of epilepsy, paralysis, limb numbness, obstructive jaundice, inflammation of the liver and spleen, ascites, corneal inflammation, kidney and bladder stones, joint pain, amenorrhea, difficulty urinating, general edema, sciatica, and gout [23][24][25]. It has also demonstrated pharmacological properties such as antimicrobial, antitumor [26], gastroprotective, antiulcer properties [27], and AChEI activity based on TLC bioautography method in recent studies [28]. In continuation of our research on the herbal ChEIs [17,18,29,30] and focusing on the medicinal properties of A. europaeum recommended in ITM, here in, the rhizome of the plant was investigated for anti-ChE and antioxidant activities as well as neuroprotectivity and metal chelating ability as important pathways involved in the creation of AD. ...
... MTT solution (5 mg/mL) was added to each well in a volume of 10 μL, and 3.5 h later, 100 μL of the solubilisation solution [10% SDS in 0.01 M HCl (w/v)] was added into each well. The plates were Res J Pharmacogn 7(3): [25][26][27][28][29][30][31][32][33] allowed to stand overnight in the incubator in a humidified atmosphere. Absorbance was measured at 570 nm with a reference wavelength of 630 nm using a plate reading spectrophotometer (BioTek ELx808, USA). ...
Background and objectives: Asarum europaeum L. is an herbal medicine belonging to the family Aristolochiaceae. The rhizome of the plant has been used for the treatment of various diseases in complementary and alternative medicine of various countries. In Iranian traditional medicine (ITM), the aqueous extract of the rhizome has been used for the improvement and enhancement of memory. Methods: In the present study, the aqueous and hydroalcoholic extracts as well as different fractions of A. europaeum rhizome were evaluated for their cholinesterase (ChE), acetyl- and butyrylcholinesterase (AChE and BChE) inhibitory activity viamodified Ellman's method. Results: The ethyl acetate fraction selectively showed the most suitable anti-AChE activity (IC50 = 99.69 µg/mL); none of the extracts or fractions demonstrated anti-BChE activity. In this regard, the ethyl acetate fraction was candidate for the investigation of further biological activities such as antioxidant activity, neuroprotectivity, and metal chelating ability related to Alzheimer’s disease. It depicted favorable neuroprotectivity at concentration of 100 μg/mL against the toxicity of exposure to H2O2 in PC12 cells (p£0.001, cell viability = 80/60%) and chelating ability towards zinc, iron, and copper ions. The results of antioxidant activity by DPPH assay showed that the ethyl acetate fraction was much more potent than BHA as the reference drug. Conclusion: The ethyl acetate fraction ofA. europaeum L. showed potent biological activities involved in Alzheimer’s disease and needs complementary investigations to develop an herbal product against Alzheimer’s disease.
