A novel skeleton alkaloid from Portulaca oleracea L. and its bioactivities.

A novel skeleton alkaloid was obtained from Portulaca oleracea L., which was identified as 10,11-dihydroxybenzo[5',6'] pentaleno[1',2':3,4]pyrrolo[2,1-b]oxazol-7(11bH)-one, named oleracone M, and its structure was determined using UHPLC-ESI-QTOF/MS, 1D NMR and 2D NMR spectroscopy, and circular dichroism. Then the bioactivities of the compound were investigated including the anti-inflammatory, anti-acetylcholinesterase and antioxidant activities. The results showed that the novel skeleton alkaloid exhibited the potent effect on inhibiting the secretion of IL-1ß at 10 µM, anticholinesterase activity with IC50 value of 49.58 µM, and antioxidant activity with IC50 value of 66.43 µM.

Plants of the Genus Mahonia as a Potential Traditional Chinese Medicine for the Prevention and Treatment of Alzheimer's Disease.

Alzheimer's disease (AD), a prevalent multiple neurodegenerative disease, has gained attention, particularly in the aging population. However, presently available therapies merely focus on alleviating the symptoms of AD and fail to slow disease progression significantly. Traditional Chinese medicine (TCM) has been used to ameliorate symptoms or interfere with the pathogenesis of aging-associated diseases for many years based on disease-modifying in multiple pathological roles with multi-targets, multi-systems and multi-aspects. Mahonia species as a TCM present potential for anti-inflammatory activity, antioxidant activity, anti-acetylcholinesterase activity, and antiamyloid- beta activity that was briefly discussed in this review. They are regarded as promising drug candidates for AD therapy. The findings in this review support the use of Mahonia species as an alternative therapy source for treating AD.

Mucuna pruriens Seed Aqueous Extract Improved Neuroprotective and Acetylcholinesterase Inhibitory Effects Compared with Synthetic L-Dopa.

L-dopa, a dopaminergic agonist, is the gold standard for the treatment of Parkinson's disease. However, due to the long-term toxicity and adverse effects of using L-dopa as the first-line therapy for Parkinson's disease, a search for alternative medications is an important current challenge. Traditional Ayurvedic medicine has suggested the use of Mucuna pruriens Linn. (Fabaceae) as an anti-Parkinson's agent. The present study aimed to quantify the amount of L-dopa in M. pruriens seed extract by HPLC analysis. The cytotoxicity and neuroprotective properties of M. pruriens aqueous extract were investigated by two in vitro models including the serum deprivation method and co-administration of hydrogen peroxide assay. The results showed the significant neuroprotective activities of M. pruriens seed extracts at a concentration of 10 ng/mL. In addition, the effects of L-dopa and M. pruriens seed extract on in vitro acetylcholinesterase activities were studied. M. pruriens seed extract demonstrated acetylcholinesterase inhibitory activity, while synthetic L-dopa enhanced the activity of the enzyme. It can be concluded that the administration of M. pruriens seed might be effective in protecting the brain against neurodegenerative disorders such as Parkinson's and Alzheimer's diseases. M. prurience seed extract containing L-dopa has shown less acetylcholinesterase activity stimulation compared with L-dopa, suggesting that the extract might have a superior benefit for use in the treatment of Parkinson's disease.

Comparison of Various Solvent Extracts and Major Bioactive Components from Unsalt-Fried and Salt-Fried Rhizomes of Anemarrhena asphodeloides for Antioxidant, Anti-α-Glucosidase, and Anti-Acetylcholinesterase Activities.

The rhizome of Anemarrhena asphodeloides Bunge (AA, family Liliaceae) is a famous and frequently used herbal drug in the traditional medicine of Northeast Asia, under vernacular name "zhimu". A. asphodeloides has been used as an anti-inflammatory, antipyretic, anti-platelet aggregation, anti-depressant, and anti-diabetic agent in traditional Chinese medicine. We examined the antioxidant, anti-acetylcholinesterase (AChE), and anti-α-glucosidase activities of various solvent extracts and the main bioactive compounds from the rhizome of A. asphodeloides. Acetone extract exhibited comparatively high antioxidant activities by 2,2-diphenyl-1-(2,4,6-trinitrophenyl)hydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging, and ferric-reducing antioxidant power (FRAP) assays. A water extract exhibited relatively strong antioxidant activity by superoxide radical scavenging test. Furthermore, dichloromethane, chloroform, and n-hexane extracts showed significant anti-α-glucosidase activities. Finally, ethanol and dichloromethane extracts exhibited relatively strong AChE inhibitory activity. HPLC analysis was used to examine and compare various solvent extracts for their compositions of isolates. We isolated four major chemical constituents and analyzed their antioxidant, anti-α-glucosidase, and AChE inhibitory activities. The bioactivity assays showed that mangiferin displayed the most potential antioxidant activities via FRAP, ABTS, DPPH, and superoxide assays and also exhibited the most effective anti-AChE and anti-α-glucosidase activities among all the isolates. The present study suggests that A. asphodeloides and its active extracts and components are worth further investigation and might be expected to develop as a candidate for the treatment or prevention of oxidative stress-related diseases, AChE inhibition, and hyperglycemia.

Dynamic changes in chemical compositions and anti-acetylcholinesterase activity associated with steaming process of stem-leaf saponins of Panax notoginseng.

Stem-leaf saponins (SLSs), the total saponins from aerial part of P. notoginseng, are by-products of notoginseng, a famous traditional Chinese medicine. SLSs have been used as a health functional food in China, but its mild effects limited clinical applications in diseases. Inspired by steaming of notoginseng to enhance its pharmacological activity, a steaming protocol was developed to treat SLSs. SLSs were steamed at 100, 120, and 140°C for 1, 2, 3, and 4 h, respectively. The ultra-performance liquid chromatography coupled with quadrupole time-of-flight MS and ultra-performance liquid chromatography-tandem triple quadrupole mass spectrometry were applied to analyze the dynamic changes in chemical compositions. The anti-acetylcholinesterase activity of steamed SLS were assessed in vitro by directly determining the metabolic product of acetylcholine/choline. The components of SLSs were significantly changed by steaming. A total of 117 saponins and aglycones were characterized, and 35 of them were newly generated. The anti-acetylcholinesterase activity of steamed SLSs gradually increased with the extension of steamed time and the increase of steamed temperature and reached the maximum after 140°C for 3 h. Furthermore, ginsenosides Rk1 and Rg5, the main components of steamed SLSs, showed dose-dependent anti-acetylcholinesterase activities with half maximal inhibitory concentration (IC50 ) values of 26.88 ± 0.53 µm and 22.41 ± 1.31 µm that were only 1.8- and 1.5-fold higher than that of donepezil with IC50 values of 14.93 ± 4.17 µM, respectively.

A new pyrrole alkaloid from the roots of Cissampelos pareira.

Phytochemical investigation of the roots of Cissampelos pareira Linn. led to the isolation of one new pyrrole alkaloid, cissampeline (1), together with ten known alkaloids, (-)-curine (2), (-)-cyclanoline (3), (+)-tetrandrine (4), (+)-obaberine (5), (+)-obamegine (6), (-)-oblongine (7), (+)-homoaromoline (8), (-)-nor-N׳-chondrocurine (9), trans-N-feruloyltyramine (10) and (+)-coclaurine (11). Their structures were elucidated by extensive NMR and MS spectroscopic analyses. Interestingly, compound 1 represents the first example of pyrrole alkaloid found in the genus Cissampelos. Moreover, compounds 5-11 were isolated for the first time from this genus. Among them, compound 6 showed the highest anti-acetylcholinesterase activity with an IC50 value of 3.26 µM, whereas compound 8 displayed the most potent cytotoxicity against human colon cancer (HT29) cells with an IC50 value of 7.89 µM.

Anti-Acetylcholinesterase Activities of Mono-Herbal Extracts and Exhibited Synergistic Effects of the Phytoconstituents: A Biochemical and Computational Study.

Alzheimer's disease (AD), a neurodegenerative disease, is the most common form of dementia. Inhibition of acetylcholinesterase (AChE) is a common strategy for the treatment of AD. In this study, aqueous, hydro-methanolic, and methanolic extracts of five potent herbal extracts were tested for their in vitro anti-AChE activity. Among all, the Tinospora cordifolia (Giloy) methanolic fraction performed better with an IC50 of 202.64 µg/mL. Of the HPLC analyzed components of T. cordifolia (methanolic extract), palmatine and berberine performed better (IC50 0.66 and 0.94 µg/mL, respectively) as compared to gallic acid and the tool compound "galantamine hydrobromide" (IC50 7.89 and 1.45 µg/mL, respectively). Mode of inhibition of palmatine and berberine was non-competitive, while the mode was competitive for the tool compound. Combinations of individual alkaloids palmatine and berberine resulted in a synergistic effect for AChE inhibition. Therefore, the AChE inhibition by the methanolic extract of T. cordifolia was probably due to the synergism of the isoquinoline alkaloids. Upon molecular docking, it was observed that palmatine and berberine preferred the peripheral anionic site (PAS) of AChE, with π-interactions to PAS residue Trp286, indicating that it may hinder the substrate binding by partially blocking the entrance of the gorge of the active site or the product release.

Polyphenolic Profiling, Quantitative Assessment and Biological Activities of Tunisian Native Mentha rotundifolia (L.) Huds.

Phenolic profiling of ten plant samples of Mentha rotundifolia (L.) Huds. collected from different bioclimatic areas of Tunisia, was for the first time carried out by using a fast ultra-high-performance liquid chromatography (UHPLC)-high resolution tandem mass spectrometry (HRMS/MS) method on a Q Exactive platform equipped with an electrospray ionization (ESI) source. An intraspecific, interpopulation variability was evidenced and a total of 17 polyphenolic metabolites were identified and quantified by using the UHPLC-HRESIMS/MS method, here validated for specificity, linearity, limit of detection, limit of quantitation, accuracy and precision. The quantitative method resulted sensitive at the nM level and reliable for rapid polyphenol quantification in vegetal matrices. The metabolomic study allowed us to identify a new compound, named salvianolic acid W, which was isolated and characterized mainly by NMR and MS analysis. A statistical correlation of the phenolic composition with antioxidant and anti-acetylcholinesterase activities was provided.

Phytochemical composition and in vitro functional properties of three wild rose hips and their traditional preserves.

The aim of the present study was investigation of the phenolic profile, ascorbic acid content, antioxidant, anti-acetylcholinesterase, anti-inflammatory and cytotoxic activity of rose hips and the preserves (purée and jam) of three insufficiently examined Rosa species: Rosa dumalis Bechst., R. dumetorum Thuill. and R. sempervirens L. The liquid chromatography-tandem mass spectrometry analysis resulted in quantification of 14 of the 45 phenolic compounds examined, with ellagic acid as the most dominant. Notable antioxidant activity of all three species was confirmed through several assays. Moderate inhibition of acetylcholinesterase by extracts of all investigated Rosa species was observed. Several extracts of examined Rosa species demonstrated inhibition potency towards production of some monitored eicosanoids in cyclooxygenase-1 and 12-lipoxygenase pathways. Two R. sempervirens extracts exerted cytotoxic activity against HeLa and HT-29 cell lines, but were inactive towards MRC-5 and MCF7. The results support the potential of these rose hips as food with health-promoting properties.