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Phytochemical profile and activity of anti-oxidative, anti-glycative, anti-α-amylase, anti-α-glucosidase, anti-lipase and anti-acetylcholinesterase (AchE) of aqueous extracts prepared from leaf and stem parts of two edible Amaranthus species, white and red amaranths, were investigated. Phytochemical analyses showed that white amaranth had more total phenolic acids than red one. The content of total flavonoids in four examined aqueous extracts was similar. Red amaranth has greater anthocyanins and carotenoids than white one. All aqueous extracts at three concentrations were used for in vitro bio-activities experiments. Results showed that four aqueous extracts displayed radical scavenging effect, Fe 2+ chelating effect, xanthine oxidase inhibition, and reducing power. Aqueous extracts prepared from red amaranth exhibited marked anti-glycative effects, anti-α-amylase, anti-α-glucosidase, anti-lipase, and anti-AchE activities. These findings suggested that these two vegetables could be developed as functional foods for diabetic prevention and/or attenuation.

The methanol extracts from Hippeastrum reticulatum (L'Hér.) Herb. (Amaryllidaceae) (HR) display acetylcholinesterase inhibitory (AChEI) activity. AChEI of alkaloids isolated from HR bulbs and the ameliorating effects of the alkaloid fraction (AHR) on memory and cognitive dysfunction in scopolamine-treated mice were investigated. Alkaloids were isolated by column chromatography and identified by spectroscopy. AChEI was evaluated using the modified Ellman's method. Sixty Swiss male mice were randomly divided into six groups, received samples for 15 days. Normal group received saline, scopolamine-treated group scopolamine (1.5 mg/kg, intraperitoneal injection). Test groups received AHR (5, 10 and 15 mg/kg, per os) and positive control group donepezil (5 mg/kg, per os), administered 1 h before the test, scopolamine was injected 30 min prior to testing. The cognitive-enhancing activity of AHR against scopolamine-induced memory impairments was investigated using Y-maze, the novel object recognition test (NORT) and the Morris water maze (MWM) test. Seven alkaloids were isolated for the first time from the genus Hippeastrum: trans-dihydronarciclasine (1), N-chloromethylnarcissidinium (2), narciprimin (3), narciclasine-4-O-β-d-xylopyranoside (4), N-methyltyramine (5), 3β,11α-dihydroxy-1,2-dehydrocrinane (6) and brunsvigine (7); three are new compounds (2, 5, 6). Among them, 2-3 and 5-6 showed AChEI in vitro with IC 50 values of 29.1, 46.4, 70.1 and 104.5 µg/mL, respectively. The anti-AChEI of 2, 5 and 6 are reported for the first time. In in vivo test, AHR (15 mg/kg) significantly increased in spontaneous alternation performance in the Y-maze test (p < 0.01), it significantly increased the time spent exploring the novel object (p < 0.05) comparison with scopolamine-treated group. The administration of AHR at doses 10 and 15 mg/kg significantly decreased escapes latency and swimming distance to the platform on day 6 compared to these in day 1 (p < 0.01 and p < 0.05, respectively). AHR could be a potential candidate of future trials for treatment of memory and cognitive dysfunction in Alzheimer's disease.

The rising incidence of neurodegenerative diseases represents a significant global health concern. The prognosis for such diseases is often unfavorable, and patients require supportive treatment to manage their condition effectively. The present study investigated the anti-oxidative, anti-acetylcholinesterase (anti-AChE) effect of hydro-alcoholic extract of Sansevieria cylindrica leaves and Plumeria obtusa seed pods in Wistar rats. Plants were authenticated followed by pharmacognostic evaluation. The antioxidant and anti-AChE activities were evaluated by scopolamine-induced oxidative stress and acetylcholine level alterations in Wistar rats. On the 0th, 7th, and 14th days during study period behavioral parameters were evaluated, including open field test, new object recognition test, and Morris water maze task. Different antioxidant enzymes were also evaluated in brain homogenate post 7 days treatment. AChE levels in rats’ brains were assessed post 14 days of treatment. Finally, histopathology of brains samples was performed. Correspondingly, in-vitro and in-silico studies were done to support the study findings. Results Sansevieria cylindrica and Plumeria obtusa exhibited strong antioxidant and anti-AChE activities due to secondary metabolites content. Rearing and, line crossing by rats showed substantial alteration ( p  < 0.05) by combination of both plants at high dose. The escape latency found to be reduced significantly ( p  < 0.05) by Sansevieria cylindrica individually and in combination with Plumeria obtusa at all doses. The lipid peroxidation level in brain was decreased significantly than standard at 1:1 combination of plants extracts. The levels of GSH, CAT and SOD were attenuated significantly by different concentration of extracts ( p  < 0.05 and p  < 0.001, respectively). The reduction in AChE levels was around 34.62% and 31.10% in male and female rats, respectively in combination of both plants at high dose compared to disease control group. It was further evident in brain histopathology. All in-vivo results were supported by in-vitro free radicals scavenging effect and in-silico study. Conclusion The hydro-alcoholic extracts from Plumeria obtusa seed pods and Sansevieria cylindrica leaves showed a strong natural antioxidant, and acetylcholinesterase inhibitions which can aid in the treatment of neurodegerative diseases including Alzheimer.

The biological activity of Rhinella icterica parotoid secretion (RIPS) and some of its chromatographic fractions (RI18, RI19, RI23, and RI24) was evaluated in the current study. Mass spectrometry of these fractions indicated the presence of sarmentogenin, argentinogenin, (5β,12β)-12,14-dihydroxy-11-oxobufa-3,20,22-trienolide, marinobufagin, bufogenin B, 11α,19-dihydroxy-telocinobufagin, bufotalin, monohydroxylbufotalin, 19-oxo-cinobufagin, 3α,12β,25,26-tetrahydroxy-7-oxo-5β-cholestane-26-O-sulfate, and cinobufagin-3-hemisuberate that were identified as alkaloid and steroid compounds, in addition to marinoic acid and N-methyl-5-hydroxy-tryptamine. In chick brain slices, all fractions caused a slight decrease in cell viability, as also seen with the highest concentration of RIPS tested. In chick biventer cervicis neuromuscular preparations, RIPS and all four fractions significantly inhibited junctional acetylcholinesterase (AChE) activity. In this preparation, only fraction RI23 completely mimicked the pharmacological profile of RIPS, which included a transient facilitation in the amplitude of muscle twitches followed by progressive and complete neuromuscular blockade. Mass spectrometric analysis showed that RI23 consisted predominantly of bufogenins, a class of steroidal compounds known for their cardiotonic activity mediated by a digoxin- or ouabain-like action and the blockade of voltage-dependent L-type calcium channels. These findings indicate that the pharmacological activities of RI23 (and RIPS) are probably mediated by: (1) inhibition of AChE activity that increases the junctional content of Ach; (2) inhibition of neuronal Na+/K+-ATPase, leading to facilitation followed by neuromuscular blockade; and (3) blockade of voltage-dependent Ca2+ channels, leading to stabilization of the motor endplate membrane.

A novel C17N Lycopodium alkaloid (LA), lycoplanine B (1), containing an unusual formyl group, along with two new LAs, lycoplanines C (2) and D (3), were isolated from the whole plant of Lycopodium complanatum. Their structures were elucidated by extensive NMR techniques, including 1D- and 2D-NMR experiments, as well as comparing their spectral data with those of the known analogues. A possible biogenetic pathway for 1 was also proposed.Graphical Abstract

During a synthesis of coumarins to obtain new candidates for treating Alzheimer’s Disease (AD), an unusual rearrangement of a benzopyran group to a benzofuran group occurred, offering a novel synthesis pathway of these benzofuran derivatives. The possible mechanism of the novel rearrangement was also discussed. All of the benzofuran derivatives have weak anti-AChE activities compared with the reference compound, donepezil.

Seven new monoterpene phenyl ethers, namely micranthumnins A-G (1–7), were isolated from the stem bark of Illicium micranthum (Illiciaceae). Their structures were elucidated by comprehensive spectroscopic analyses including MS, IR, 1D and 2D NMR. All compounds were evaluated for their anti-AChE activities.