Microwave-assisted extraction of three bioactive alkaloids from Peganum harmala L. and their acaricidal activity against Psoroptes cuniculi in vitro.
Peganum harmala L. is a perennial herbaceous, glabrous plant that grows in semi-arid conditions, steppe areas and sandy soils. It is used to treat fever, diarrhoea, subcutaneous tumours, arthralgia, rheumatism, cough, amnesia and parasitic diseases in folk medicines. In this paper, we aimed to develop a simpler and faster method for the extraction of three alkaloids from Peganum harmala L. than other conventional methods by optimizing the parameters of a microwave-assisted extraction (MAE) method, and to investigate the acaricidal activities of three compounds against Psoroptes cuniculi.
After optimizing the operating parameters with the single factor experiment and a Box-Behnken design combined with a response-surface methodology, a MAE method was developed for extracting the alkaloids from the seeds, and a high-performance liquid chromatography was used to quantify these compounds. An in vitro experiments were used to study the acaricidal activities.
The optimal conditions of MAE method were as follows: liquid-to-solid ratio 31.3:1mL/g, ethanol concentration 75.5%, extraction time 10.1min, temperature 80.7°C, and microwave power 600W. Compared to the heat reflux extraction (HRE, 60min) and the ultrasonic-assisted extraction (UAE, 30min) methods, MAE method require the shortest time (10min) and obtain the highest yield of three compounds (61.9mg/g). Meanwhile, the LT50 values for the vasicine (1.25 and 2.5mg/mL), harmaline (1.25 and 2.5mg/mL), harmine (1.25 and 2.5mg/mL) and MAE extract (100mg/mL) against Psoroptes cuniculi were 12.188h, 9.791h, 11.994h, 10.095h, 11.293h, 9.273h and 17.322h, respectively.
The MAE method developed exhibited the highest extraction yield within the shortest time and thus could be used to extract the active compounds from Peganum harmala L. on an industrial basis. As the active compounds of Peganum harmala L., vasicine, harmalin and harmine presented the marked acaricidal activities against Psoroptes cuniculi, and could be widely applied for the treatments of acariasis in animals.
Shang X
，Guo X
，Li B
，Pan H
，Zhang J
，Zhang Y
，Miao X
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Evaluation of anti-amnesic effect of extracts of selected Ocimum species using in-vitro and in-vivo models.
Ocimum species are traditionally used for the treatment of anxiety, nerve pain, convulsions and a variety of neurodegenerative disorders. The present study was undertaken to evaluate the anti-amnesic effect of O. basilicum L., O. sanctum L. and O. gratissimum L. extracts using in-vitro and in-vivo models.
In-vitro acetylcholinesterase (AChE) inhibitory and antioxidant activities of hydro-methanol extracts of plants were evaluated using Ellman and DPPH and FRAP assays, respectively. The most active extract i.e. O. basilicum extract (OBE) was further explored for the possible anti-amnesic activity in mouse model of scopolamine induced amnesia using behavioral models (elevated plus maze and passive shock avoidance task). Brain AChE activity, oxidative profile and histopathological studies were assessed to outline the anti-amnesic mechanism of the extract.
Significant antioxidant and AChE inhibition activity was observed with all prepared extracts and however, OBE showed most marked free radical scavenging, reducing power and AChE inhibition (IC50 0.65±0.15mg/ml) activity. Basil leaves were standardized with respect to content of 7 phenolic acids using a HPLC-PDA method. A TLC densitometric method was employed to determine the quercetin content in the leaves. The in-vivo studies showed that OBE pre-treatment (200 and 400mg/kg, p.o.) reversed the memory deficit induced by scopolamine in mice, evident by significant (p<0.05) decrease in the transfer latency time and increase in step down latency in elevated plus maze and passive shock avoidance task, respectively. Moreover, OBE significantly reduced the brain AChE activity and oxidative stress. Further, histopathological examination of brain tissues displayed decrease in vacuolated cytoplasm and increase in pyramidal cells in hippocampal and cortical regions with OBE pre-treatment.
OBE possesses antioxidant and AChE inhibitory activity. These biochemical changes are responsible for the anti-amnesic and neuroprotective activities of O. basilicum which may be attributed to the presence of phenolic and flavonoid compounds. This can be developed as an effective anti-amnesic drug.
Singh V
，Kahol A
，Singh IP
，Saraf I
，Shri R
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Ameliorative effect of lotus seedpod proanthocyanidins on cognitive impairment and brain aging induced by D-galactose.
This study mainly investigated the ameliorative effect of lotus seedpod proanthocyanidins (LSPC) and the mechanism underlying such effect on cognitive impairment and brain aging induced by d-galactose. Aging mice induced by d-galactose (150 mg/kg, sc injection daily for 6 weeks) were chosen for the experiment. LSPCs (30, 60, and 90 mg/kg, ig) were provided after d-galactose injection. Learning and memory functions were detected by Y-maze and step-down avoidance tests. Then, some biochemical indexes related to cognitive ability and aging were measured. Histopathological feature and P53 protein expression in the hippocampus were observed. Results showed that the three different doses of LSPC could significantly ameliorate the learning and memory abilities impaired by d-galactose. LSPC significantly reduced the levels of malondialdehyde and nitric oxide (i.e. 90 mg/kg LSPC group vs. model group, P=0.008), reduced the content of β-amyloid peptide 1-42 (i.e. 90 mg/kg LSPC group vs. model group, P=0.009), decreased the activities of acetylcholinesterase, monoamine oxidase B, total nitric oxide synthase (i.e. 90 mg/kg LSPC group vs. model group, P=0.006), and neuronal nitric oxide synthase and synchronously increased the activities of superoxide dismutase and glutathione peroxidase in the brain. Furthermore, LSPC could prevent neuron damage and could lessen the expression of P53 protein in the hippocampus. These findings demonstrated that LSPC effectively attenuated cognitive damage and improved parameters related to brain aging in senescent mice induced by d-galactose, and may be used to treat Alzheimer's disease.
Gong YS
，Guo J
，Hu K
，Gao YQ
，Xie BJ
，Sun ZD
，Yang EN
，Hou FL
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beta-Carboline alkaloids in Peganum harmala and inhibition of human monoamine oxidase (MAO).
Peganum harmala L. is a multipurpose medicinal plant increasingly used for psychoactive recreational purposes (Ayahuasca analog). Harmaline, harmine, harmalol, harmol and tetrahydroharmine were identified and quantified as the main beta-carboline alkaloids in P. harmala extracts. Seeds and roots contained the highest levels of alkaloids with low levels in stems and leaves, and absence in flowers. Harmine and harmaline accumulated in dry seeds at 4.3% and 5.6% (w/w), respectively, harmalol at 0.6%, and tetrahydroharmine at 0.1% (w/w). Roots contained harmine and harmol with 2.0% and 1.4% (w/w), respectively. Seed extracts were potent reversible and competitive inhibitors of human monoamine oxidase (MAO-A) with an IC(50) of 27 microg/l whereas root extracts strongly inhibited MAO-A with an IC(50) of 159 microg/l. In contrast, they were poor inhibitors of MAO-B. Inhibition of MAO-A by seed extracts was quantitatively attributed to harmaline and harmine whereas inhibition by root extracts came from harmine with no additional interferences. Stems and leaves extracts were poor inhibitors of MAO. The potent inhibition of MAO-A by seed and root extracts of P. harmala containing beta-carbolines should contribute to the psychopharmacological and toxicological effects of this plant and could be the basis for its purported antidepressant actions.
Herraiz T
，González D
，Ancín-Azpilicueta C
，Arán VJ
，Guillén H
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