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Neuroprotective effects of Sophora secundiflora, Sophora tomentosa leaves and formononetin on scopolamine-induced dementia
Abstract
Five flavonoids were isolated from the ethyl acetate fraction of leaves of Sophora secundiflora; formononetin (1), 5-hydroxy-4’-methoxyflavone (2), genistein (3), 5-hydroxy-8-(1-hydroxy-1-methyl-ethyl)-2-(4-hydroxyphenyl)-4H-furo-[2, 3-h]-chromen-4-one (4) and ononin (5). Additionally, LC-ESI-MS/MS analysis of the ethyl acetate fraction of S. secundiflora leaves had led to tentative identification of eighteen compounds. Formononetin, S. tomentosa and S. secundiflora leaves methanolic extract were evaluated in vivo for their neuroprotective activity where formononetin and S. tomentosa showed promising neuroprotective activity with reduction in acetylcholine esterase (AchE) enzyme activity and elevation of acetylcholine (Ach) and glutathione(GSH) brain levels and attenuation of dopamine (DA), nor-adrenaline (NA) and malonedialdehyde (MDA) brain level significantly, However S. secundiflora leaves methanolic extract didn’t attenuate the AchE enzyme activity, DA and NA brain levels.
... The leaves of Sophora japonica (Fabaceae), known as Japanese pagoda, have been traditionally used as a haemostatic, hypotensive, detoxifying and anti-inflammatory agent as well [26,27]. The genus Sophora is known for its variety of secondary metabolites and biological activities [28,29]. The major secondary metabolites include flavonoids, isoflavonoids, triterpenoids and alkaloids [26,27,[30][31][32][33]. ...
... The results established the presence of higher concentrations of the total phenolics in G. glabra and higher flavonoids contents in S. japonica. The results revealed that S. japonica is a rich source with phenolics as compared to the other species, S. secundiflora and S. tomentosa, which showed phenolics contents of 18.01 and 4.72 mg/g of GAE, respectively [28]. ...
... Tentative metabolite identification was accomplished by extensive comparison of the UPLC-MS data from both extracts and the reported data [21,28,31,[37][38][39], as well as online databases. ...
Glycyrrhiza glabra and Sophora japonica (Fabaceae) are well-known medicinal plants with
valuable secondary metabolites and pharmacological properties. The flavonoid-rich fractions of
G. glabra roots and S. japonica leaves were prepared using Diaion column chromatography, and the
confirmation of flavonoid richness was confirmed using UPLC-ESI-MS profiling and total phenolics
and flavonoids assays. UPLC-ESI-MS profiling of the flavonoid-rich fraction of G. glabra roots
and S. japonica leaves resulted in the tentative identification of 32 and 23 compounds, respectively.
Additionally, the wound healing potential of topical preparations of each fraction, individually
and in combination (1:1) ointment and gel preparations, were investigated in vivo, supported by
histopathological examinations and biomarker evaluations, as well as molecular docking studies for
the major constituents. The topical application of G. glabra ointment and gel, S. japonica ointment and
gel and combination preparations significantly increase the wound healing rate and the reduction
of oxidative stress in the wound area via MDA reduction and the elevation of reduced GSH and
SOD levels as compared to the wound and Nolaver®-treated groups. The molecular docking study
revealed that that major compounds in G. glabra and S. japonica can efficiently bind to the active
sites of three proteins related to wound healing: glycogen synthase kinase 3-b (GSK3-b), matrix
metalloproteinases-8 (MMP-8) and nitric oxide synthase (iNOS). Consequently, G. glabra roots and
S. japonica leaves may be a rich source of bioactive metabolites with antioxidant, anti-inflammatory
and wound healing properties.
... [63] Apiaceae Carum carvi [64] Centella asiatica [65] Apocynaceae Catharanthus roseus [66,67] Araceae Arecha catechu [68] Araliaceae Panax gingseng [69] Asteraceae Artemisia absinthum [70] Bromeliaceae Ananas comosus [71] Cannabaceae Cannabis sativa [72] Cyperaceae Cyperus rotundus [73] Ericaceae Vaccinium myrtillus [74] Fabaceae Glycine max [75] Physostigma venenosum [76,77] Sophora sp. [78][79][80] Ginkgoceae Ginkgo biloba [17,[81][82][83] Hypericaceae Hypericum sp. [84][85][86][87][88] Iridaceae Crocus sativus [89] Lamiaceae Melissa officinalis [65,69,90] Rosmarinus officinalis Salvia officinalis ...
... In one research, S. tomentosa methanol extract and formononetin inhibited acetylcholine esterase enzyme activity and reduced acetylcholine and glutathione brain levels and dopamine, nor-adrenaline, and malondialdehyde brain levels. Methanol extracts of S. secundiflora, on the other hand, had no significant impact [78,79]. ...
Alzheimer’s disease accounts for high percentages of dementia cases in elderly individuals. This type of brain disease is caused by damage of the brain cells affecting the ability of the patients to communicate, as well as their thinking, behavior, and feelings. Although numerous research laboratories focus on advancements for the treatment of Alzheimer’s disease, the currently approved pharmacological approaches seem to only alleviate the symptoms. Consequently, there is an urgent need for alternative pharmacological options which can prevent the progressive impairment of neurons. Natural substances were used from ancient times for the treatment of various disorders given their biological activities such as antioxidant, anti-inflammatory, and antiapoptotic properties. Besides, their cost-effectiveness as well as their accessibility to anyone who needs them, are their most significant characteristics. Therefore, the possible use of phytochemical compounds for the possible management or even prevention of Alzheimer’s disease is currently under investigation. In this review article, the present status of Alzheimer’s disease diagnosis and underlying mechanisms, the potential phytochemicals, and their carriers along with future perspectives are summarized. It is suggested that in the future natural substances can play a role as an adjunct therapy for neurodegenerative forms of dementia, such as Alzheimer’s disease.
... The adverse effects linked to anti-TB drugs prompted drug researchers to shift their focus toward natural alternatives [12][13][14][15]. Medicinal plants have garnered significant global interest due to their diverse biological activities and potential applications in various diseases [16][17][18][19]. This has led the scientific community to explore their potential as novel drug candidates for preventing and treating the ranges of toxicity associated with diseases, including tuberculosis [20][21][22]. ...
Citation: Abdel-Hameed, U.K.; Abualghaith, A.S.; Aly, S.H.; Soliman, M.M.; Munshi, L.A.; Mohammed, S.A.A.; Eldahshan, O.A.; Abdelghffar, E.A.R. GC/MS Analysis and Protective Effects of Mentha longifolia (Linnaeus) L. Essential Oil Against Antituberculosis Drug-Induced Organs Toxicity in Wistar Albino Rats. Plants 2024, 13, 3231. https://doi. Abstract: Mentha longifolia (L.) L., also known as wild mint, is a perennial herbaceous plant that belongs to the Lamiaceae family. This study aimed to investigate the effects of essential oil of M. longifolia (MLEO) on oxidative stress and inflammatory responses in the liver and kidneys in the context of drug-induced liver injury caused by the anti-TB drugs rifampicin, isoniazid, and pyrazinamide (INH-RIF-PZA). The chemical composition of MLEO was characterized using GC/MS analysis, which revealed the presence of pulegone, trans-p-menthan-3-one, piperitenone, and β-caryophyllene as its major volatile constituents. An INH/RIF/PZA mixture was administered to Wistar rats for 30 days, and silymarin was administered as a standard drug. MLEO was administered p.o. at doses of 50 mg and 100 mg/kg b.w. Both doses of the MLEO therapy effectively regulated all biochemical indicators of hepatic impairment and reduced the damage caused by the INH/RIF/PZA mixture. It may be deduced that MLEO has the ability to protect organs against INH/RIF/PZA-induced damage and could potentially be a valuable natural remedy for treating anti-TB-induced liver and kidney injuries.
... The results of previous studies have demonstrated the neuroprotective effects of FMN [17,[24][25][26], though its effects on PD remain unclear. To explore the predicted effects and targets of FMN in PD, we screened 2059 PD-related targets using the GeneCards and OMIM databases. ...
Parkinson’s disease (PD) is a prevalent neurodegenerative disease for which no effective treatment currently exists. In this study, we identified formononetin (FMN), a neuroprotective component found in herbal medicines such as Astragalus membranaceus and Glycyrrhiza uralensis, as a potential agent targeting multiple pathways involved in PD. To investigate the anti-PD effects of FMN, we employed Caenorhabditis elegans (C. elegans) PD models, specifically the transgenic strain NL5901 and the MPP(+)-induced strain BZ555, to investigate the effects of FMN on the key pathological features of PD, including dyskinesia, dopamine neuron damage, and reactive oxygen species (ROS) accumulation. The MPP(+)-induced SH-SY5Y cell PD model was utilized to evaluate the effects of FMN on cell viability, ROS accumulation, and mitochondrial dysfunction. The signaling pathway induced by FMN was analyzed using transcriptomic techniques and subsequently validated in vitro. Our results indicate that FMN significantly reduced ROS accumulation and improved both dopaminergic neuron vitality and dyskinesia in the C. elegans PD models. In the cell PD model, FMN significantly reduced ROS accumulation and enhanced mitochondrial membrane potential (MMP) and cell viability. A transcriptomic analysis suggested that the effects of FMN are associated with Nrf2 activation. Furthermore, ML385, a specific Nrf2 inhibitor, blocked the beneficial effects of FMN in vitro, indicating that FMN ameliorates dyskinesia and protects dopaminergic neurons through Nrf2 signaling pathway activation. In addition, the effects of FMN on ameliorating dyskinesia and protecting dopamine neurons were comparable to those of the Nrf2 agonist of sulforaphane (SFN) in vivo. The results of this study confirm that FMN exerts significant anti-PD effects primarily through the Nrf2 signaling pathway. These findings provide crucial insights for the development of anti-PD therapies.
... Phytochemicals, antioxidant properties, and hepatoprotective potential of Moricandia sinaica leaves type of secondary metabolites, possess numerous biological activities such as antioxidant, cytotoxic, antidiabetic, and anti-inflammatory effects [63][64][65]. The methanol extract of M. sinaica leaves exhibited total phenolics and total flavonoid contents corresponding to 59.37 ± 2.19 mgGAE/g and 38.94 ± 2.72 mgQE/g, respectively. ...
Thirteen components were identified in the methanol extract of Moricandia sinaica leaves (MSLE) through analysis utilizing HPLC-ESI-MS/MS., including flavonoids, anthocyanins, phenolic acids, and fatty acids. The methanol extract of M. sinaica leaves contained total phenolics and flavonoids (59.37 ± 2.19 mg GAE/g and 38.94 ± 2.72 mg QE/g), respectively. Furthermore, it revealed in vitro antioxidant properties as determined by the DPPH and FRAP assays, with respective IC50 values of 10.22 ± 0.64 and 20.89 ± 1.25 μg/mL. The extract exhibited a notable hepatoprotective effect in rats who experienced paracetamol-induced hepatotoxicity. When a dose of 250 mg/kg was given, there was a 52% reduction in alanine transaminase and a 30% reduction in aspartate transaminase compared to the group with the disease. Furthermore, it demonstrated a 3.4-fold, 2.2-fold, and 2.6-fold increase in superoxide dismutase, non-protein sulfhydryl, and glutathione peroxidase, respectively. In addition, it demonstrated a 68% decrease in lipid peroxide levels compared to the group with paracetamol-induced condition. The verification was conducted using a histological study, which identified improved liver histology with a small number of distended hepatocytes. Moreover, in silico studies focused on the enzymes NADPH oxidase, butyrylcholinesterase, and tyrosinase as the targets for the major compounds. In conclusion, MSLE showed promising hepatoprotective and antioxidant activities due to its richness in antioxidant metabolites.
... The HPLC chromatogram of T. pratense ethanolic extract at 254 nm is shown in Figure 1. Four major peaks were identified as ononin 1) (Lewis et al., 1998), sissotrin 2) (Lewis et al., 1998), formononetin 3) (Aly et al., 2020), and biochanin A 4) (Wang et al., 2019), respectively, based on our data of MS and 1 H NMR spectrometry analyses and compared to the published references. The HPLC profile and the 4 index compounds were used to ensure the batch-to-batch consistency of the TP plant and extracts in the supplementation feeds. ...
Coccidiosis, caused by a protozoan parasite of the genus Eimeria, is one of the most severe contagious parasite diseases affecting the poultry industry worldwide. Using phytogenics to prevent chicken coccidiosis is a strategy aimed at combating the increasing issue of drug-resistant strains of Eimeria spp. This study demonstrates the anticoccidial activities of a medicinal herb, Trifolium pratense (TP) powder, and its ethanolic extract (designated TPE) against Eimeria spp. TPE exhibited significant suppressive activity against E. maxima oocyst sporulation and E. tenella sporozoite invasion and reproduction in Madin-Darby bovine kidney cells. Furthermore, administration of basal chicken diets containing TP powder or TPE to Eimeria-infected chickens significantly reduced the output of oocysts and severity of intestinal lesions. Dietary supplementation with TP significantly improved relative weight gain in E. tenella- and E. acervulina-infected chickens, while there was no significant improvement in E. maxima-infected chickens. The anticoccidial activities of TP and TPE on E. acervulina, E. tenella and E. maxima were further supported by anticoccidial index scores, which showed greater efficacy than those of amprolium, a commercial coccidiostat used in poultry. TP supplementation positively impacted the primary metabolism of chickens challenged with E. tenella or E. acervulina. The chemical fingerprints of TPE were established using liquid column chromatography; TPE contained 4 major compounds: ononin, sissotrin, formononetin, and biochanin A. In addition, various spectrometric methods were used to ensure the batch-to-batch consistency of TP/TPE. In conclusion, T. pratense is demonstrated to be a novel phytogenic supplement that can be used to control Eimeria-induced coccidiosis in chickens.
... Firstly, the cholinergic hypothesis is explained by the progressive decline in the acetylcholine (Ach) neurotransmitter which is responsible for neuronal activity, plasticity, and network connectivity. This major concern in acetylcholine level occurs due to the degeneration of cholinergic neurons, appearance of cholinergic lesions, or overactivity of acetylcholinesterase enzyme (AchE) that subsequently leads to the depletion of the level of Ach [6,7]. Secondly, the deposition of Aβ plaques is one of the hallmarks of Alzheimer's disease pathogenesis that causes brain structure abnormalities [2,8]. ...
Background
Alzheimer’s disease is a neurodegenerative age-related disease that primarily affects the elderly population leading to progressive memory impairments and neural deficits. It is counted as a major cause of geriatric dependency and disability. The pathogenesis of Alzheimer’s disease incidence is complex and involves various hypotheses, including the cholinergic hypothesis, deposition of β-amyloid plaques, neuroinflammation, oxidative stress, and apoptosis. Conventional treatments such as donepezil aim to delay the symptoms but do not affect the progression of the disease and may cause serious side effects like hepatoxicity. The use of natural candidates for Alzheimer’s disease treatment has drawn the attention of many researchers as it offers a multitargeted approach.
Methods
This current study investigates the metabolic profiles of total defatted methanolic extract of Vitex pubescens bark and its polar fractions, viz. ethyl acetate and n-butanol, using ultra-performance liquid chromatography-electrospray ionization-quadrupole time-of-flight tandem mass spectrometry(UPLC-ESI-QTOF/MS/MS) technique as well as evaluate the antioxidant using free radical scavenging assays, viz. DPPH and ABTS assays and in-vitro acetylcholinesterase inhibitory activities using Ellman’s microplate assay.
Results
Metabolic profiling revealed a total of 71, 43, and 55 metabolites tentatively identified in the defatted methanolic extract, ethyl acetate, and n-butanol fractions, respectively. Phenolic acids were the most abundant class, viz. benzoic acids, and acyl quinic acid derivatives followed by flavonoids exemplified mainly by luteolin-C-glycosides and apigenin-C-glycosides. Quantification of the total phenolic and flavonoid contents in the total defatted methanolic extract confirmed its enrichment with phenolics and flavonoids equivalent to 138.61 ± 9.39 µg gallic acid/mg extract and 119.63 ± 4.62 µg rutin/mg extract, respectively. Moreover, the total defatted methanolic extract exhibited promising antioxidant activity confirmed through DPPH and ABTS assays with a 50% inhibitory concentration (IC50) value equivalent to 52.79 ± 2.16 µg/mL and 10.02 ± µg/mL, respectively. The inhibitory activity of acetylcholine esterase (AchE) was assessed using in-vitro Ellman’s colorimetric assay, the total defatted methanolic extract, ethyl acetate, and n-butanol fractions exhibited IC50 values of 52.9, 15.1 and 108.8 µg/mL that they proved the significant inhibition of AchE activity.
Conclusion
The results obtained herein unraveled the potential use of the total methanolic extract of Vitex pubescens bark and its polar fractions as natural candidates for controlling Alzheimer’s disease progression.
... A round-shaped, non-woven, uniform, beads-free and well-oriented nanofibers of smooth surface were obtained at an average diameter of 300 ± 50 nm. Besides, their medicinal and therapeutic efficacy plays an important role in development of natural treatments of various diseases [32,33]. The total phenolic content and total flavonoid content values were obtained from the calibration curve of gallic acid (y = 0.0042× -0.0293 with R 2 = 0.9991) and rutin (y = 0.002× -0.0138 with R 2 = 0.998) where x is the absorbance and y is the concentration of gallic acid and rutin solution (μg/mL), respectively (Fig. S1, Supplementary Materials). ...
... Formononetin (FORM) is a phytoestrogen isoflavone that demonstrated a wide range of physiological activities that benefit health via estrogen-dependent and independent pathways (Machado Dutra et al., 2021). FORM was isolated from S. secundiflora and S. flavescens (Jiang et al., 2019;Aly et al., 2021b). An in vivo study compared the therapeutic potency of three phytoestrogens, including genistein, daidzein, and FORM. ...
Bone metabolism is characterized by an interplay between the deposition of bone matrix and mineralization and the resorption process. Osteoporosis is a form of systemic metabolic bone condition that causes bone density to decline and its microarchitecture to deteriorate, increasing the risk of fracture owing to fragility. The underlying cause of this clinical disease lies in the imbalance in bone remodeling, in which bone resorption by osteoclasts predominates over bone creation by osteoblasts. Natural remedies have long been used to cure and prevent osteoporosis. Genus Sophora of the Fabaceae family comprises about 69 species that showed many pharmacological effects, including bone health preservation. The activity of Sophora sp. in maintaining bone health was attributed to its antioxidant, regenerative, and anti-inflammatory qualities. In this review, we focused on the therapeutic properties of the extracts and isolated compounds from the genus Sophora in maintaining bone health, with special emphasis on the management of osteoporosis.
... Moreover, the interaction of probiotic bacteria with epithelial cell surface receptors can stimulate the production of cytokines, affecting the performance of mucosal lymphocytes [9,10]. Bioactive secondary metabolites can be sourced from plants and used to develop new natural products with properties such as antiviral, antioxidant, anti-inflammatory, and cytotoxic effects, making them valuable resources in the treatment of various diseases [11][12][13][14]. ...
... Moreover, the interaction of probiotic bacteria with epithelial cell surface receptors can stimulate the production of cytokines, affecting the performance of mucosal lymphocytes [9,10]. Bioactive secondary metabolites can be sourced from plants and used to develop new natural products with properties such as antiviral, antioxidant, anti-inflammatory, and cytotoxic effects, making them valuable resources in the treatment of various diseases [11][12][13][14]. ...
... Moreover, the interaction of probiotic bacteria with epithelial cell surface receptors can stimulate the production of cytokines, affecting the performance of mucosal lymphocytes [9,10]. Bioactive secondary metabolites can be sourced from plants and used to develop new natural products with properties such as antiviral, antioxidant, anti-inflammatory, and cytotoxic effects, making them valuable resources in the treatment of various diseases [11][12][13][14]. ...
Background
The emergence of different viral infections calls for the development of new, effective, and safe antiviral drugs. Glycyrrhiza glabra is a well-known herbal remedy possessing antiviral properties.
Objective
The objective of our research was to evaluate the effectiveness of a newly developed combination of the probiotics Lactobacillus acidophilus and G. glabra root extract against two viral models, namely the DNA virus Herpes simplex virus-1 (HSV-1) and the RNA virus Vesicular Stomatitis Virus (VSV), with regards to their antiviral properties.
Methodology
To examine the antiviral impacts of various treatments, we employed the MTT assay and real-time PCR methodology.
Results
The findings of our study indicate that the co-administration of L. acidophilus and G. glabra resulted in a significant improvement in the survival rate of Vero cells, while also leading to a reduction in the titers of Herpes Simplex Virus Type 1 (HSV-1) and Vesicular Stomatitis Virus (VSV) in comparison to cells that were not treated. Additionally, an investigation was conducted on glycyrrhizin, the primary constituent of G. glabra extract, utilizing molecular docking techniques. The results indicated that glycyrrhizin exhibited a greater binding energy score for HSV-1 polymerase (− 22.45 kcal/mol) and VSV nucleocapsid (− 19.77 kcal/mol) in comparison to the cocrystallized ligand (− 13.31 and − 11.44 kcal/mol, respectively).
Conclusions
The combination of L. acidophilus and G. glabra extract can be used to develop a new, natural antiviral agent that is safe and effective.
... For millennia, the spotlight has been directed toward medicinal plants as a plentiful supply of bioactive compounds, and many of the therapeutic medications currently in use are natural products or compounds derived from plants [1][2][3][4][5]. According to the World Health Organization (WHO), about 80% of the world's population lives in developing and underdeveloped countries and relies on medicines of natural origin as a remedy for medical ailments [6]. ...
The genus Moricandia (Brassicaceae) comprises about eight species that were used in traditional medicine. Moricandia sinaica is used to alleviate certain disorders such as syphilis and exhibits analgesic, anti-inflammatory, antipyretic, antioxidant, and antigenotoxic properties. Throughout this study, we aimed to figure out the chemical composition of lipophilic extract and essential oil obtained from M. sinaica aerial parts using GC/MS analysis, as well as their cytotoxic and antiox-idant activities correlated with the major detected compounds' molecular docking. The results revealed that both the lipophilic extract and the oil were found to be rich in aliphatic hydrocarbons , accounting for 72.00% and 79.85%, respectively. Furthermore, the lipophilic extract's major constituents are octacosanol, γ-sitosterol, α-amyrin, β-amyrin acetate, and α-tocopherol. Contrarily, monoterpenes and sesquiterpenes accounted for the majority of the essential oil. The essential oil and the lipophilic extract of M. sinaica showed cytotoxic properties towards human liver cancer cells (HepG2) with IC 50 values of 126.65 and 220.21 µg/mL, respectively. The lipophilic extract revealed antioxidant activity in the DPPH assay with an IC 50 value of 2679 ± 128.13 µg/mL and in the FRAP assay, moderate antioxidant potential was expressed as 44.30 ± 3.73 µM Trolox equivalent/mg sample. The molecular docking studies revealed that β-amyrin acetate, α-tocopherol, γ-sitosterol, and n-pentacosaneachieved the best docking scores for NADPH oxidase, phosphoinositide-3 kinase, and protein kinase B. Consequently, M. sinaica essential oil and lipophilic extract can be employed as a viable management strategy for oxidative stress conditions and the formulation of improved cytotoxic treatment regimens.
... Eighteen compounds were identified in the leaf extracts of Sophora secundiflora and Sophora tomentosa using LC-ESI-MS/MS analysis. In vivo investigations revealed promising neuroprotective benefits by lowering AChE, nor-adrenaline, and dopamine levels and increasing glutathione and acetylcholine levels [21]. Eugenol, β-elemene, eugenyl acetate, and methyl eugenol were found in essential-oil fractions of Piper divaricatum and were found to have strong inhibitory effects against AChE [22]. ...
Neurodegenerative disorders encompass a wide range of pathological conditions caused by progressive damage to the neuronal cells and nervous-system connections, which primarily target neuronal dysfunction and result in problems with mobility, cognition, coordination, sensation, and strength. Molecular insights have revealed that stress-related biochemical alterations such as abnormal protein aggregation, extensive generation of reactive oxygen and nitrogen species, mitochondrial dysfunction, and neuroinflammation may lead to damage to neuronal cells. Currently, no neurodegenerative disease is curable, and the available standard therapies can only provide symptomatic treatment and delay the progression of the disease. Interestingly, plant-derived bioactive compounds have drawn considerable attention due to their well-established medicinal properties, including anti-apoptotic, antioxidant, anti-inflammatory, anticancer, and antimicrobial properties, as well as neuroprotective, hepatoprotective, cardioprotective, and other health benefits. Plant-derived bioactive compounds have received far more attention in recent decades than synthetic bioactive compounds in the treatment of many diseases, including neurodegeneration. By selecting suitable plant-derived bioactive compounds and/or plant formulations, we can fine tune the standard therapies because the therapeutic efficacy of the drugs is greatly enhanced by combinations. A plethora of in vitro and in vivo studies have demonstrated plant-derived bioactive compounds’ immense potential, as proven by their capacity to influence the expression and activity of numerous proteins implicated in oxidative stress, neuroinflammation, apoptosis, and aggregation. Thus, this review mostly focuses on the antioxidant, anti-inflammatory, anti-aggregation, anti-cholinesterase, and anti-apoptotic properties of several plant formulations and plant-derived bioactive compounds and their molecular mechanisms against neurodegenerative disorders.
... The spray voltage was 4.48 kV, the tube lens voltage was 10.00 V, and the capillary voltage was 39.6 V. A full scan mode was adjusted in the mass range of 100-2000 m/z [64]. ...
Culex pipiens mosquitoes are transmitters of many viruses and are associated with the transmission of many diseases, such as filariasis and avian malaria, that have a high rate of mortality. The current study draws attention to the larvicidal efficacy of three methanolic algal extracts, Cystoseira myrica, C. trinodis, and C. tamariscifolia, against the third larval instar of Cx. pipiens. The UPLC-ESI-MS analysis of three methanol fractions of algal samples led to the tentative characterization of twelve compounds with different percentages among the three samples belonging to phenolics and terpenoids. Probit analysis was used to calculate the lethal concentrations (LC 50 and LC 90). The highest level of toxicity was attained after treatment with C. myrica extract using a lethal concentration 50 (LC 50) of 105.06 ppm, followed by C. trinodis (135.08 ppm), and the lowest level of toxicity was achieved by C. tamariscifolia (138.71 ppm) after 24 h. The elevation of glutathione-S-transferase (GST) and reduction of acetylcholine esterase (AChE) enzymes confirm the larvicidal activity of the three algal extracts. When compared to untreated larvae, all evaluated extracts revealed a significant reduction in protein, lipid, and carbohydrate contents, verifying their larvicidal effectiveness. To further support the observed activity, an in silico study for the identified compounds was carried out on the two tested enzymes. Results showed that the identified compounds and the tested enzymes had excellent binding affinities for each other. Overall, the current work suggests that the three algal extractions are a prospective source for the development of innovative, environmentally friendly larvicides.
... Recently, there has been a great demand for the development of natural products to cure different conditions owing to their safety, availability, versatile biological activities, and unique secondary metabolites [27][28][29][30][31]. Consequently, the exploration of medicinal plants as new candidates for wound healing would be valuable and beneficial, especially medicinal plants that are characterised by biocompatibility, wound healing, and anti-inflammatory properties [22,23,32,33]. ...
The chemical composition of the n-hexane extract of Tamarindus indica's various organs-bark, leaves, seeds, and fruits (TIB, TIL, TIS, TIF)-was investigated using gas chromatography-mass spectrometry (GC/MS) analysis. A total of 113 metabolites were identified, accounting for 93.07, 83.17, 84.05, and 85.08 % of the total identified components in TIB, TIL, TIS, and TIF, respectively. Lupeol was the most predominant component in TIB and TIL, accounting for 23.61 and 22.78%, respectively. However, n-Docosanoic acid (10.49%) and methyl tricosanoate (7.09%) were present in a high percentage in TIS. However, α-terpinyl acetate (7.36%) and α-muurolene (7.52%) were the major components of TIF n-hexane extract. By applying a principal component analysis (PCA) and hierarchal cluster analysis (HCA) to GC/MS-based metabolites, a clear differentiation of Tama-rindus indica organs was achieved. The anti-inflammatory activity was evaluated in vitro on lipo-polysaccharide (LPS)-induced RAW 264.7 macrophages. In addition, the wound healing potential for the n-hexane extract of various plant organs was assessed using the in-vitro wound scratch assay using Human Skin Fibroblast cells. The tested extracts showed considerable anti-inflammatory and wound-healing activities. At a concentration of 10 µg/mL, TIL showed the highest nitric oxide (NO) inhibition by 53.97 ± 5.89%. Regarding the wound healing potential, after 24 h, TIB, TIL, TIS, and TIF n-hexane extracts at 10 g/mL reduced the wound width to 1.09 ± 0.04, 1.12 ± 0.18, 1.09 ± 0.28, and 1.41 ± 0.35 mm, respectively, as compared to the control cells (1.37 ± 0.15 mm). These findings showed that the n-hexane extract of T. indica enhanced wound healing by promoting fibroblast migration. Additionally, a docking study was conducted to assess the major identified phytoconstitu-ents' affinity for binding to glycogen synthase kinase 3-β (GSK3-β), matrix metalloproteinases-8 (MMP-8), and nitric oxide synthase (iNOS). Lupeol showed the most favourable binding affinity to GSK3-β and iNOS, equal to −12.5 and −13.7 Kcal/mol, respectively, while methyl tricosanoate showed the highest binding affinity with MMP-8 equal to −13.1 Kcal/mol. Accordingly, the n-hexane extract of T. indica's various organs can be considered a good candidate for the management of wound healing and inflammatory conditions. Citation: Aly, S.H.; El-Hassab, M.A.; Elhady, S.S.; Gad, H.A. Comparative Metabolic Study of Tamarindus indica
... Phenolics compounds are present in most natural products that induce many biological activities [41][42][43][44]. The total phenolic and flavonoid content in the n-hexane extract of P. guajava leaves, was quantitatively determined, according to Zengin and Aktumsek, 2014 [45]. ...
Psidium guajava (Guava tree) is one of the most widely known species in the family Myrtaceae. The Guava tree has been reported for its potential antioxidant, anti-inflammatory, antimicrobial, and cytotoxic activities. In the current study, the chemical compositions of the n-hexane extract and the essential oil of P. guajava were investigated using the GC/MS analysis, along with an evaluation of their antioxidant potential, and an investigation into the enzyme inhibition of acetylcholinesterase (AChE), butyrylcholinesterase (BchE), tyrosinase, α-amylase, and α-glucosidase. Moreover, molecular docking of the major identified active sites of the target enzymes were investigated. The chemical characterization of the n-hexane extract and essential oil revealed that squalene (9.76%), α-tocopherol (8.53%), and γ-sitosterol (3.90%) are the major compounds in the n-hexane extract. In contrast, the major constituents of the essential oil are D-limonene (36.68%) and viridiflorol (9.68%). The n-hexane extract showed more antioxidant potential in the cupric reducing antioxidant capacity (CUPRAC), the ferric reducing power (FRAP), and the metal chelating ability (MCA) assays, equivalent to 70.80 ± 1.46 mg TE/g, 26.01 ± 0.97 mg TE/g, and 24.83 ± 0.35 mg EDTAE/g, respectively. In the phosphomolybdenum (PM) assay, the essential oil showed more antioxidant activity equivalent to 2.58 ± 0.14 mmol TE/g. The essential oil demonstrated a potent BChE and tyrosinase inhibitory ability at 6.85 ± 0.03 mg GALAE/g and 61.70 ± 3.21 mg KAE/g, respectively. The α-amylase, and α-glucosidase inhibitory activity of the n-hexane extract and the essential oil varied from 0.52 to 1.49 mmol ACAE/g. Additionally, the molecular docking study revealed that the major compounds achieved acceptable binding scores upon docking with the tested enzymes. Consequently, the P. guajava n-hexane extract and oil can be used as a promising candidate for the development of novel treatment strategies for oxidative stress, neurodegeneration, and diabetes mellitus diseases.
... Further research revealed that formononetin inhibited the elevation of dopamine (DA), norepinephrine (NA) and malondialdehyde (MDA) levels, reduction of glutathione (GSH) and acetylcholine (ACh) levels, enhancement of acetylcholinesterase (AChE) activity in the brain of scopolamine-treated mice. Formononetin seemed to play a neuroprotective role in scopolamine-induced dementia through regulating brain AChE activity and suppressing oxidative stress (Aly et al., 2021). Diabetes is a risk factor for the dysfunction of nervous system. ...
Nervous system is the most complex system of the human body, hence, the neurological diseases often lack effective treatment strategies. Natural products have the potential to yield unique molecules and produce integrative and synergic effects compared to standard therapy. Mounting evidence has shown that isoflavonoids contained in traditional medicinal plant or dietary supplementation may play a crucial role in the prevention and treatment of neurological diseases due to their pronounced biological activities correlating to nervous system. Formononetin, a non-steroidal isoflavonoid, is a bioactive constituent of numerous medicinal plants such as red clover (Trifolium pratense) and Astragalus membranaceus. Emerging evidence has shown that formononetin possesses considerable anti-inflammatory, antioxidant and anti-cancer effects. This review intends to analyze the neuropharmacological potential of formononetin on the therapy of nervous system disorders. The neuroprotective properties of formononetin are observed in multiple neurological disorders including Alzheimer’s disease, dementia, cerebral ischemia, traumatic brain injury, anxiety, and depression. The beneficial effects of formononetin are achieved partially through attenuating neuroinflammation and oxidative stress via the related signaling pathway. Despite its evident effects in numerous preclinical studies, the definite role of formononetin on humans is still less known. More well-designed clinical trials are required to further confirm the neuroprotective efficacy and safety profile of formononetin before its application in clinic.
... The acetylcholinesterase enzyme is responsible for the hydrolysis of acetylcholine, which is considered a key enzyme in the treatment of Alzheimer's disease. Several plants have been reported for their inhibitory activity against acetylcholinesterase [33][34][35]. The essential oil of S. cumini showed moderate inhibitory ability against AChE with an IC 50 value of 32.90 ± 2.10 µg/mL as compared to donepezil (IC 50 = 7.89 ± 1.30 µg/mL) as a reference drug. ...
Syzygium cumini (Pomposia) is a well-known aromatic plant belonging to the family Myrtaceae, and has been reported for its various traditional and pharmacological potentials, such as its antioxidant, antimicrobial, anti-inflammatory, and antidiarrheal properties. The chemical composition of the leaf essential oil via gas chromatography–mass spectrometry (GC/MS) analysis revealed the identification of fifty-three compounds representing about 91.22% of the total oil. The identified oil was predominated by α-pinene (21.09%), followed by β-(E)-ocimene (11.80%), D-limonene (8.08%), β-pinene (7.33%), and α-terpineol (5.38%). The tested oil revealed a moderate cytotoxic effect against human liver cancer cells (HepG2) with an IC50 value of 38.15 ± 2.09 µg/mL. In addition, it effectively inhibited acetylcholinesterase with an IC50 value of 32.9 ± 2.1 µg/mL. Furthermore, it showed inhibitory properties against α-amylase and α-glucosidase with IC50 values of 57.80 ± 3.30 and 274.03 ± 12.37 µg/mL, respectively. The molecular docking studies revealed that (E)-β-caryophyllene, one of the major compounds, achieved the best docking scores of −6.75, −5.61, and −7.75 for acetylcholinesterase, α-amylase, and α-glucosidase, respectively. Thus, it is concluded that S. cumini oil should be considered as a food supplement for the elderly to enhance memory performance and for diabetic patients to control blood glucose.
... Among these flavonoids, formononetin (4-Omethyl ether of daidzein) and ononin (formononetin-7-O-glucoside) are valuable therapeutic isoflavonoids (Fig. 1). Both these substances have demonstrated anti-proliferative effects in cancer cells (Wu et al., 2015) and neuroprotective (Aly et al., 2020), estrogenic (Spagnuolo et al., 2014), antidiabetic (Guo et al., 2020), cholesterol-lowering (Clifton-Bligh et al., 2015), antioxidant and anti-inflammatory (Bottamedi et al., 2021) activities. ...
Licorice is an herbal plant in the Leguminosae family, and its roots and rhizomes are used as sweeteners in food and confectionery products. Moreover, it has a distinct inflammatory activity. In the present study, a sample pre‐treatment method to induce the deglycosylation of active metabolites in callus cultures of Glycyrrhiza inflata (GI) and Glycyrrhiza glabra (GG) was developed. The results of the method evaluation showed the biotransformation of ononin to formononetin, a rare flavonoid found in trace amounts in licorice. The magnitude of enhancement was 3‐ and 19‐fold in the GI and GG samples, respectively. Moreover, the anti‐inflammatory activity assay showed that the potency of the sample pre‐treatment group was higher than that of the untreated group because it exerted an enhanced suppression of cyclo‐oxygenase 2 (COX‐2), interleukin‐6 (IL‐6) and inducible nitric oxide synthase (iNOS) gene expression. This is the first report on the anti‐inflammatory activity of licorice callus, which has the potential to be utilised as a functional food for health promotion. These findings support the idea of using sample preparation to impart nutraceutical properties to plant products.
Herbal Medicine for Autoimmune Diseases addresses the immune system's role in autoimmune conditions and introduces evidence-based herbal therapies for diseases like lupus, diabetes, rheumatoid arthritis, and more. Chapters highlight innovative approaches such as phyto-nanotechnology for enhanced drug delivery and the therapeutic benefits of berry fruits. Readers will gain insights into bioactive compounds, their efficacy in clinical settings, and the integration of traditional wisdom with contemporary research. Ideal for students, researchers, and pharmaceutical professionals, this book bridges the gap between ancient remedies and cutting-edge healthcare solutions, offering a valuable resource for understanding and managing autoimmune disorders. Key Features: - Detailed exploration of herbal treatments for specific autoimmune diseases. - Integration of phyto-nanotechnology for advanced drug delivery systems. - Evidence-based insights supported by preclinical and clinical research. - Practical implications for academia, pharmaceutical research, and clinical practice.
Breast cancer’s complexity and heterogeneity continue to present significant challenges in its treatment and management. Emerging research has underscored the pivotal role of microRNAs (miRNAs) in breast cancer pathogenesis, acting as crucial regulators of gene expression. This review delivers an in-depth analysis of miRNAs, highlighting their dual functions as both oncogenes and tumor suppressors, and detailing their impact on key biological processes, including cell proliferation, apoptosis, and metastasis. The mechanisms underlying miRNA action, particularly their interactions with target mRNAs and the factors influencing these dynamics, are thoroughly explored. Additionally, the review discusses the therapeutic prospects of miRNAs, with a focus on innovative delivery systems like nanoparticles that improve the stability and effectiveness of miRNA-based therapies. It also addresses the anticancer effects of natural compounds, such as genistein, hesperidin, quercetin, curcumin, resveratrol, epigallocatechin-3-gallate (EGCG), and glyceollins, which modulate miRNA expression and contribute to tumor growth inhibition. These advances seek to address the limitations of conventional therapies, paving the way for targeted interventions in breast cancer. By integrating current insights on miRNA biology, therapeutic strategies, and the potential of natural products to regulate miRNA expression, this review aims to shed light on miRNA- and natural product-based approaches as promising avenues for enhancing breast cancer treatment outcomes.
Background: Stress is an aversive stimulus that disrupts the organism's biological balance. Formononetin, an isoflavone, has been implicated in anxiolytic responses. However, the intra-hypothalamic molecular mechanisms by which formononetin controls stress remain unknown. Objectives: This study aimed to investigate the impact of formononetin on hypothalamic Mch and Crh gene expression in a rat model of stress. Methods: Male Wistar rats (200 - 220 g) were used. Thirty minutes before exposure to stress, the rats were injected with either saline or formononetin. Two hours after stress induction, hypothalamic samples were dissected and stored at -70°C until the measurement of Mch and Crh gene expression using real-time PCR. Results: Stress induction led to a significant increase in Mch and Crh mRNA levels. However, animals receiving formononetin showed a significant reduction in Mch and Crh mRNA levels compared to the stressed rats. Conclusions: Formononetin may exert anxiolytic effects by down-regulating intra-hypothalamic CRH and MCH signaling pathways.
The leaf extract of Alnus rugosa (AR) together with the isolated compound baicalein
5,6‐dimethyl ether (BME) were investigated for their antioxidant, radical scavenging,
antiaging, and neuroprotective properties using the Caenorhabditis elegans model.
The stress resistance and antiaging potential of AR and BME were assessed in wildtype
N2 and transgenic C. elegans strains CF1553, TJ356, and BA17. Transgenic
CL4176 expressing the human amyloid‐beta peptide (Aβ) was used as a model for Aβ
toxicity, whereas transgenic AM141 expressing polyQ aggregates was employed as a
model for Huntington's disease. An in silico molecular docking study using Discovery
Studio 4.5 was performed to elucidate the putative binding mode of BME to the
active sites of Daf‐2 protein, involved in longevity and oxidative stress resistance in
C. elegans. BME and AR significantly delayed the appearance of oxidative stress
markers in wild‐type N2 and transgenic strains TJ356 and CF1553, affecting the
DAF‐16/FOXO transcription factor subcellular distribution and inducing expression
of the sod‐3 antioxidative gene. Pretreatment with AR significantly reduced the
aging marker lipofuscin accumulation in BA17 worms, its effect was greater than
that of epigallocatechin gallate, suggesting a potential antiaging effect. Neuroprotective
effects of AR and BME were confirmed in AM141 transgenic worms,
inducing a significant reduction in the score of polyQ40::GFP aggregates. Moreover,
BME (25 μg/mL) resulted in a significant delay in Aβ‐induced paralysis in CL4176
worms. In silico molecular modeling revealed that BME exhibited good fitting scores
within the active sites of the Daf‐2 protein. AR and BME exert beneficial effects in
the modulation of age‐related markers and attenuation of neurotoxicity in neurodegenerative
disorders. Hence, AR and BME could be recognized as promising
antioxidant and neuroprotective natural drug candidates that could be included in
neuro‐nutraceuticals.
Stellaria media L., also called chickweed, is widespread in all parts of the world. In the present study, we investigated the biological properties and chemical profiles of different extracts (ethyl acetate, ethanol, ethanol/water, and water) of S. media. The chemical profiles were examined using UHPLC/MS/MS technique. Regarding the biological properties, antioxidant properties as well as enzyme‐inhibiting and cytotoxic effects of the extracts were demonstrated by in vitro methods. To obtain further information about the structure‐ability relationship, network pharmacology and molecular docking were also performed. Twelve phenolic compounds were identified in the extracts and most of them were flavonoids (apigenin, kaempferol derivatives, etc.). The water extract showed the best free radical scavenging activity, while the ethanol was the most active in reducing power tests. When inhibiting AChE, the ethyl acetate extract showed the best inhibitory effect. The water extract has a good cytotoxic effect on HepG2 (cell viability: 33.9% at a concentration of 100 g/mL). The analysis, performed using the STRING database, included these 45 cancer‐associated targets. The identified hub genes were TP53, CDKN2A, PTEN, KRAS, and HRAS. In molecular docking analysis, acacetin‐O‐hexoside‐O‐deoxyhexoside and napigenin‐7‐O‐hexoside exhibit remarkable binding energies with proteins. Consequently, S. media can be potential raw materials for designing functional formulations in the pharmaceutical, nutraceutical, and cosmeceutical industries.
Alzheimer’s Disease (AD) is a neurodegenerative disorder mainly characterized by dementia and cognitive decline. AD is essentially associated with the presence of aggregates of the amyloid-β peptide and the hyperphosphorylated microtubule-associated protein tau. The available AD therapies can only alleviate the symptoms; therefore, the development of natural treatments that exhibit neuroprotective effects and correct the behavioral impairment is a critical requirement. The present review aims to collect the natural substances that have been evaluated for their neuroprotective profile against AD-like behaviors induced in zebrafish (Danio rerio) by scopolamine. We focused on articles retrieved from the PubMed database via preset searching strings from 2010 to 2023. Our review assembled 21 studies that elucidated the activities of 28 various natural substances, including bioactive compounds, extracts, fractions, commercial compounds, and essential oils. The listed compounds enhanced cognition and showed several mechanisms of action, namely antioxidant potential, acetylcholinesterase’s inhibition, and reduction of lipid peroxidation. Additional studies should be achieved to demonstrate their preventive and therapeutic activities in cellular and rodent models. Further clinical trials would be extremely solicited to support more insight into the neuroprotective effects of the most promising drugs in an AD context.
Breast cancer is the most prevalent type of cancer, the fifth leading cause of cancer-related deaths, and the second leading cause of cancer deaths among women globally. Recent research has provided increasing support for the significance of phytochemicals, both dietary and non-dietary, particularly triterpenoids, in the mitigation and management of breast cancer. Recent studies showed that triterpenoids are promising agents in the treatment and inhibition of breast cancer achieved through the implementation of several molecular modes of action on breast cancer cells. This review discusses recent innovations in plant triterpenoids and their underlying mechanisms of action in combating breast cancer within the timeframe spanning from 2017 to 2023. The present work is an overview of different plant triterpenoids with significant inhibition on proliferation, migration, apoptosis resistance, tumor angiogenesis, or metastasis in various breast cancer cells. The anticancer impact of triterpenoids may be attributed to their antiproliferative activity interfering with angiogenesis and differentiation, regulation of apoptosis, DNA polymerase inhibition, change in signal transductions, and impeding metastasis. The present review focuses on several targets, mechanisms, and pathways associated with pentacyclic triterpenoids, which are responsible for their anticancer effects. We could conclude that natural triterpenoids are considered promising agents to conquer breast cancer.
Graphical Abstract
The increased prevalence of neurological illnesses is a burgeoning challenge to the public healthcare system and presents greater financial pressure. Formononetin, an O‐methylated isoflavone, has gained a lot of attention due to its neuroprotective potential explored in several investigations. Formononetin is widely found in legumes and several types of clovers including Trifolium pratense L., Astragalus membranaceus, Sophora tomentosa , etc. Formononetin modulates various endogenous mediators to confer neuroprotection. It prevents RAGE activation that results in the inhibition of neuronal damage via downregulating the level of ROS and proinflammatory cytokines. Furthermore, formononetin also increases the expression of ADAM‐10, which affects the pathology of neurodegenerative disease by lowering tau phosphorylation, maintaining synaptic plasticity, and boosting hippocampus neurogenesis. Besides these, formononetin also increases the expression of antioxidants, Nrf‐2, PI3K, ApoJ, and LRP1. Whereas, reduces the expression of p65‐NF‐κB and proinflammatory cytokines. It also inhibits the deposition of Aβ and MAO‐B activity. An inhibition of Aβ/RAGE‐induced activation of MAPK and NOX governs the protection elicited by formononetin against inflammatory and oxidative stress‐induced neuronal damage. Besides this, PI3K/Akt and ER‐α‐mediated activation of ADAM10, ApoJ/LRP1‐mediated clearance of Aβ, and MAO‐B inhibition‐mediated preservation of dopaminergic neurons integrity are the major modulations produced by formononetin. This review covers the biosynthesis of formononetin and key molecular pathways modulated by formononetin to confer neuroprotection.
Phytonutrients and Neurological Disorders: Therapeutic and Toxicological Aspects provides and assesses the latest research and developments surrounding the use of phytonutrients for the treatment of neurological disorders. The volume analyzes advances in phytonutrient isolation, characterization and therapeutic applications, giving particular emphasis to mechanisms and safety profiles. The book takes toxicological considerations into account, including adverse drug reactions, toxicokinetics and toxicodynamics. Sections cover bioactive compound classes and biosynthesis pathways, general considerations, including quality control, standardization, and technology, and toxicology. This title is a comprehensive work on the latest research in phytonutrients and neurological disorders that will be useful to researchers and medical practitioners.
Toxicodynamics defined the dynamic reciprocity of toxic phytochemical/toxicant with biological targets and its physiological responses. As a phytochemical toxicant enters in the body, it elicits a response after interaction with receptors or binding proteins based on its structural and chemical nature. Medicinal plants/phytonutrients have presumed health benefits and nutritional values, therefore they employed throughout early civilisation. Plants are a common part of human routine diet. However, always plant consumption in diet is not safe. Some phytochemicals in plants have neurotoxic potential through modulation of multiple signaling pathways. This chapter comprehensively describes the toxic nature of phytochemical, mechanism of toxic phytochemical with biological targets, and adverse outcomes.
Algal biomass is currently recognized as a potential source of unique and valuable metabolites with particular emphasis on marine subtypes. Stressful marine conditions provoke the production of secondary metabolites with unique biological activities. Brown algae (Phaeophyta) represents one of the three major classes of marine algae characterized by a high concentration of the brown pigment fucoxanthin. The presence of macro- and micronutrients in marine brown algae has led to its recognition as a potential food source for centuries, especially for coastal communities. Besides its nutritional value, brown algae represent a rich source of primary and secondary metabolites with unique biological activities; thus, they act as a potential drug source for medicinal and cosmetic applications, besides their importance as excipients for the drug industry. Brown algal extracts have been investigated for their potential use in treating many common health problems, including diabetes, inflammation, microbial and viral infections, coagulation problems, and different kinds of cancer; their role in the cosmetic industry is due to the high content of antioxidant metabolites. Chemical investigations of different species of brown algae revealed a wide array of secondary metabolites with terpenoids, especially diterpenes, polymeric phenolics, phenolic acids, and flavonoids, differentiating brown algae from other classes of macroalgae.
Gastrointestinal cancer is one of the most prevalent causes of cancer-related deaths in the world. Recent research demonstrates that phytochemicals are critical in preventing and managing gastrointestinal cancer. The increased intake of phytochemicals could reduce the risk of cancer by inhibiting cancer cell proliferation, inducing apoptosis and autophagy, and suppressing angiogenesis as well as cancer cell metastasis. These mechanisms are also known to counter Helicobacter pylori infection and modulate gut microbiota. There is preliminary data suggesting that daily supplementation with high doses of certain vitamins combined with conventional therapeutic agents may enhance their growth inhibitory effects on tumor cells and protect normal tissues against some of their toxic effects. This book attempts to fill gaps on the role of phytonutrients in the treatment of cancer in the gastrointestinal tract (GIT). It discusses the action of individual vitamins on cellular and molecular parameters and describes how vitamins inhibit protein kinase C activity, increase the production of certain growth factors, and modulate the expression of a number of oncogenes. The book is divided into 2 parts. The first part summarizes the pathophysiology of GIT cancers and introduces readers to anticancer phytonutrients. A chapter on the status of FDA approved nutraceuticals rounds up this section. The second part of the book provides a systematic review on the different plant derived chemicals that can be used to treat GIT cancer. Each chapter in this section focuses on a specific type of phytochemical agent and its molecular mechanisms relevant to the disease. This book will give the reader a holistic view of gastrointestinal cancer treatment and the value of natural compounds in developing functional food and drugs for preventive medicine.
Alzheimer's disease (AD) is the most frequent type of dementia characterized by the deposition of amyloid beta (Aβ) plaque and tau-neurofibrillary tangles (TNTs) in the brain. AD is associated with the disturbances of various neurotransmitters including gamma-aminobutyric acid (GABA). Of note, GABA is reduced in AD, and restoration of GABA effect by benzodiazepines (BDZs) may improve AD outcomes. However, BDZs may adversely affect cognitive functions chiefly in elderly AD patients with sleep disorders. Besides, there is a controversy regarding the use of BDZs in AD. Consequently, the objective of the present review was to disclose the possible role of BDZs on the pathogenesis of AD that might be beneficial, neutral, or detrimental effects on AD. Prolonged use of intermediate-acting BDZ lorazepam exerts amnesic effects due to attenuation of synaptic plasticity and impairment of recognition memory. However, BDZs may have a protective effect against the development of AD by reducing tau phosphorylation, neuroinflammation, and progression of AD neuropathology. On the other side, other findings highlighted that extended use of BDZs was not associated with the development of AD. In conclusion, there are controversial points concerning the use of BDZs and the risk for the progression of AD. Thus, preclinical, and clinical studies are essential in this regard.
Background:
Depression is a common complication after myocardial infarction (MI) that can seriously affect the prognosis of MI.
Purpose:
To investigate whether formononetin could ameliorate MI injury and depressive behaviours in a mouse model of MI with depression and elucidate its underlying molecular mechanisms.
Methods:
Haemodynamic measurements (systolic blood pressure (SYS), the maximum rate of rise of LV pressure (± dp/dtmax)) and behavior tests (tail suspension test, sucrose preference test, forced swimming test) were used to evaluate the effects of formononetin on male C57BL/6N mice after left anterior descending (LAD) coronary artery ligation and chronic unpredictable stress. RT-qPCR, immunohistochemistry, immunofluorescence analysis, western blotting, molecular docking technology, surface plasmon resonance and gene-directed mutagenesis were used to clarify the underlying mechanism.
Results:
Formononetin significantly suppressed the depressive behaviours and improved cardiac dysfunction in MI with depression mice model. Formononetin inhibited M1 polarization in macrophages/microglia, while promoting M2 polarization. Importantly, elevated serum IL-6 and IL-17A levels were found in patient with MI, and the patient serum induced M1 microglial polarization; however, formononetin reversed the polarization. Further mechanistic studies showed that formononetin inhibited GSK-3β activity and downstream Notch1 and C/EBPα signaling pathways. Covalent molecular docking showed that formononetin bound to Cys199 of GSK-3β and it has a high affinity for GSK-3β. When Cys199 was mutation, the inhibitory effect of formononetin on GSK-3β activity and M1 polarization in macrophages/microglia were also partly blocked.
Conclusions:
Our results firstly uncovered that formononetin improved cardiac function and suppressed depressive behaviours in mice after MI with depression by targeting GSK-3β to regulate macrophage/microglial polarization. More importantly, IL-6 and IL-17A produced after MI may cause neuroinflammation, which might be the key factors for depression. Formononetin may be a potential drug for treating MI with depression.
Previous studies reported the neuroprotective effects of formononetin (FMN), however, whether it has antidepressant-like effects have not been reported. To evaluate the antidepressant-like effects of FMN, a mice model of depression was established by chronic corticosterone (CORT) injection. The serum corticosterone levels and hippocampal protein expression were detected by ELISA and Western blot. Nissl staining was used to observe the damage of hippocampal neurons and immunofluorescence was used to observe the neurogenesis in the hippocampus. Our results showed that FMN significantly increased the sucrose preference and shorten the immobility time in the forced swimming test in CORT-treated mice. Moreover, FMN reduced the serum corticosterone levels, upregulated the protein expression levels of the glucocorticoid receptor (GR), and brain-derived neurotrophic factor (BDNF) in the hippocampus, protected against the CORT-induced neuronal impairment, and promoted the neurogenesis in the hippocampus. Taken together, the present study was the first to demonstrate the antidepressant-like effects of FMN in the CORT-induced mice model of depression, which may contribute to the discovery of a new candidate for treating depression.
Sophora is deemed as one of the most remarkable genera of Fabaceae, and the third largest family of flowering plants. The genus Sophora comprises approximately 52 species, 19 varieties, and 7 forms that are widely distributed in Asia and mildly in Africa. Sophora species are recognized to be substantial sources of broad spectrum biopertinent secondary metabolites namely flavonoids, isoflavonoids, chalcones, chromones, pterocarpans, coumarins, benzofuran derivatives, sterols, saponins (mainly triterpene glycosides), oligostilbenes, and mainly alkaloids. Meanwhile, extracts and isolated compounds from Sophora have been identified to possess several health-promising effects including anti-inflammatory, anti-arthritic, antiplatelets, antipyretic, anticancer, antiviral, antimicrobial, antioxidant, anti-osteoporosis, anti-ulcerative colitis, antidiabetic, anti-obesity, antidiarrheal, and insecticidal activities. Herein, the present review aims to provide comprehensive details about the phytochemicals and biological effects of Sophora species. The review spotlighted on the promising phytonutrients extracted from Sophora and their plethora of bioactivities. The review also clarifies the remaining gaps and thus qualifies and supplies a platform for further investigations of these compounds.
Phytochemical investigation of Sophora secundiflora alkaloid fraction led to isolation of one new quinolizidine alkaloid (1) 13-methoxyanagyrine together with six known ones (2–7). The insecticidal activity of 70% methanol extract of leaves of S. secundiflora, S. tomentosa and the isolated alkaloids were assessed against 3rd instar larvae of Culex pipiens (Diptera: Culicidae) using different concentrations and mortality rate was recorded. Sophora tomentosa extract showed highest mortality rate with median lethal concentration LC50 3.11 ppm after 24 h and 0.66 ppm after 48 h and anagyrine (6) exhibited remarkably insecticidal activity with LC50 value of 3.42 ppm after 24 h of exposure. Additionally, cytotoxic activity of alkaloid fraction of S. secundiflora, S. tomentosa and isolated alkaloids was also studied using crystal violet assay against MCF-7 and HEPG-2 cell lines. Anagyrine (6) exhibited IC50 values of 27.3 ± 0.7 and 30.2 ± 0.9 µg/mL against MCF-7 and HEPG-2 cancer cells, respectively.
Genus Sophora L. belonging to family Fabaceae comprises about 80 species. It is a heterogeneous genus, ranging from tall trees to small, herbaceous plants. Morphological and genetic characteristics of two Sophora species, viz. S. secundiflora (Ortega) DC. and S. tomentosa L. were subjected to detailed study to delimit these species, where such data are lacking. During this study comparative morphology and anatomy of stem, leaves and petioles of both species was carried out. Moreover, DNA fingerprinting of both plants was carried out using 11 decamer random primers. The obtained results revealed that, many differences in morphological characters viz. the color of the flower, shape of the petiole and leaf dimensions. While the anatomical study reflecting other differential characters among them: the non-glandular hairs and the dimensions of some microelements. The features of the powdered stems and leaves are also described. Moreover, the DNA fingerprinting; created a total of 232 bands, out of the 99 were polymorphic representing a level of polymorphism of 42.67%. The primer (OPO-02) showed the highest degree of similarities (85.71%), while the lowest (35.29%) was recorded by the primer (OPO-10). This study concludes that the retrieved morphological, anatomical and genetic features provide a powerful identification and characterization tool for both of the studied Sophora species; even when used as powdered material. This study is a pioneer regarding the detailed botanical structure of both species; in addition to, the DNA fingerprinting to distinguish these species; in different prescriptions.
Schinus terebinthifolius is a plant well recognized for its therapeutic profile such as anti-inflammatory and antitumor activities, promoting antibacterial activity and antioxidant and antidiabetic properties. .is study aimed at examining whether Schinus terebinthifolius memory-enhancing activities are mediated by cholinergic and brain antioxidant systems in a scopolamine zebrafish model. Schinus terebinthifolius essential oil (10, 25, and 50 μL/L) was delivered to zebrafish by immersion in water for 8 days. Memory deficits were induced by scopolamine (100 μM) administration. Zebrafish were divided into seven groups (n � 15/ group): vehicle group, scopolamine (100 μM) group, Schinus terebinthifolius essential oil groups (STF; 10, 25, and 50 μL/L), the imipramine group (IMP; 20 mg/L, as the positive control in the NTT test), and the donepezil group (DP; 10 mg/L, as the positive control in the Y-maze test). Memory status was estimated by the novel tank diving test (NTT) and the Y-maze test and finally was validated by comparison with imipramine (20 mg/L) and donepezil (10 mg/L). Gas chromatography-mass spectrometry (GC-MS) was used to detect oil compounds. Brain levels of acetylcholinesterase (AChE) and antioxidant enzymes were measured. After being exposed to Schinus terebinthifolius essential oil, the scopolamine zebrafish exhibited an improvement of memory processes in the NTT and Y-maze tests. .e essential oil attenuated the elevated level of AChE and brain oxidative stress. Schinus ter-ebinthifolius essential oil was found to support memory formation through the inhibition of the AChE activity and decreasing oxidative stress in the scopolamine-treated zebrafish brains.
Sophora species are used as dietary medicines in aging-associated symptoms. Sophora tomentosa L. (ST) is a native medicinal plant in Southeast Asia; however, there is no pharmacological literature about ST extract. The present study evaluates the antioxidant phytoconstituent contents and radical scavenging capacities of ST extract. The further investigation was to clarify the neuroprotective mechanism of ST extract against 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced Parkinsonism by assaying the activities of the dopaminergic system and antioxidant defenses, glycogen synthase kinase 3β (GSK3-β) phosphorylation, and α-synuclein levels in C57BL/6 mice. The results show that ST extract alleviated the motor deficits in MPTP-induced Parkinsonism with four behavioral tests, including a rearing locomotor, catalepsy test, balance beam walking test, and pole test. ST extract reversed the number of tyrosine hydroxylase (TH)-positive neurons in substantia nigra (SN) that had decreased by MPTP. ST extract also restored the decreased levels of dopamine and the expression of tyrosine hydroxylase (TH) in the striatum. Furthermore, ST extract restored the levels of glutathione (GSH) and the activities of antioxidant enzymes, and decreased the elevated levels of malondialdehyde (MDA) in mouse striatum. ST extract also decreased α-synuclein overexpression and GSK-3β phosphorylation in mouse striatum. In vitro, ST extract exerted higher 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical scavenging capacities through its higher phenolic contents, especially protocatechuic acid and epicatechin. These results suggest that ST extract has the potential to counteract MPTP-induced motor deficit. The neuroprotective mechanism of ST extract against MPTP-induced Parkinsonism might be related to decreasing GSK-3β phosphorylation and restoring the activities of striatal antioxidant defenses to restore the nigrostriatal dopaminergic function and decrease α-synuclein accumulation.
Two new furanoflavonoids, retamasins A and B (1 and 2, resp.), along with five known flavonoids, 3–7, were isolated from the aerial parts of Retama raetam. Their structures were determined on the basis of extensive spectroscopic (IR, MS, and 1D‐ and 2D‐NMR) analyses and by comparison with the literature data. This is the first report of the isolation of new furanoflavonoids 1 and 2 from Retama genus, while compounds 3, 5, and 6 were found for the first time from R. raetam. Antioxidant and anti‐inflammatory activities of the isolated compounds were also evaluated. Compounds 2, 3, and 5–7 exhibited potent inhibitions of iNOS activity with IC 50 values of 2.9, 5.0, 3.1, 1.2, and 4.8 μg/ml, respectively. All compounds inhibited NF‐κB except 1 and 5. Compound 6 was most active in inhibiting iNOS and NF‐κB activity, as well as in decreasing oxidative stress.
During the past several years, there has been enormous progress in the understanding of the causative factors that initiate neuronal damage in various neurodegenerative diseases, including Alzheimer disease, Parkinson disease, multiple sclerosis, amyotrophic lateral sclerosis, and Huntington disease. Preventing neuronal damage and neuronal death will have a huge clinical benefit. However, despite major advances in causative factors that trigger these neurodegenerative diseases, to date there have been no therapies available that benefit patients who suffer from these diseases. Because most neurodegenerative diseases are late-onset and remain asymptomatic for most of the phases, the therapies initiated in advanced stages of the disease have limited value to patients. It may be possible to prevent or halt the disease progression to a great extent if therapies start at the initial stage of the disease. Such therapies may restore neuronal function by reducing or even eliminating the primary stressor. Flavonoids are key compounds for the development of a new generation of therapeutic agents that are clinically effective in treating neurodegenerative diseases. Regular consumption of flavonoids has been associated with a reduced risk of neurodegenerative diseases. In addition to their antioxidant properties, these polyphenolic compounds exhibit neuroprotective properties by their interaction with cellular signaling pathways followed by transcription and translation that mediate cell function under both normal and pathologic conditions. This review focuses on human intervention studies as well as animal studies on the role of various flavonoids in the prevention of neurodegenerative diseases.
© 2015 American Society for Nutrition.
Sophora is a genus of the Fabaceae family, contains about 52 species, nineteen varieties, and seven forms that are widely distributed in Asia, Oceanica, and the Pacific islands, in the family Fabaceae of herbaceous (Sophora flavescens Aiton) to trees (Sophora japonica L.). More than fifteen species in this genus have a long history of use in traditional Chinese medicines. In the last decades the use of this genus in traditional Chinese drugs has led to rapid increase in the information available on active components and reported to posses various pharmacological/ therapeutic properties. The paper reviews the ethnopharmacology, the biological activities and the correlated chemical compounds of genus Sophora, Fabaceae. More than 300 compounds has been isolated, among them major are quinolizidine alkaloids particularly matrine and oxymatrine and flavonoids particularly prenylated and isoprenylated flavonoids. Modern pharmacological studies and clinical studies demonstrated that these chemical constituens possess wide reaching pharmacological actions like anti oxidant, anticancer, anti-asthamatic, anti-neoplastic, antimicrobial, antiviral, antidote, anti pyretic, cardiotonic, antinflammatory, diuretic and in the treatment of skin diseases like eczema, colitis and psoriasis.
Flavonoids uncharacteristic of intact plants were isolated from callus tissue of Iris ensata and were identified as 5-hydroxy-4′-methoxyflavone, 5-hydroxy-3′-methoxyflavone, and 5-hydroxy-2′-methoxyflavone using PMR
and mass spectrometry. It was proposed that the lack of growth of callus tissue after changing cultivation conditions was
related to the inhibiting effect of these flavones on cell proliferation.
The present study investigated the hypoglycemic, hypolipidemic and cardioprotective effects of 100 - 400mg/kg/day/oral route of the aqueous seed extract of Carica papaya Linn (CPE) in normal male Wistar rats for 30days. The rats, weighing between 120 and 150 g which were divided into groups I - V of six rats each and were orallyadministered with 10 ml/kg/day of distilled water, 0.1 mg/kg/day of glibenclamide, 100, 200, and 400 mg/kg/day ofextract respectively, for 30 days. In addition, the acute oral toxicity and phytochemical analyses of the extract wereconducted. On day 31, after an overnight fast, blood samples were obtained by cardiac puncture under inhaleddiethyl ether anesthesia for the determination of the fasting blood glucose (FBS), serum triglyceride (TG), totalcholesterol (TC), low density lipoprotein cholesterol (LDL-c), very low density lipoprotein cholesterol (VLDL-c), andhigh density cholesterol (HDL-c). The atherogenic (AI) and coronary artery (CAI) indices were also calculated.Results showed that CPE significantly and progressively (p<0.05, p<0.01 and p<0.001) lowered the FBS, TG, TC,LDL-c, and VLDL-c dose-dependently, while significantly (p<0.05, p<0.01, p<0.001) causing dose-related elevation inHDL-c concentration when compared to the untreated control and glibenclamide treated rats. The extract alsosignificantly (p<0.05, p<0.01 and p<0.001) lowered the AI and CAI indices dose-dependently. The acute oral toxicityshowed the extract to be safe. Phytochemical analyses revealed the presence of alkaloids, flavonoids, saponins,tannins, anthraquinones, anthocyanosides and reducing sugars. Thus, lending support to its folkloric use in themanagement of suspected type 2 diabetic patients.
The activity of the noradrenergic marker enzyme dopamine-beta-hydroxylase was measured in brains removed postmortem from control patients and patients with Alzheimer's disease. Enzyme activity was decreased in the frontal and temporal cortices and hippocampus in patients with Alzheimer's disease, but was within the normal range in patients with depression, multiinfarct dementia, and terminal coma.The decrease in enzyme activity in Alzheimer's disease may reflect an abnormality of cortical noradrenergic fibres in some patients with the disease.
Background
The genus Sophora (Fabaceae) represents one of the important medicinal plant genera regarding its chemical constituents and outstanding pharmacological activities.
Purpose
In this review, we surveyed the latest findings on the bioactivities of different Sophora extracts and isolated phytochemicals during the past 8 years (2011-2019) updating the latest review article in 2011. The aim of this review is to focus on the molecular pharmacology of Sophora species to provide the rationale basis for the development of novel drugs.
Results
Sophora and its bioactive compounds possess outstanding pharmacological properties, especially as anticancer and anti-inflammatory drugs, in addition to its antioxidant, antibacterial, antifungal and antiviral properties.
Conclusion
Based on their use in traditional medicine, Sophora species exert a plethora of cellular and molecular activities, which render them as attractive candidates for rationale drug development. Randomized, placebo-controlled clinical trials are required for further integration of Sophora-based phototherapies into conventional medicine.
Background
Agathisflavone, a biflavonoid isolated from Schinus polygamus (Cav.) Cabrera leaves been reported to promote various biological activities such as anti-inflammatory properties, promoting cognition and preventing cancer, antioxidant and antiapoptotic activities.
Purpose
Here, we tested the hypothesis whether anxiety, amnesia, and brain oxidative stress induced by scopolamine could be counteracted in zebrafish model by agathisflavone and tried to ascertain the underlying mechanism.
Methods
Agathisflavone (1, 3 and 5 µg/l) was administered by immersion to zebrafish once daily for 8 days period. Anxiety and memory impairment were induced with scopolamine (100 µM) and measured with the novel tank diving test (NTT) and the Y-maze test. Zebrafish were divided into seven groups (n = 20/group): first group - control, second group - scopolamine (100 μM), the third, fourth and fifth group - agathisflavone treatment groups (FAB, 1 µg/l, 3 µg/l, and 5 µg/l), the sixth group - imipramine (IMP, 20 mg/l, as the positive control in NTT test), and the seventh group - donepezil group (DP, 10 mg/l, as the positive control in Y-maze test). The identification of the agathisflavone was done by spectroscopy, and the structure of the compound was confirmed by (-) Electrospray Ionisation Mass Spectrometry (ESI-MS). The brain oxidative status and acetylcholinesterase (AChE) activity were also investigated.
Results
Agathisflavone from Schinus polygamus (Cav.) Cabrera leaves was identified. Also, we demonstrated that agathisflavone significantly reversed scopolamine-induced behavioral score alteration in the NTT and Y-maze tests. Consequently, agathisflavone promoted inhibition of AChE activity and restored the brain antioxidant status.
Conclusion
Our results demonstrate that agathisflavone promotes brain antioxidant action and ameliorates scopolamine-induced anxiety and memory deficits in zebrafish.
Licochalcone B (LCB), an extract from the root of Glycyrrhiza inflate, has the same caffeic acid scaffold as curcumin (Cur), which is known as an anti-Alzheimer's disease (AD) agent. However, there is no relevant research about anti-AD activity of LCB. In this study, the anti-AD activity of LCB was investigated. LCB could inhibit amyloid beta (Aβ42) self-aggregation (IC50 = 2.16 ± 0.24 μM) and disaggregate pre-formed Aβ42 fibrils, reduce metal-induced Aβ42 aggregation through chelating metal ions. Molecular docking further revealed that LCB inhibited Aβ42 self-aggregation through forming two hydrogen bonds with Lys28 to block the salt bridge interaction at the C-terminus of Aβ42. Anti-oxidant property of LCB was also observed by DCFH-DA assay. In addition, LCB did show neuroprotective activity against H2O2-induced cell death in SH-SY5Y cells. In general, our results demonstrate that LCB, as a multifunctional agent, is likely to be promising therapeutics for AD.
A new matrine-type alkaloid, 7α-hydroxysophoramine (1), was isolated from the aerial parts of Sophora alopecuroides together with eight known alkaloids, 12β-hydroxysophocarpine (2), sophoramine (3), 14β-hydroxymatrine, matrine, sophoridine, sophocarpine, adenocarpine, and baptifoline. The structures of compounds 1-3 were confirmed through single-crystal X-ray diffraction analysis.
The polysaccharide (PSH) extracts from the edible mushroom species Coprinus comatus and Coprinellus truncorum were screened in liquid for their acetylcholinesterase inhibitory (AChE) activity. Both extracts were found to display inhibition of the aforementioned enzyme reaching similar IC50 values of 0.62 ± 0.07 and 0.61 ± 0.03 mg/mL, respectively. According to the means of FTIR spectroscopy, these PSH extracts mostly contained β-glucans. However, the presence of some proteins and polyphenolics as minor ingredients were also detected. Compared with existing literature data for anti-AChE activity of the sugar samples, the findings within this study may be treated as a profound bioactivity. Consequently, this study puts some light on the possible use of the screened macrofungi in the palliative treatment of Alzheimer’s disease.
Sophora pachycarpa Schrenk ex C.A.Mey. is an annual plant belonging to the family Fabaceae. The cytotoxic activities of methanol-dichloromethane extracts (1:1) of different parts of S. pachycarpa were investigated on DU145 (prostate cancer cell line) and MCF-7 (breast cancer cell line) cell lines. The root extract of S. pachycarpa was the only extract that showed significant cytotoxic activity with IC50 values of 39.88 and 16.49 μg/mL on DU145 and MCF-7 cell lines, respectively. The root extract was then subjected to RP-HPLC for further fractionations. Among the isolated fractions from root extract, only one of them had remarkable cytotoxic effects with IC50 value of 26.43 on MCF-7 and 7.54 μg/mL on DU145 cell lines. Further purification led to isolation of a compound with IC50 values of 5.44 and 2.44 μg/mL on MCF-7 and DU145 cell lines, respectively. Based on ¹H NMR and ¹³C NMR spectra, together with LC-MS, the structure of the purified compound was assigned as the flavonostilbene alopecurone A.
Seven isoflavones were isolated from sprouted chickpea seeds by chromatography on silica gel column, polyamide column, sephadex LH-20 column and preparing thin-layer chromatography (TLC), respectively. The structures were characterised with one- and two-dimensional NMR in combination with mass and IR spectrometry. The obtained isoflavones were biochanin A (5,7-dihydroxyflavone-4′-methoxyflavone, (1); calycosin (7,3′-dihydroxy-4′-methoxyisoflavone, (2); formononetin (7-hydroxy-4′-methoxyisoflavone, (3); genistein (5,7,4′-trihydroxyisoflavone, (4); trifolirhizin (maackiain-3-O-β-d-glucopyranoside, (5); ononin (7-O-β-d-glucosyl-7-hydroxy-4′-methoxyisoflavone, (6); sissotrin (7-O-β-d-glucosyl-5,7-dihydroxy-4′-methoxyisoflavone, (7).
Two novel flavonoid compounds, an isoflavanone, tetrapterol A, and a pterocarpan, tetrapterol B, and three new isoflavanones, tetrapterols C-E, were isolated from the roots of Sophora tetraptera, in addition to eight known phenolic compounds (kenusanone A, lespedeol B, euchenone a9, lonchocarpol A, cajanone, (−)-maackiain, isoneorautenol and pentacosanyl caffeate). The two novel compounds had a common characteristic partial structure which is derived from a geranyl group which forms a new aromatic ring after cyclization with a hydroxyl group located at a side ring in a flavonoid framework and dehydrogenation. The new isoflavanones had a geranyl or an isoprenyl group on their A or B ring. The structures were determined by analysis of spectral data, in particular, 2D-NMR.
13C CP MAS NMR spectra of the flavonoids: morin, kaempferol, 3,7-dihydroxyflavone, tricin and isoflavones: genistein and formononetin were recorded to characterize solid-state conformations. Intramolecular hydrogen bonds forming five-, six- and seven-membered rings are present in the two morin molecules in the crystals – their 13C resonances have been assigned with the aid of the calculated shielding constants. Linear relationships between the calculated shielding constants σDFT (ppm) and chemical shifts (δCPMAS, ppm) were obtained for all studied compounds. Higher correlation coefficients suggest that the conformation with “clockwise” orientation of both OH groups is more probable in the solid 3,7-dihydroxyflavone, whereas in the solid formononetin the OH and OCH3 substituents are directed “anticlockwise”. The barrier to the rotation of phenyl ring B decreases in the order: morin (2′-OH, 3-OH)>kaempferol (3-OH)>tricin.
THE existence of the same species in countries widely separated by oceans, an apparent exception to the hypothesis of single centres of creation, was explained by nineteenth century naturalists in two ways: by transoceanic dispersal or by continental extension. Darwin supported the first explanation, and argued against major continental extensions so recent as to be “within the period of existing species”1. Explanations by continental drift can be criticized on the same grounds2. But in most widely dispersed species we still lack detailed knowledge of the seed and its means of dispersal. Thus the possibility of long-distance dispersal by ocean currents of seed of certain species of Sophora (Papilionaceae) has long been discussed. Studies of S. tomentosa, a pan-tropic littoral species with buoyant seeds, show that this species must certainly be distributed in this way3–5; and since Darwin's time there has been speculation as to whether the close relation between the sophoras of New Zealand, southern Chile and Gough Island can be explained in the same way. We made the following observations on the problem on the Kermadec Islands (W. R. S.) and in New Zealand and southern Chile (E. J. G.).
This work was accomplished at the sandbank of Joaquina Beach on Santa Catarina Island, Florianópolis, SC. The rate of formation of Sophora tomentosa fruits from buttons was 25.4%. Out of the fruits actually formed, 28.9% failed to reach maturity and were eliminated by the plant. The fruits formed during the spring took 7.9 weeks to mature, and those formed during the autumn took about 11.1 weeks. The average length of the fruits collected in 2001 was 7.8cm, and in 2002 it was 9.2cm. In 2001 and 2002, the fruits presented a rate of predation by insects of 30% and 59%, respectively. The average quantity of seeds for fruit was 4.8 in 2001, and 6.2 in 2002. In 2001, 60.2% of the seeds presented some kind of damage, and in 2002, 42.5% of them did. The most common types of damage among the seeds were due to fungus (92.3%) and predator (53%) attack. Among the fruits of S. tomentosa, two beetles, Cryptophilus sp. (Cryptophagidae) and Acylomus sp. (Phalacridae), were found. A Cadra sp. (Pyralidae) moth emerged while the seeds were stored. A Myrmelachista sp. (Formicidae) ant and three species of Heterospilus (Braconidae) were also found.
The integrity of dopaminergic, noradrenergic and serotonergic neurons in normal aging and Alzheimer's disease is reviewed. Loss of dopaminergic innervation of the neostriatum is a prominent age-related change, which corresponds with the age-related loss of dopaminergic cell bodies from the substantia nigra. This change is regionally specific, since dopaminergic innervation of the neocortex and the neostriatum are not affected. Although there is an age-related loss of noradrenergic cell bodies from the locus coeruleus, most studies indicate normal concentrations of noradrenaline in target areas. There is also evidence for reduced serotonergic innervation of the neocortex and, less convincingly, the neostriatum. Alzheimer's disease is associated with more pronounced noradrenergic and serotonergic denervation but, unlike normal aging, dopaminergic innervation of neostriatum is intact; although dopamine neurons are probably dysfunctional in this region. Studies relating neuronal markers to the symptomatology of Alzheimer's disease indicate that dysfunction of monoamine neurons is more closely linked to non-cognitive than to cognitive changes in behavior. In addition, monoaminergic therapies have been successful in ameliorating affective and psychotic behaviors along with sleep disturbances in both Alzheimer's disease and senescence. It seems likely that monoaminergic therapies (developed as we learn more about alterations in dopamine, noradrenaline and serotonin) will continue to be necessary to treat such behavioral disturbances.
A new matrine-type alkaloid, 7alpha-hydroxysophoramine (1), was isolated from the aerial parts of Sophora alopecuroides together with eight known alkaloids, 12beta-hydroxysophocarpine (2), sophoramine (3), 14beta-hydroxymatrine, matrine, sophoridine, sophocarpine, adenocarpine, and baptifoline. The structures of compounds 1-3 were confirmed through single-crystal X-ray diffraction analysis.
Alzheimer's disease (AD) is considered to be the most common dementing disorder. The understanding of this disorder has greatly advanced over the past few years, and new therapeutic options have been developed. Another disorder, vascular dementia (VaD), is a syndrome with multiple etiologies operating through a variety of different mechanisms. The combination of AD and VaD is extremely common, making mixed dementia the most common type of dementia. Risk factors for VaD, which are the common vascular risk factors, are presently known to apply also to AD. Cholinergic deficits occur in both conditions. The identification of several genetic factors that can contribute to vascular damage, as well as possible auto-immune damage to vascular components, are important. It is remarkable that amyloid precursor protein (APP) mutations can cause the typical pathological changes of AD as well as amyloid deposition around blood vessels. These may lead to deficient blood perfusion to the brain, changes of the blood-brain barrier, as well as cerebral hemorrhages. Interestingly, attention to risk factors, such as hypertension, coronary artery disease, hyperlipidemia and smoking could reduce or delay the incidence of dementia, both vascular and AD.
- Cross AJ
The biology of the subtropical and pantropic shrub, Sophora tomentosa L. (Fabaceae): in coastal dune environments
- R I Lonard
- Judd F Stalter
Lonard RI, Judd F, Stalter R. 2015. The biology of the subtropical and pantropic shrub, Sophora
tomentosa L. (Fabaceae): in coastal dune environments. Int Biol Rev. 2:1-16.
The polysaccharide extracts from the fungi Coprinus comatus and Coprinellus truncorum do exhibit AChE inhibitory activity
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AChE inhibitory activity. Nat Prod Res. 33(5):750-754.
Sophora secundiflora (Texas mountain laurel). Florida Cooperative Extension Service, Fact Sheet ST-597
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Gilman EF, Watson DG. 1994. Sophora secundiflora (Texas mountain laurel). Florida Cooperative
Extension Service, Fact Sheet ST-597, University of Florida.
New names in Dermatophyllum (Fabaceae)
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Turner BL. 2012. New names in Dermatophyllum (Fabaceae). Phytoneuron. 3:1-4.
Texas mountain laurel). Florida Cooperative Extension Service, Fact Sheet ST-597
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Reduced dopamine-beta-hydroxylase activity in Alzheimer's disease
- A J Cross
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