A theoretical screening of phytochemical constituents from Millettia brandisiana as inhibitors against acetylcholinesterase.

Alzheimer's disease is one of the causes associated with the early stages of dementia. Nowadays, the main treatment available is to inhibit the actions of the acetylcholinesterase (AChE) enzyme, which has been identified as responsible for the disease. In this study, computational methods were used to examine the structure and therapeutic ability of chemical compounds extracted from Millettia brandisiana natural products against AChE. This plant is commonly known as a traditional medicine in Vietnam and Thailand for the treatment of several diseases. Furthermore, machine learning helped us narrow down the choice of 85 substances for further studies by molecular docking and molecular dynamics simulations to gain deeper insights into the interactions between inhibitors and disease proteins. Of the five top-choice substances, γ-dimethylallyloxy-5,7,2,5-tetramethoxyisoflavone emerges as a promising substance due to its large free binding energy to AChE and the high thermodynamic stability of the resulting complex.

Antiviral Rotenoids and Isoflavones Isolated from Millettia oblata ssp. teitensis.

Three new (1-3) and six known rotenoids (5-10), along with three known isoflavones (11-13), were isolated from the leaves of Millettia oblata ssp. teitensis. A new glycosylated isoflavone (4), four known isoflavones (14-18), and one known chalcone (19) were isolated from the root wood extract of the same plant. The structures were elucidated by NMR and mass spectrometric analyses. The absolute configuration of the chiral compounds was established by a comparison of experimental ECD and VCD data with those calculated for the possible stereoisomers. This is the first report on the use of VCD to assign the absolute configuration of rotenoids. The crude leaves and root wood extracts displayed anti-RSV (human respiratory syncytial virus) activity with IC50 values of 0.7 and 3.4 µg/mL, respectively. Compounds 6, 8, 10, 11, and 14 showed anti-RSV activity with IC50 values of 0.4-10 µM, while compound 3 exhibited anti-HRV-2 (human rhinovirus 2) activity with an IC50 of 4.2 µM. Most of the compounds showed low cytotoxicity for laryngeal carcinoma (HEp-2) cells; however compounds 3, 11, and 14 exhibited low cytotoxicity also in primary lung fibroblasts. This is the first report on rotenoids showing antiviral activity against RSV and HRV viruses.

Antidiabetic Evaluation of Kigelia pinnata Root Bark Extract in Streptozotocin-Induced Type-2 Diabetes Model of Rats.

Diabetes mellitus (DM) is the most common endocrine disorder characterized by increased blood glucose levels resulting from defective insulin secretion, resistance to insulin action, or both. DM is often associated with severe complications, and there is an increasing appreciation that cognitive function declines in DM. The aim of this research work was to evaluate Kigelia pinnata root bark extract in Streptozotocin (STZ)-induced type-2 diabetes. Experimental diabetes was induced by a single administration of STZ (60 mg/kg, intraperitoneal [i.p.]), immediately after the STZ administration, and all animals were fed with normal food and water. Nicotinamide was administered (120 mg/kg, i.p.) 15 min before STZ. The development of hyperglycemia was confirmed by the elevated blood glucose levels determined at fixed intervals, which was confirmed by measuring fasting blood glucose levels in rats' blood taken from the tail vein. Supplementation with ethanolic extract of K. pinnata root bark (EEKP) significantly reduced the elevated blood glucose in STZ-induced hyperglycemia in rats. EEKP significantly restored the biochemical and antioxidant defense system. On the final day of the protocol, the extract also reduced inflammatory cytokines in the blood serum.

Phytochemical, bactericidal, antioxidant and anti-inflammatory properties of various extracts from Pongamia pinnata and functional groups characterization by FTIR and HPLC analyses.

The present research looked into possible biomedical applications of Pongamia pinnata leaf extract. The first screening of the phytochemical profile showed that the acetone extract had more phytochemicals than the other solvent extracts. These included more saponins, proteins, phenolic compounds, tannins, glycosides, flavonoids, steroids, and sugar. The P. pinnata acetone extract exhibited highest antibacterial activity against C. diphtheriae. The bactericidal activity was found in the following order: C. diphtheria (14 mm) > P. aeruginosa (10 mm) > S. flexneri (9 mm) > S. marcescens (7 mm) > S. typhi (7 mm) > S. epidermidis (7 mm) > S. boydii (6 mm) > S. aureus (3 mm) at 10 mg mL-1 concentration. MIC value of 240 mg mL-1 and MBC is 300 mg mL-1 of concentration with 7 colonies against C. diphtheriae was noticed in acetone extract. Acetone extract of P. pinnata was showed highest percentage of inhibition (87.5 %) at 625 mg mL-1 concentrations by DPPH method. Furthermore, the anti-inflammatory activity showed the fine albumin denaturation as 76% as well as anti-lipoxygenase was found as 61% at 900 mg mL-1 concentrations correspondingly. FT-IR analysis was used to determine the functional groups of compounds with bioactive properties. The qualitative examination of selected plants through HPLC yielded significant peak values determined by intervals through the peak value. In an acetone extract of P. pinnata, 9 functional groups were identified. These findings concluded that the acetone extract has high pharmaceutical value, but more in-vivo research is needed to assess its potential.

Natural Phosphodiesterase-4 Inhibitors with Potential Anti-Inflammatory Activities from Millettia dielsiana.

The results of in silico screening of the 50 isolated compounds from Millettia dielsiana against the target proteins PDE4 (PDE4A, PDE4B, and PDE4D) showed binding affinity ranges from -5.81 to -11.56, -5.27 to -13.01, and -5.80 to -12.12 kcal mol-1, respectively, with median values of -8.83, -8.84, and -8.645 kcal mol-1, respectively. Among these compounds, Millesianin F was identified as the most promising PDE4A inhibitor due to its strongest binding affinity with the target protein PDE4A. (-11.56 kcal mol-1). This was followed by the compound 5,7,4'-trihydroxyisoflavone 7-O-ß-d-apiofuranosyl-(1→6)-ß-d-glucopyranoside (D50) with the binding affinity value of -11.35 kcal mol-1. For the target protein PDE4B, compound D50 exhibited the strongest binding affinity value of -13.01 kcal mol-1, while showing poorer inhibition ability for PDE4D. The 100 ns MD simulation examination (radius of gyration, Solvent Accessible Surface Area (SASA), Root-Mean-Square Deviation (RMSD), Root-Mean-Square Fluctuation (RMSF), and hydrogen bonding) was carried out to examine the overall stability and binding efficiency of the protein-ligand complex between compounds (Millesianin F, Millesianin G, Claclrastin-7-O-ß-d-glucopyranoside, 7-hydroxy-4',6 dimethoxyisoflavone-7-O-ß-d-apiofuranosyl-(1→6)-ß-d-glucopyranoside, 7-hydroxy-4',8-dimethoxyisoflavone 7-O-ß-d-apiofuranosyl-(1→6)-ß-d-glucopyranoside, Odoratin-7-O-ß-d-glucopyranoside, and 5,7,4'-trihydroxyisoflavone 7-O-ß-d-apiofuranosyl-(1→6)-ß-d-glucopyranoside) and PDE4 (A, B) subtype proteins. Compound D50 has shown strong anti-inflammatory activity, as evidenced by experimental results. It effectively inhibits PDE4B and PDE4D, with IC50 values of 6.56 ± 0.7 µM and 11.74 ± 1.3 µM, respectively. Additionally, it reduces NO production, with an IC50 value of 5.40 ± 0.9 µM. Based on these findings, it is promising and considered a potential novel anti-inflammatory drug for future development.

Millettia speciosa Champ cellulose-based hydrogel as a novel delivery system for Lactobacillus paracasei: Its relationship to structure, encapsulation and controlled release.

We report for the first time the usage of Millettia speciosa Champ cellulose (MSCC) and carboxymethylcellulose (MSCCMC) for the fabrication of 3D-network hydrogel as delivery system for probiotics. The structural features, swelling behavior and pH-responsiveness of MSCC-MSCCMC hydrogels and their encapsulation and controlled-release behavior for Lactobacillus paracasei BY2 (L. paracasei BY2) were mainly studied. Structural analyses demonstrated that MSCC-MSCCMC hydrogels with porous and network structures were successfully synthesized through the crosslinking of -OH groups between MSCC and MSCCMC molecules. An increasing concentration of MSCCMC significantly improved the pH-responsiveness and swelling ability of the MSCC-MSCCMC hydrogel toward neutral solvent. Besides, the encapsulation efficiency (50.38-88.91 %) and release (42.88-92.86 %) of L. paracasei BY2 were positively correlated with the concentration of MSCCMC. The higher the encapsulation efficiency was, the higher the release in the target intestine. However, due to the existence of bile salts, controlled-release behavior decreased the survivor rate and physiological state (degrading cholesterol) of encapsulating L. paracasei BY2. Even so, the number of viable cells encapsulated by hydrogels still reached the minimum effective concentration in the target intestine. This study provides an available reference for the practical application of hydrogels fabricated from the cellulose of the Millettia speciosa Champ plant for probiotic delivery.

Estrogenic and anti-amnesic potential of Millettia griffoniana Baill. (Fabaceae) ethanolic extract on scopolamine-induced memory impairment in ovariectomized Wistar rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Dementias including Alzheimer disease (AD) are three times higher in menopausal women than in men. Phytoestrogens, a group of plant-derived compounds are known to alleviate menopausal complaints including dementia. Millettia griffoniana Baill is a phytoestrogen-rich plant used to treat menopausal complaints and dementia. AIM: Evaluating the estrogenic and neuroprotective potential of Millettia griffoniana on ovariectomized (OVX) rats. MATERIALS AND METHODS: The in vitro safety of M. griffoniana ethanolic extract was assayed by MTT in human mammary epithelial (HMEC) and mouse neuronal (HT-22) cells and its lethal dose 50 (LD50) was estimated following OECD 423 guidelines. For estrogenicity, in vitro the well known E-screen assay on MCF-7 cells was performed and in vivo four groups of OVX rats were treated either with 75, 150 and 300 mg/kg M. griffoniana extract doses or estradiol (1 mg/kg BW) for three days; and changes in uterine and vagina were analyzed. Then, for neuroprotective effect, Alzheimer-type dementia induction was achieved by scopolamine (1.5 mg/kg B.W., i.p.) injection four days/week and M. griffoniana extract as well as piracetam (standard) were administered daily for 2 weeks to evaluate the extract's neuroprotective potential. The endpoints were the assessment of learning and working memory, oxidative stress state (SOD, CAT, and MDA) in brain, acetylcholine esterase (AChE) activity and the histopathological changes in hippocampus. RESULTS: No toxic effect was observed when incubating mammary (HMEC) and neuronal (HT-22) cells with M. griffoniana ethanol extract for 24 h and its LD50 was found >2000 mg/kg. The extract also exhibited both in vitro and in vivo estrogenic activities, displayed by a significant (p < 0.01) increment in MCF-7 cells population in vitro and an increase in the epithelium height of the vagina and the wet weight of the uterus mainly with the 150 mg/kg BW extract dose compared to untreated OVX rats. The extract also reversed scopolamine-induced memory impairment in rat by improving learning, working and reference memory. This was associated with an increment in CAT and SOD expression, alongside a decrement in MDA content and AChE activity in hippocampus. Further, the extract reduced neuronal cell loss in hippocampal structures (CA1, CA3 and dentate gyrus). High Performance Liquid Chromatography coupled with Mass Spectrometry (HPLC-MS) spectra, revealed the presence of numerous phytoestrogens in M. griffoniana extract. CONCLUSION: M. griffoniana ethanolic extract has estrogenic, anticholinesterase and antioxidant activities that could account for its anti-amnesic effects. These findings therefore sheds light on why this plant is commonly used in the therapy of menopausal complaints and dementia.

Purification, structural elucidation and biological activities of exopolysaccharide produced by the endophytic Penicillium javanicum from Millettia speciosa Champ.

An acid polysaccharide, named HP, was produced by endophytic Penicillium javanicum MSC-R1 isolated from southern medicine Millettia speciosa Champ. The molecular weight of HP was 37.8 kDa and consisted of Ara f, Galр, Glcр, Manр, and GlcрA with a molar ratio of 1.09: 3.47: 68.48: 16.59: 8.85. The glycosidic linkage of HP was proven to be →3, 4)-α-D-Glcр-(1→6)-α-D-Manр-(1→, →3, 4)-α-D-Glcр-(1→4)-α-D-Glcр-(1→, →3), →6)-α-D-Manр-(1→4)-α-D-Glcр-(1→, →3), ß-D-Galр-(1→3)-α-D-Glcр-(1→, →4), →5)-α-L-Ara f -(1→3)-α-D-Glcр-(1→, →4), →6)-α-D-Manр-(1→4)-α-D-GlcAр-(1→ and →4)-α-D-GlcAр-(1→4)-α-D-Glcр-(1→, →3). Additionally, 250 µg/mL of HP possessed nontoxicity to RAW 264.7 cells and exhibited anti-inflammation activity. HP could significantly restrain the amount of tumor necrosis factor-α, interleukin-6 and NO release in RAW264.7, which property is possibly associated with its abundant glucosidic linkage. These results indicated that HP could be regarded as a ponderable ingredient for the health-beneficial functional foods.

Extraction and characterization of a functional protein from Millettia speciosa Champ. leaf.

Natural plant-derived protein with excellent bioactivities has attracted much attention so a functional protein with molecular weight of 15.2 kDa was extracted from Millettia speciosa Champ. leaf for the first time. Under the pH of 12.0, solid-liquid ratio of 1:40 (w/v), extraction time of 2.0 h, and extraction temperature of 50 °C, the highest extracting efficiency (79.25 ± 0.78%) of the Millettia speciosa Champ. leaf protein (MLP) was achieved. The main structure of MLP contained ß-fold and ß-corner by Fourier transform infrared spectroscopy (FTIR) and Circular dichroism (CD) spectra analysis. Additionally, MLP was predominant with glutamic acid, aspartic acid, and leucine, which could be considered as a high quality natural protein. MLP showed great water holding capacity (WHC), oil absorption capacity (OAC), as well as emulsifying and foaming properties. Simultaneously, MLP exhibited considerable antioxidant activity. These results suggested that MLP could be utilised as a promising ingredient of functional foods.

Cytotoxic effect and antioxidant activity of pterocarpans from Millettia aboensis root.

Chemical analysis of the methanol extract of the root bark of Millettia aboensis led to the isolation of homopterocarpin (1), secundiflorol I (2), and maackain (3). The structures of these compounds were elucidated based on their MS and NMR spectra. The crude methanol root extract was screened for its cytotoxic activity on mouse lymphoma cell line (L5178Y), and the isolated compounds were tested for their antioxidant activity using a 2, 2-diphenylhydrazyl (DPPH) radical scavenging model. The crude methanol root extract gave a percentage growth inhibition of 87.5% on the mouse lymphoma cell line (L5178Y). Compound 3 gave the highest antioxidant activity with an IC50 of 83 µg/ml. These compounds can serve as leads for anticancer agents.

Hepatoprotective Effect of Millettia dielsiana: In Vitro and In Silico Study.

In silico docking studies of 50 selected compounds from Millettia dielsiana Harms ex Diels (family Leguminosae) were docked into the binding pocket of the PI3K/mTOR protein. In there, compounds trans-3-O-p-hydroxycinnamoyl ursolic acid (1) and 5,7,4'-trihydroxyisoflavone 7-O-ß-D-apiofuranosyl-(1→6)-ß-D-glucopyranoside (2) are predicted to be very promising inhibitors against PI3K/mTOR. They direct their cytotoxic activity against Hepatocellular carcinoma with binding affinity (BA) values, the pulling work spent to the co-crystallized ligand from the binding site of PI3K/mTOR (W and Fmax), and the non-equilibrium binding free energy (∆GneqJar) as BA values = -9.237 and -9.083 kcal/mol, W = 83.5 ± 10.6 kcal/mol with Fmax = 336.2 ± 45.3 pN and 126.6 ± 21.7 kcal/mol with Fmax = 430.3 ± 84.0 pN, and ∆GneqJar = -69.86074 and -101.2317 kcal/mol, respectively. In molecular dynamic simulation, the RMSD value of the PI3K/mTOR complex with compounds (1 and 2) was in the range of 0.3 nm to the end of the simulation. Therefore, the compounds (1 and 2) are predicted to be very promising inhibitors against PI3K/mTOR. The crude extract, ethyl acetate fraction and compounds (1 and 2) from Millettia dielsiana exhibited moderate to potent in vitro cytotoxicity on Hepatocellular carcinoma cell line with IC50 values of 81.2 µg/mL, 60.4 µg/mL, 23.1 µM, and 16.3 µM, respectively, and showed relatively potent to potent in vitro antioxidant activity on mouse hepatocytes with ED50 values of 24.4 µg/mL, 19.3 µg/mL, 30.7 µM, and 20.5 µM, respectively. In conclusion, Millettia dielsiana and compounds (1 and 2) are predicted to have very promising cytotoxic activity against Hepatocellular carcinoma and have a hepatoprotective effect.

Brandisianones F and G from Millettia brandisiana Kurz and their cytotoxicity.

A new flavanone and a new chalcone, brandisianones F and G, were purified from the roots of Millettia brandisiana Kurz, moreover, sixteen known compounds were found. The chemical structures of all isolated compounds were identified using spectroscopic methods including 1D-NMR, 2D-NMR, MS, IR and CD data. Chalcone 15 exhibited the most cytotoxic activity against liver cancer, HepG2, and cholangiocarcinoma, KKU-M156, cell lines with IC50 values of 1.74 ± 0.91 and 1.95 ± 0.95 µg/mL, respectively. Chalcones 2, 14, 16 and 18 as well as flavones 5, 6 and 12 showed moderate cytotoxicity with IC50 values ranging from 5.39 to 14.00 µg/mL.[Formula: see text].

Utilisation of Non-Edible Source (Pongamia pinnata Seeds Shells) for Producing Methyl Esters as Cleaner Fuel in the Presence of a Novel Heterogeneous Catalyst Synthesized from Waste Eggshells.

Waste eggshells were considered for synthesising a precursor (CaO) for a heterogeneous catalyst, further impregnated by alkali caesium oxide (Cs2O). The following techniques were used to characterise the synthesised catalysts: X-ray Diffraction (XRD), Scanning Electron Microscopy (SEM), Energy-dispersive X-ray spectroscopy (EDS), X-ray photoelectron spectroscopy (XPS) and Temperature Programmed Desorption (CO2-TPD). The synthesised catalyst revealed its suitability for transesterification to produce biodiesel. The biodiesel production process was optimised, and it showed that the optimal biodiesel yield is 93.59%. The optimal set of process parameters is process temperature 80 °C, process time 90 min, methanol-to-oil molar ratio 8 and catalyst loading 3 wt.%. It has been found that the high basicity of the catalyst tends to give a high biodiesel yield at low methanol-to-oil ratio 8 when the reaction time is also less (90 min). The fuel properties of biodiesel also satisfied the standard limits defined by ASTM and the EN standards. Thus, the synthesised catalyst from waste eggshells is highly active, improved the biodiesel production conditions and PPSS oil is a potential nonedible source.

A comparative appraisal of three important oil yielding plants for their biodiesel potential.

In the present scenario, alternative energy sources are required to achieve the future economic prosperity where shortage of fossil fuels will be a limiting factor and hamper the global economic growth. Therefore, interest in biofuel is increasing continuously. The best way of sustainable development is fossil fuel supplementation with biodiesel to reduce the fossil fuel demand. Biodiesel is a clean burning, ester-based, oxygenated fuel derived from natural and renewable sources. Till now, majority of the people have worked on the biodiesel derived from edible oil. Instead of using edible oil, non-edible oil needs to be explored as feedstock for biofuel because half of the world's population is unable to afford the food oil as feedstock for fuel production. Looking at the significance of biodiesel and the resources of biofuel, in this paper, a comparative exhaustive study has been reported with for three important plants, namely Jatropha curcas, Pongemia pinnata and Balanites aegyptiaca. These plants were selected based on their biodiesel potential, availability, cultivation practices and general information available. The present study involves scientometric publications, comparison of fatty acid composition and biodiesel parameters. We have also compared climatic conditions for the growth of the plants, economic feasibility of biodiesel production and other ecological services. The study paves a way for sustainable solution to policy makers and foresters looking for selection of plant species as bioenergy resource.

Health promoting benefits of pongamol: An overview.

Plant-derived chemicals are a source of novel chemotherapeutic agents. Throughout the human civilization, these novel chemicals have led to the discovery of new pharmacological active agents. Research on herbal medicine is of great importance, as most of the active agents used for treating numerous diseases are from natural sources, while other agents are either semisynthetic or synthetic. Pongamol, a flavonoid, which is the main constituent of Pongamia pinnata, is one such active agents, which exhibits diverse pharmacological activities. Various in vivo and in vitro studies revealed that pongamol is a potentially active agent, as it exerts anticancer, anti-inflammatory, antioxidant, antimicrobial, and anti-diabetic activities. Accordingly, the aim of the present review was to give an up-to-date overview on the chemistry, isolation, bioavailability, pharmacological activity, and health benefits of pongamol. This review focuses on the medicinal and health promoting activities of pongamol, along with possible mechanisms of action. For this purpose, this review summarizes the most recent literature pertaining to pongamol as a therapeutic agent against several diseases. In addition, the review covers information related to the toxicological assessment and safety of this phytochemical, and highlights the medicinal and folk values of this compound against various diseases and ailments.

Cytotoxicity of isoflavones from Millettia dura.

The first phytochemical investigation of the flowers of Millettia dura resulted in the isolation of seven isoflavones, a flavonol and a chalcone. Eleven isoflavones and a flavonol isolated from various plant parts from this plant were tested for cytotoxicity against a panel of cell lines, and six of these showed good activity with IC50 values of 6-14 µM. Durmillone was the most active with IC50 values of 6.6 µM against A549 adenocarcinomic human alveolar basal epithelial cancer cell line with low cytotoxicity against the non-cancerous cell lines BEAS-2B (IC50 = 58.4 µM), LO2 hepatocytes (IC50 78.7 µM) and CCD19Lu fibroblasts (IC50 >100 µM).

Quantification and Optimization of Ethanolic Extract Containing the Bioactive Flavonoids from Millettia pulchra Radix.

Millettia pulchra is traditionally used for treating diseases, including joint pain, fever, anemia, and allergies. It is also a potential resource of natural flavonoid derivatives, which represents major constituents of this plant. This study aimed to isolate the major compounds from M. pulchra radix, develop and validate the HPLC-PDA method to determine their contents, and optimize its extraction. Four major flavonoid derivatives (karanjin, lanceolatin B, 2",2"-dimethylpyrano-[5″,6″:7,8]-flavone, and pongamol) were isolated using silica gel column chromatography, crystallization techniques in large amounts with high purities (>95%). A simple, accurate high-performance liquid chromatography-photodiode array (HPLC-PDA) detection method has been developed and validated with significantly statistical impacts according to International Conference on Harmonization (ICH) guidelines. The Response Surface Methodology (RSM), Artificial Neural Network (ANN) models were employed to predictive performance and optimization of the extraction process. The optimized conditions for the extraction of major flavonoids were: extraction time (twice), solvent/material ratio (9.5), and ethanol concentration (72.5%). Our research suggests an effective method, which will be helpful for quality control in the pharmaceutical development of this species.

Derrischalcone suppresses cholangiocarcinoma cells through targeting ROS-mediated mitochondrial cell death, Akt/mTOR, and FAK pathways.

Chemotherapy is a palliative treatment for unresectable patients with cholangiocarcinoma (CCA). However, drug resistance is a major cause of the failure of this treatment. Derrischalcone (DC), a novel chalcone isolated from Derris indica fruit, has been shown pharmacologically active; though, the effect of DC on CCA is unknown. The present study investigated the cytotoxic, antiproliferative, anti-migration, and anti-invasion effects and underlying mechanisms of DC on CCA KKU-M156 and KKU-100 cells. Cytotoxicity and apoptosis were evaluated by acridine orange and ethidium bromide fluorescent staining. Reactive oxygen species (ROS) was measured by dihydroethidium assay. Cell proliferation and reproductive cell death were assessed by sulforhodamine B staining and colony-forming assay. Migration and invasion were determined by wound healing and transwell chamber assays. Protein expressions associated with cell death, proliferation, migration, and invasion were analyzed by western immunoblotting. We found that DC induced cytotoxicity and apoptosis in association with ROS formation and oxidative stress. Treatment with N-acetylcysteine suppressed ROS formation and attenuated DC-induced cytotoxic and apoptotic effects. DC increased the expression of p53, p21, Bax, and cytochrome c proteins in association with cell death. DC-induced antiproliferation, colony formation, anti-migration, and anti-invasion were associated with the suppression of Akt/mTOR/cyclin D1 and FAK signaling pathways. These findings suggest that the multi-targeting strategies with DC may be a novel treatment for cancer therapy.

Ameliorating effect on glycolipid metabolism and chemical profile of Millettia speciosa champ. extract.

ETHNOPHARMACOLOGICAL RELEVANCE: Millettia speciosa Champ., also called Niu dali, is a fabaceous medicinal plant mainly distributed in southeast China, where it is a functional food for developing physical strength, and often used traditionally in medicinal treatment of numbness of the wrists, diabetes, hepatitis, and so on. AIM OF THE STUDY: To investigate the chemical profile, ameliorating effects of MSC on glycolipid metabolism in diabetic mice and to identify the possible mechanism of action. MATERIALS AND METHODS: High-performance liquid chromatography coupled with electrospray ionization quadrupole time of flight mass spectrometry (HPLC-ESI-QTOF-MS) was applied to analyze the chemical compositions from M. speciosa extract (MSC). MSC was orally administered to high-fat diet and STZ-induced diabetic mice at doses of 4.55, 9.10 and 13.65 mg/(kg·d) respectively for 10 weeks. Indices of glycolipid metabolism, including fasting blood glucose (FBG), fasting insulin, insulin resistance index (IRI), blood lipids, HPA-axis hormones, and related gene expressions were evaluated. RESULTS: 86 compounds were tentatively identified from MSC, counting for 91.97% of the total extract, mainly including 23 alkaloids (including 2 cyanogenetic glycosides firstly identified in this species, total content accounted to 39.71%), 23 flavonoids (11.91%), 17 acids (including 3 amino acids, 9 phenolic acids and 5 organic acids; 9.2%), 9 terpenoids and steroids (20.13%), 7 esters (3.33%), 3 lignans (3.73%), 3 saccharides (4.0%) and 1 anthraquinone (0.18%). MSC could ameliorate the glycolipid disorder in diabetic mice markedly, and significant regulations on CRH and ACTH hormones were observed. Moreover, the cellular morphology of liver and pancreas were significantly improved and the expressions of IRS2, PI3K, Akt and GLUT4 were significantly up-regulated by MSC treatment. CONCLUSION: This was the first time to study the chemical profile and ameliorating effect on glycolipid metabolism of M. speciosa. It was found to be rich in flavonoids and alkaloids, which might support the potential relation of material foundation and the activity in regulating glycolipid metabolism. The ameliorating effect on glycolipid disorder in diabetic mice might be associated to the regulation of related hormones of the HPA axis and the IRS2/PI3K/Akt/GLUT4 signalling pathway. It was of great significance for advanced directed separation and pharmacological activity research of MSC.

Antimicrobial, antibiofilm, antioxidant, anticancer, and phytochemical composition of the seed extract of Pongamia pinnata.

Ethyl acetate seed extract of Pongamia pinnata displayed the highest antimicrobial potential against all test pathogens and Staphylococcus epidermidis was reported as the most sensitive strain with MIC/MBC 1.56/3.12 mg ml-1. It inhibited S. epidermidis biofilm 97.43% at MIC and LM as well as FE-SEM micrographs displayed extensive disintegration in biofilm. It showed the highest TPC (1.23 ± 0.04 g GAE g-1), TFC (0.95 ± 0.05 g CE g-1), and antioxidant activity with IC50 18.47 ± 0.33 µg ml-1. MTT assay displayed concentration-dependent strong cytotoxicity on K562 cells on the treatment of ethyl acetate extract with an IC50 value of 84.41 µg ml-1. On the other hand, it showed minute cytotoxicity on normal PBMCs with an IC50 value of 410.14 µg ml-1. GC-MS analysis revealed that Hexadecanoic acid (35.97%); 2-(1,3-Benzodioxol-5-yl)furo[2,3-h]chromen-4-one (Pongaglabrone) (22.82%); 2,2-Dimethylindane-1,3-dione- (13.05%) were the three major components in ethyl acetate extract. The present investigation showcases ethyl acetate extract as a potent antimicrobial, antibiofilm, antioxidant, and anticancer agent that opens a new avenue for its phytochemicals as a therapeutic agent.