Dual Function Antimicrobial Loaded Lectin Carrier: A Strategy to Overcome Biomolecular Interference without Detectable Resistance.

The disposition of a drug in a biological system may be altered by complex biological fluids; especially, protein binding to drugs influences their activity. Herein, we demonstrated a convenient method involving the noncovalent formulation of butea monosperma seed lectin (BMSL) with an antimicrobial lipid, cationic N-acylethanolamine (cNAE) to mitigate the serum protein interference. Fluorescence spectroscopy and molecular docking study revealed that cNAEs readily formed noncovalent complexes with serum protein, bovine serum albumin. The resulting complexes interfered with the antimicrobial activity of cNAEs. Strikingly, the noncovalent conjugates developed with BMSL and cNAEs (BcNAE) overcame the interference from serum protein and displayed remarkable antimicrobial activity against uropathogenic Escherichia coli (UPEC). Strikingly, the minimum inhibitory concentration (MIC) of the lectin conjugates (7.81 µM) was 4-fold lower than the MIC of pure cNAE. Mechanistic studies showed that BcNAE depolarized the bacterial membrane and affected the integrity to exert the antimicrobial activity. The membrane directed activities of BcNAE on UPEC efficiently eliminated the development of resistance even after 25 passages. The hemocompatibility results and the biosafety assessed in a zebrafish model suggested that BcNAE was nontoxic with good selectivity to bacteria. While testing the therapeutic efficacy against UPEC infected zebrafish, we found that 1× MIC cNAE is ineffective due to interference from biological fluids, which is in agreement with in vitro studies. Remarkably, the infected fish treated with 1× MIC BcNAE conjugates were rescued from infection and restored to the normal life in less than 9 h. Bacterial colony count assay revealed that BcNAE was more efficient in overcoming the biological fluid interference and eliminated the bacterial burden in infected zebrafish. Histopathology analysis supported that BcNAE treatment restored the pathological changes induced by UPEC and, thus, increased survival. The high antimicrobial intensity with limited chance for resistance development and potential to overcome biomolecular interference with a lack of toxicity enhance the merits of exploring lectin conjugates against infectious pathogens.

Antitumor potential of the protein phosphatase inhibitor, cantharidin, and selected derivatives.

Cantharidin is a potent natural protein phosphatase monoterpene anhydride inhibitor secreted by several species of blister beetle, with its demethylated anhydride analogue, (S)-palasonin, occurring as a constituent of the higher plant Butea frondosa. Cantharidin shows both potent protein phosphatase inhibitory and cancer cell cytotoxic activities, but possible preclinical development of this anhydride has been limited thus far by its toxicity. Thus, several synthetic derivatives of cantharidin have been prepared, of which some compounds exhibit improved antitumor potential and may have use as lead compounds. In the present review, the potential antitumor activity, structure-activity relationships, and development of cantharidin-based anticancer drug conjugates are summarized, with protein phosphatase-related and other types of mechanisms of action discussed. Protein phosphatases play a key role in the tumor microenvironment, and thus described herein is also the potential for developing new tumor microenvironment-targeted cancer chemotherapeutic agents, based on cantharidin and its naturally occurring analogues and synthetic derivatives.

A Novel Serum Glycobiomarker for Diagnosis and Prognosis of Cholangiocarcinoma Detected by Butea monosperma Agglutinin.

Plant lectins are widely used in medical glycosciences and glycotechnology. Many lectin-based techniques have been applied for the detection of disease-associated glycans and glycoconjugates. In this study, Butea monosperma agglutinin (BMA), a lectin purified from seeds of the medicinal plant Butea monosperma, was used for the detection of cholangiocarcinoma (CCA)-associated glycans. Expression of BMA-binding N-acetyl galactosamine/galactose (GalNAc/Gal)-associated glycan (BMAG) in CCA tissues was determined using BMA lectin histochemistry; the results showed that BMAG was undetectable in normal bile ducts and drastically increased in preneoplastic bile ducts and CCA. The study in hamsters showed that an increase of BMAG was associated with carcinogenesis of CCA. Using an in-house double BMA sandwich enzyme-linked lectin assay, BMAG was highly detected in the sera of CCA patients. The level of serum BMAG in CCA patients (N = 83) was significantly higher than non-CCA controls (N = 287) and it was applicable for diagnosis of CCA with 55.4% sensitivity, 81.9% specificity, and 76.0% accuracy. A high level of serum BMAG (≥82.5 AU/mL) was associated with unfavorable survival of CCA patients; this information suggested the potential of serum BMAG as a poor prognostic indicator of CCA. In summary, BMAG was aberrantly expressed in preneoplastic bile ducts and CCA, it was also highly detected in patient serum which potentially used as a marker for diagnosis and prognostic prediction of CCA.

Revealing the Significance of the Glycan Binding Property of Butea monosperma Seed Lectin for Enhancing the Antibiofilm Activity of Silver Nanoparticles against Uropathogenic Escherichia coli.

The incompetence of conventional antibiotics against bacteria residing in biofilms demands newer therapeutic intervention. In this study, we demonstrated that the interaction between silver nanoparticles (AgNPs) and Butea monosperma seed lectin (BMSL) forms efficient surface-functionalized AgNPs with excellent antibiofilm competency against uropathogenic Escherichia coli (UPEC). The minimum biofilm inhibitory concentration (MBIC) of AgNPs and the BMSL-AgNP conjugate (BAgNP) against UPEC was 75 and 9.37 µM, respectively. The eight-fold reduction in the MBIC of AgNPs was attributed to lectin functionalization. The chemical modification of serine amino acids affects the hemagglutination activity of BMSL but not its interaction with the AgNPs. At the same time, AgNPs surface-functionalized with modified BMSL display poor antibiofilm activity. Molecular docking studies revealed that BMSL binds to galactose with a free energy of -5.72 kcal/mol, whereas the serine residue-modified BMSL showed the lowest free energy values, suggesting incompetence for binding galactose. These results showcase that the sugar binding site of BMSL aids in the adhesion of AgNPs to the biofilm matrix and disturbs the formation of the biofilm, which was confirmed by light microscopy using crystal violet staining. At 37.5 µM, BAgNPs also have the capability to eradicate preformed biofilm. As a proof of concept, UPEC biofilm prevention and eradication were demonstrated on a urinary catheter. A scanning electron microscopy study showed that BAgNPs prevent bacterial colonization and thereby curtail biofilm growth. In addition to antibiofilm activity, BAgNPs exert antibacterial activity at 18.75 µM, which is four-fold lower than the MIC of AgNPs. A mechanistic study revealed that BAgNPs affect the integrity of the bacterial outer membrane and generate an imbalance in the antioxidant defense, which induces cell death. The results highlight that lectin functionalization can be extended to other nanoparticles and different antibiotics to enhance their efficacy against drug-resistant bacteria.

Functional characterization and in vitro screening of Fructobacillus fructosus MCC 3996 isolated from Butea monosperma flower for probiotic potential.

The fructophilic bacterium Fructobacillus fructosus MCC 3996 described in the present investigation was isolated from the nectar of Butea monosperma flower and evaluated in vitro for the manifestation of probiotic features. The strain utilizes fructose faster than glucose and is capable to grow in the range of 1-35% fructose concentration (optimum 5% w/v) and thus denotes its fructophilic nature. In vitro assessments of the strain have examined for the endurance in acidic environment/gastric juice, the better auto-aggregation ability even in the presence of hydrolytic enzymes, co-aggregation with pathogenic bacteria, hydrophobicity properties and no haemolytic activity to elucidate its feasible probiotic use. The significant antagonistic activity against several detrimental bacteria, despite lacking the bacteriocin secretion, is an astonishing feature. Owing to the indigenous origin of the isolate, it could be used as a probiotic, starter culture, and/or the active ingredient of food formulation may contribute to improve the desirable fermentation, long-term storage and nutritional benefits of foods especially rich in fructose. SIGNIFICANCE AND IMPACT OF THE STUDY: This study provided in vitro evidence that Fructobacillus fructosus MCC 3996 have endurance in acidic gastric juice, better co-aggregation, auto-aggregation properties, splendid antagonistic activities against several bacteria involved in food spoilage/human infections, pertinent antibiotic susceptibility profile and no haemolytic activity. Also, F. fructosus have the capability to survive in the appreciable amount of fructose, and this advocates that the strain could be used as starter culture and/or the active ingredient of fructose-rich foods. The current in vitro study provided a strong basis for further in vivo research to identify the health beneficial characteristics of F. fructosus and its potential could be effectively utilized as health-boosting ingredient in food and pharmaceutical industries.

Butea monosperma (Lam.) Taub. Bark fractions protect against free radicals and induce apoptosis in MCF-7 breast cancer cells via cell-cycle arrest and ROS-mediated pathway.

Butea monosperma (Lam.) Taub. is an ethnomedicinal tree of remedial value in the treatment of diabetes, bone fractures, and liver and neurological disorders. However, the information available on DNA-protective and anti-proliferative potential of bark of this tree is scarce. In the present study, the extract/fractions obtained from bark of B. monosperma were evaluated for antioxidant, DNA-protective, and anti-proliferative activities, along with their phytochemical profiling for identifying major constituents present in them. Different extract/fractions, namely, Bmth (methanol), Bhex (hexane), Bchl (chloroform), and Beac (ethyl acetate), were prepared and evaluated for antioxidant activity using in vitro assays. Extract/fractions were also evaluated for anti-proliferative and apoptotic activity in human breast carcinoma cell line MCF-7, using in vitro assays, namely, MTT, clonogenic, and neutral comet assay, along with confocal microscopy and flow cytometry. Among all extract/fractions, a pronounced antioxidant activity was exhibited by Bchl and Beac fractions, in DPPH· (EC50 213.2 and 161.5 µg/mL, respectively), ABTS+· (EC50 139.3 and 44.1 µg/mL, respectively), and reducing power assay (EC50 86.7 and 84.5 µg/mL, respectively). Both fractions protected plasmid DNA against hydroxyl radical induced damage in plasmid nicking assay. Bchl and Beac were also observed to inhibit the growth of MCF-7 cells (GI50 203.7 and 246.5 µg/mL, respectively). Both fractions induced apoptosis in MCF-7 cells, by arresting the cell cycle in G1 and sub-G1 phase, respectively, enhancing ROS levels, decreasing mitochondrial membrane potential, and inducing double-strand DNA breaks. HPLC analysis revealed high kaempferol content in Bchl, and catechin, epicatechin, and gallic acid in Beac.

Biological activities of three medicinal plants from district Mirpur, AJK, Pakistan.

Present research work was aimed to investigate the biological activities i.e. antibacterial, antifungal, antioxidant, cytotoxic and antitumor activities of crude methanolic extract of Anagallis arvensis L., Butea monosperma (Lam.) Kuntze and Coronopus didymus (L.) Pers. against Gram positive strains (Bacillus subtilis, Staphylococcus aureus) and gram negative strains (Vibrio cholera, Enterobacter aerogenes, Klebsiella pneumonia, Agrobacterium tumefaciens, Escherichia coli) were screened. Best activity was observed against K. pneumonia and S. aureus by A. arvensis compared with other strains. Butea monosperma exhibited considerable activity against S. aureus, V. cholera, E. aerogenes and K. pneumonia compared with other strains. Methanolic extract of A. arvensis L. inhibited fungal growth against A. niger up to 30.2%. B. monosperma inhibited the growth of A. niger up to 43.5% and against A. fumigatus 27.3%. C. didymus inhibited the A. fumigates up to 27.3% and against A. niger, it inhibited 48%. Brine shrimps lethality bioassay was used to evaluate the cytotoxic activity and LD50 value was calculated by using probit analysis. Potato disc bioassay was designed to screen antitumor activity and data was analyzed by one way ANOVA.

Protective effects of Butea frondosa leaves against stress induced immune impairment in sprague dawley rats.

Stress is thought to impair immune function through emotional or behavioral manifestations thus the present study was done to assessed the effect of ethanolic extract of Butea frondosa (BF) leaves on behaviour, immunomodulatory activity and brain acetyl cholinesterase activity in normal and stress induced male rats. Neuroprotective effects of BF, doses (100,200,400mg/kg p.o) were measured by assessing the changes in the behaviour and the immunity of the rats. In stress control, the results indicated that the retention transfer latency, time spent in a closed arm, agglutination, total leukocytes counts (TLC), total paw edema ,size of spleen , decreased significantly (p<0.01) while glucose level, size of the kidney and the liver, AChE activity increased significantly (p<0.01) in comparison with normal control. In BF (200mg/kg) treated rats, the results indicated that the time spent in a closed arm (p<0.01), agglutination (p<0.01), TLC (p<0.01), total paw edema (p<0.05), size of spleen(p<0.01), increased significantly while glucose level (p<0.01), size of the kidney and the liver (p<0.01), AChE activity (p<0.01) decreased significantly in comparison with stress control. This study therefore concluded that the ethanolic extract of BF (200mg/kg) showed a protective effect against the stress induced impaired immune system and the psychological disorders.

Superbanone, A New 2-Aryl-3-benzofuranone and Other Bioactive Constituents from the Tube Roots of Butea superba.

Phytochemical investigation from the tube roots of Butea superba, led to the isolation and identification of a new 2-aryl-3-benzofuranone named superbanone (1), one benzoin, 2-hydroxy-1-(2-hydroxy-4-methoxyphenyl)-2-(4-methoxyphenyl)ethanone (2), eight pterocarpans (3 - 10), and eleven isoflavonoids (11 - 21). Compound 2 was identified for the first time as a natural product. The structure of the isolated compounds was elucidated using spectroscopic methods, mainly 1D- and 2D-NMR. The isolated compounds and their derivatives were evaluated for α-glucosidase inhibitory and antimalarial activities. Compounds 3, 7, 8, and 11 showed promising α-glucosidase inhibitory activity (IC50  = 13.71 ± 0.54, 23.54 ± 0.75, 28.83 ± 1.02, and 12.35 ± 0.36 µm, respectively). Compounds 3 and 11 were twofold less active than the standard drug acarbose (IC50  = 6.54 ± 0.04 µm). None of the tested compounds was found to be active against Plasmodium falciparum strain 94. On the basis of biological activity results, structure-activity relationships are discussed.

Inhibitory Activities of Butanol Fraction from Butea monosperma (Lam.) Taub. Bark Against Free Radicals, Genotoxins and Cancer Cells.

The present study was undertaken to investigate antioxidant, antigenotoxic, and antiproliferative activity of butanol fraction (Bmbu) from bark of medicinal plant Butea monosperma. Antioxidant potency of Bmbu was examined by various in vitro assays. It was also investigated for antigenotoxic activity using Escherichia coli. PQ37 employing SOS chromotest. Further, cytotoxic and apoptosis inducing activity of Bmbu was evaluated in MCF-7 breast cancer cells. Bmbu showed potent free radical scavenging ability in ABTS assay (IC50 56.70 µg/ml) and anti-lipid peroxidation ability (IC50 40.39 µg/ml). 4NQO and H2 O2 induced genotoxicity was suppressed by Bmbu in SOS chromotest by 74.26% and 82.02% respectively. It also inhibited the growth of MCF-7 cells with GI50 value of 158.71 µg/ml. Induction of apoptosis in MCF-7 cells by Bmbu treatment was deciphered using confocal microscopy, flow cytometry, and neutral comet assay. Bmbu treatment increased cell population in sub-G1 phase (69.6%) indicating apoptotic cells. Further, Bmbu treatment resulted in increased reactive oxygen species generation and decreased mitochondrial membrane potential indicating involvement of mitochondrial dependent pathway of apoptosis. HPLC profiling showed the presence of polyphenols such as ellagic acid, catechin, quercetin, and gallic acid as its major constituents. Consequently, it is suggested that the phytoconstituents from this plant may be further exploited for development of novel drug formulation with possible therapeutic implication.

Comparative protein profiles of Butea superba tubers under seasonal changes.

Seasonal changes are major factors affecting environmental conditions which induce multiple stresses in plants, leading to changes in protein relative abundance in the complex cellular plant metabolic pathways. Proteomics was applied to study variations in proteome composition of Butea. superba tubers during winter, summer and rainy season throughout the year using two-dimensional polyacrylamide gel electrophoresis coupled with a nanoflow liquid chromatography coupled to electrospray ionization quadrupole-time-of-flight tandem mass spectrometry. A total of 191 protein spots were identified and also classified into 12 functional groups. The majority of these were mainly involved in carbohydrate and energy metabolism (30.37 %) and defense and stress (18.32 %). The results exhibited the highest numbers of identified proteins in winter-harvested samples. Forty-five differential proteins were found in different seasons, involving important metabolic pathways. Further analysis indicated that changes in the protein levels were due mainly to temperature stress during summer and to water stress during winter, which affected cellular structure, photosynthesis, signal transduction and homeostasis, amino-acid biosynthesis, protein destination and storage, protein biosynthesis and stimulated defense and stress mechanisms involving glycolytic enzymes and relative oxygen species catabolizing enzymes. The proteins with differential relative abundances might induce an altered physiological status within plant tubers for survival. The work provided new insights into the better understanding of the molecular basis of plant proteomes and stress tolerance mechanisms, especially during seasonal changes. The finding suggested proteins that might potentially be used as protein markers in differing seasons in other plants and aid in selecting B. superba tubers with the most suitable medicinal properties in the future.

[New study on species of Chinese medicine dragon's blood].

Through comprehensive study on the descriptions of dragon's blood in traditional medical books, we pointed out that before Tang Dynasty, Butea monosperma was used as dragon's blood; during Tang and Song Dynasty, Liquidambar formosana. was used as dragon's blood; in Commentaries on the illustrations of Song Dynasty, the author made a mistake by combined the descriptions of Butea monosperma with the descriptions of the prepared medicine of Dracaena cochinchinensis in dragon's blood, and thus the oversea species D. cochinchinensis became the mainstream of dragon's blood source in homeland. Until the foundation of the Republic of China, Daemonorops draco replaced D. cochinchinensis to the main source of dragon's blood.

Butea superba-induced amelioration of cognitive and emotional deficits in olfactory bulbectomized mice and putative mechanisms underlying its actions.

This study investigated the effects of alcoholic extract of Butea superba (BS) on cognitive deficits and depression-related behavior using olfactory bulbectomized (OBX) mice and the underlying molecular mechanisms of its actions. OBX mice were treated daily with BS (100 and 300 mg/kg, p.o.) or reference drugs, tacrine (2.5 mg/kg, i.p.) and imipramine (10 mg/kg, i.p.) from day 3 after OBX. OBX impaired non-spatial and spatial cognitive performances, which were elucidated by the novel object recognition test and modified Y maze test, respectively. These deficits were attenuated by tacrine and BS but not imipramine. OBX animals exhibited depression-like behavior in the tail suspension test in a manner reversible by imipramine and BS but not tacrine. OBX down-regulated phosphorylation of synaptic plasticity-related signaling proteins: NMDA receptor, AMPA receptor, calmodulin-dependent kinase II, and cyclic AMP-responsive element-binding protein. OBX also reduced choline acetyltransferase in the hippocampus. BS and tacrine reversed these neurochemical alterations. Moreover, BS inhibited ex vivo activity of acetylcholinesterase in the brain. These results indicate that BS ameliorates not only cognition dysfunction via normalizing synaptic plasticity-related signaling and facilitating central cholinergic systems but also depression-like behavior via a mechanism differing from that implicated in BS amelioration of cognitive function in OBX animals.

Ethanol extract of Butea monosperma bark modulates dyslipidemia in streptozotocin-induced diabetic rats.

CONTEXT: Dyslipidemia is one of the major risk factors for cardiovascular disease in diabetes mellitus (DM). The availability of multiple lipid-lowering drugs and supplements provides new opportunities for patients to regulate lipid levels. OBJECTIVE: The present study was designed to evaluate the effect of Butea monosperma Lam. (Fabaceae) bark extract in diabetes-induced dyslipidemia. MATERIALS AND METHODS: A daily dose of B. monosperma bark extract (BMBE, 500 mg/kg body weight) was given orally to streptozotocin (STZ)-induced diabetic rats for 60 d. Several indices such as blood glucose, insulin, glycosylated hemoglobin, TC, TG, high-density lipoprotein-cholesterol (HDL-C), apo A1, apo B, activities of lipogenic enzymes in tissues, liver function tests, and histopathology of liver were analyzed to assess the modulation of STZ-induced diabetic dyslipidemia by B. monosperma bark. RESULTS: BMBE significantly reduced blood glucose (40.79%) and increased plasma insulin (37.5%) levels in diabetic rats. Altered levels of serum lipids, lipoproteins, and activities of lipogenic enzymes in tissues were partially restored upon the administration of BMBE in diabetic rats. Liver function tests and histopathological examination revealed that consumption of BMBE at a dose of 500 mg/kg body weight had no toxic effects in experimental rats. CONCLUSION: The findings suggest that BMBE supplementation could ameliorate dyslipidemia in DM.

Free radical scavenging and anti-isolated human LDL oxidation activities of Butea superba Roxb. extract.

BACKGROUND: Butea superba Roxb. (B. superba), is an herbal plant traditionally used for rejuvenation. Additionally, there have been reports on its antioxidant properties. Low-density lipoproteins (LDL) oxidation is the leading cause of cardiovascular diseases (CVDs). Natural products with antioxidant properties have the potential to inhibit LDL oxidation. However, no work has been done about the anti-isolated human LDL oxidation of B. superba extract (BSE). This study aimed to investigate the antioxidant potential of BSE and its ability to prevent isolated human (LDL) oxidation induced by free radical agents. METHODS: The antioxidant properties were investigated by antioxidant assays, including 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azinobis-(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS), ferric reducing ability power (FRAP), nitric oxide (NO) and peroxynitrite scavenging assay. More so, anti-isolated human LDL oxidation activities were evaluated by 2,2'-azobis (2-amidinopropane) dihydrochloride (AAPH) and 3-morpholinosydnonimine hydrochloride (SIN-1) induced LDL oxidation assay. RESULTS: BSE exhibited a significant (p < 0.05) antioxidant activity in all the test systems, demonstrating its potential as a potent free radical scavenger. It displayed scavenging effects on DPPH (p < 0.05; IC50 = 487.67 ± 21.94 µg/ml), ABTS (p < 0.05; IC50 = 30.83 ± 1.29 µg/ml). Furthermore, it generated significantly (p < 0.05) increased antioxidant capacity in a dose-dependent manner in FRAP assay and exhibited significantly (p < 0.01) higher percent NO scavenging activity than gallic acid. Besides, BSE at 62.5 µg/ml exhibited a considerable percent peroxynitrite scavenging of 71.40 ± 6.59% after a 2 h period. Moreover, BSE demonstrated anti-isolated human LDL oxidation activity induced by AAPH and SIN-1 (p < 0.05) and revealed scavenging activity similar to ascorbic acid (p > 0.05). Identifying the main constituents of BSE revealed the presence of genistein, daidzein, and biochanin A through Liquid Chromatography-Mass Spectrometer/Mass Spectrometer (LC-MS/MS) analysis. CONCLUSION: This is the first report that the presence of isoflavones in BSE could play an important role in its antioxidation and isolated human LDL oxidation scavenging properties. These findings suggest the potential for developing antioxidant herbal supplements. However, further studies must be investigated, including efficacious and safe human dosages.

Antinociceptive effect of Butea monosperma on vincristine-induced neuropathic pain model in rats.

Neuropathic pain is a chronic neurodegenerative disease. It is well characterized by spontaneous pain, hyperalgesia, hypothesia, dysesthesia and allodynia. The present study was designed to investigate the antinociceptive potential of Butea monosperma on vincristine-induced painful neuropathy in rats. Vincristine was administered for induction of neuropathic pain in experimental animals. Hot plate, acetone drop, paw pressure, Von Frey hair and tail immersion tests were performed to assess the degree of thermal hyperalgesia, cold chemical allodynia, mechanical hyperalgesia and allodynia in the hind paw and tail thermal hyperalgesia, respectively, as an index of peripheral and central pain sensation. Tissue thiobarbituric acid reactive substances (TBARSs), reduced glutathione (GSH) and total calcium levels were estimated to assess the biochemical changes in the sciatic nerve tissue. Microscopically, histopathological changes were also observed in the sciatic nerve tissue. Ethanolic extract of B. monosperma leaves and pregabalin were administered for 14 consecutive days. Vincristine administration resulted in significant reduction in behavioural (i.e. hyperalgesia and allodynic pain sensation) changes along with a rise in the levels of TBARS, total calcium and decrease in GSH levels when compared with the normal control group. Moreover, significant histological changes were also observed. Pretreatment with B. monosperma significantly attenuated vincristine-induced development of painful behavioural, biochemical and histological changes in a dose-dependent manner, which is similar to that of pregabalin-pretreated group. B. monosperma ameliorated vincristine-induced painful neuropathy. It may be due to its potential of antioxidative, neuroprotective and calcium channel inactivation.

Ameliorating effect of lyophilized extract of Butea frondosa leaves on scopolamine-induced amnesia in rats.

CONTEXT: Butea frondosa (BF) Roxb. & Koen. (syn. B. monosperma Lam.) (Fabaceae) leaves have been used in folklore medicine for the treatment of diabetes, conjunctivitis, gastrointestinal tract, and central nervous system disorders such as anxiety, amnesia, etc. OBJECTIVE: To evaluate the effect of lyophilized hydroalcoholic extract of BF leaves (BFLE) at 100, 200 and 400 mg/kg, p.o., for its memory enhancing activity against scopolamine-induced amnesia in rats. MATERIALS AND METHODS: Antiamnesic effect of the BFLE was evaluated using Morris water maze and object recognition test models. The effect of BFLE on acetylcholinesterase activity and malondialdehyde and glutathione levels were also evaluated in brain homogenate. RESULT: BFLE ameliorates scopolamine-induced amnesia in both the models with maximum effect at 400 mg/kg. BFLE (400 mg/kg) decreased escape latency and increased time spent in target quadrant (24.2 and 42.5 s, respectively) in comparison to scopolamine (82 and 18.2 s, respectively) in the Morris water maze task. In the object recognition test, BFLE produced significant increase in ability to discriminate between novel and familiar objects. The highest investigated dose of BFLE (400 mg/kg), produced a significant decrease in acetylcholinesterase activity and malondialdehyde levels, and improves glutathione levels in comparison to scopolamine. Moreover, this effect of BFLE at 400 mg/kg was comparable to that of standard, donepezil. CONCLUSION: BFLE exhibited significant antiamnesic activity in rats thereby validating its folklore use.

Curcumin-loaded Butea monosperma gum-based hydrogel: A new excipient for controlled drug delivery and anti-bacterial applications.

The wide spectrum of applications provided by curcumin has attracted researchers worldwide to identify its molecular targets and employ it in various biomedical applications. The present research work focuses on the development of a Butea monosperma gum-based hydrogel encapsulated with curcumin and further employing it for two diverse applications, i.e., drug delivery and anti-bacterial application. A central composite design was utilized for the optimization of significant process variables to achieve maximum swelling. A maximum of 662 % swelling was attained at initiator (0.06 g), monomer (3 ml), crosslinker (0.08 g), solvent (14 ml), and time (60 s). Furthermore, the characterization of the synthesized hydrogel was performed via FTIR, SEM, TGA, H1-NMR, and XRD analysis. Various important properties like swelling rate under different solutions, water retention capacity, re-swelling capability, porosity, and density measurement suggested that the prepared hydrogel exhibited a highly stable crosslinked network with high porosity (0.23) and density (62.5 g/cm3) values. The encapsulation efficiency of curcumin in the hydrogel was reported to be 93 % and 87.3 %, respectively, wherein BM-g-poly(AA) âˆ¼ Cur exhibited excellent sustained pH-responsive site release of curcumin at two different pH values, with the maximum amount of release taking place at pH 7.4 (792 ppm) and a minimum at pH 5 (550 ppm) due to the lesser ionization of the functional groups present in the hydrogel at a lower pH value. Additionally, the results from the pH shock studies indicated our material to be stable and efficient even with fluctuations in pH, resulting in the optimal amount of drug release at each pH range. Furthermore, anti-bacterial studies revealed that the synthesized BM-g-poly(AA) âˆ¼ Cur was effective against both gram-negative and gram-positive bacteria, with maximum values of zones of inhibition of 16 mm in diameter, thereby showing the best results in comparison to the already developed matrices till date. As a result, the newly discovered BM-g-poly(AA) âˆ¼ Cur properties reflect the hydrogel network's suitability for drug release and anti-bacterial applications.

Plasticity of photosynthetic performance of the Indian tree Butea monosperma TAUB at three sites with different microclimates.

The Fabaceae tree Butea monosperma (TAUB.; syn. Erythrina monosperma (LAM.)) is widely distributed in Central and West-India. We studied it at three sites, i.e. at two locations with contrasting exposure (NE and SW, respectively) in a small mountain range with poor soil on highly drained rocky slopes and at a third location in a plane with deeper soils and better water supply. The two mountain range sites differed in the light climate where the NE-slope obtained more day-integrated irradiance. Chlorophyll fluorescence was measured with a portable fluorometer and leaf samples for stable isotope analyses (δ(13)C, δ(15)N, δ(18)O) were collected. No differences were seen in carbon and nitrogen contents of leaves at the three sites. N and O isotope signatures of the leaves were similar at the two rocky hill slope sites. More positive values for both signatures were obtained in the leaves in the plane. For all sites saturation of ETR was only achieved well above a PPFD of 1,000 µmol m(-2) s(-1) indicating that the leaves were sun-type leaves. The photosynthetic performance of Butea at the plane was very similar to that at the SW-slope of the mountain range and higher ETRs were obtained at the NE-slope. Ecophysiological flexibility allows Butea to perform well in a variety of habitats and yet gives it particular fitness at specific sites. The best performance was observed in the highly insolated steep rocky hill site (NE-slope) underlining the suitability of the tree for reforestation.

Butea superba (Roxb.) improves penile erection in diabetic rats.

The objective of the present study was to investigate the effect of ethanolic extract of Butea superba (Roxb.) on erectile dysfunction in diabetic rats by the measurement of intracavernous pressure (ICP) and on cavernosal smooth muscle relaxation. Male Sprague-Dawley rats were induced to become diabetic by a single intravenous injection of Streptozotocin (55 mg kg(-1) body weight). The ethanolic extract at the concentration of 1, 10 and 100 mg kg(-1) BW was administered orally once a day to diabetic rats in each group for 4 weeks. Diabetic rats showed a significant decrease in both ICP and the relaxation of the cavernosal smooth muscle compared with the normal rats. The extract of B. superba significantly increased the ICP with the effective dose of 10 mg kg(-1) BW (61.00 ± 11.11 mmHg versus 39.61 ± 11.01 mmHg in the diabetic control group). Moreover, the B. superba-treated group also showed enhanced relaxation of the cavernosal smooth muscle with EC(50) of 1.17 mg ml(-1). These results suggest that the extract of B. superba enhanced penile erection in diabetic rats by increasing the ICP. This might be explained by the increased blood flow as a result of the relaxation of the cavernous smooth muscle.