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The aim of the study was to explore the antioxidant and free radical scavenging activity of bark of Dillenia indica L. The methanolic extract (CME) of coarse powder of the dried bark was fractionated with pet-ether (PETF), chloroform (CHF), and water (AQF) and each fraction was investigated for antioxidant and free radical potentials. The phenolic contents of CME, CHF, PETF and AQF were found to be 90.2, 171.1, 52.1 and 158.1 and flavonoid contents 182.6, 340.2, 285.9, and 362.6 mg of GAE/g of dried extract, respectively. The total antioxidant activity of CME, PETF, CHF, AQF and standard catechin in terms of absorbance were 0.373, 0.707, 0.88, 1.051 and 0.804, respectively at 160 μg/ml concentration indicating AQF possessing the highest total antioxidant activity. In DPPH radical scavenging activity, the AQF and CHF showed potential radical scavenging activity followed by CME and PETF with IC50 values of 1.5, 2.5, 23 and 61 μg/ml, respectively, whereas standard ascorbic acid showed IC50 at 8 μg/ml. Among the extractives, AQF and CHF exhibited potent hydroxyl radical scavenging activity with IC50 values of 49.0 and 42 μg/ml followed by CME and PETF with IC50 of 86 and 168 μg/ml, respectively. In ferric-reducing antioxidant assay, AQF, CHF and CME (absorbance 2.262, 2.418 and 2.157, respectively) showed higher activity than that of standard (1.793) followed by PETF (absorbance 0.593). Since polyphenols like flavonoids play a vital role in controlling antioxidants, polyphenol rich extracts are potent source of antioxidants. Our data showed that the chloroform fraction of the bark of D. indica provided highest polyphenols and antioxidant activities, hence, can be used further as a source of natural antioxidants. Bangladesh Pharmaceutical Journal 25(1): 38-43, 2022 (January)

The health professionals require scientific knowledge to advise their patients on complementary and alternative medicines (CAM). Previously, several studies were conducted regarding the CAM perception, attitude and use on health care professionals only; in contrast, our study encompasses both students of health care professionals and other disciplines. The aim of this study was to compare the attitudes and perception about CAM practices between students of biological sciences (Biochemistry and Molecular Biology, Microbiology and Botany) and health care professionals (Pharmacy and medical students) in public and private universities located in the southeastern region in Bangladesh. The questionnaire-based study conducted on 332 systematically sampled students (four private and one public universities) located in the southeastern region in Bangladesh. The cross-sectional study was conducted from March to July, 2018. All students showed a positive attitude towards CAM use. Herbal medicine, homeopathy, nutritional supplements followed by hypnosis, massage, spiritual healing, and meditation were the most commonly known and used CAM modalities. Most of the students (40.7%) believed that the integration of CAM and conventional medicine should be essential in health care setting. The major obstacles for CAM use are patient interest (48.2%) and lack of physician interest (43.4%). In addition, 36.7% students believed that CAM practices should be included in their school’s curriculum. Moreover, 39.5% students assumed that CAM knowledge is important to their daily life. Biological sciences and healthcare professional students of Bangladesh showed positive perception on CAM uses. Bangladesh Pharmaceutical Journal 24(2): 159-167, 2021

Background Wedelia chinensis has been reported as a folk medicine for the treatment of different diseases including neurodegenerative disease. Although the plant has been studied well for diverse biological activities, the effect of this plant in neurological disorder is largely unknown. The present study was undertaken to evaluate the cholinesterase inhibitory and antioxidant potential of W. chinensis. Methods The extract and fractions of the plant were evaluated for acetylcholinesterase and butyrylcholinesterase inhibitory activity by modified Ellman method. The antioxidant activity was assessed in several in vitro models/assays such as reducing power, total antioxidant capacity, total phenolic and flavonoid content, scavenging of 2,2′-diphenyl-1-picrylhydrazyl (DPPH) free radical and hydroxyl radical, and inhibition of brain lipid peroxidation. Chromatographic and spectroscopic methods were used to isolate and identify the active compound from the extract. Results Among the fractions, aqueous fraction (AQF) and ethylacetate fraction (EAF) exhibited high inhibition against acetylcholinesterase (IC50: 40.02 ± 0.16 μg/ml and 57.76 ± 0.37 μg/ml) and butyrylcholinesterase (IC50: 31.79 ± 0.18 μg/ml and 48.41 ± 0.05 μg/ml). Similarly, the EAF and AQF had high content of phenolics and flavonoids and possess strong antioxidant activity in several antioxidant assays including DPPH and hydroxyl radical scavenging, reducing power and total antioxidant activity. They effectively inhibited the peroxidation of brain lipid in vitro with IC50 values of 45.20 ± 0.10 μg/ml and 25.53 ± 0.04 μg/ml, respectively. A significant correlation was observed between total flavonoids and antioxidant and cholinesterase inhibitory activity. Activity guided chromatographic separation led to the isolation of a major active compound from the EAF and its structure was elucidated as apigenin by spectral analysis. Conclusions The potential ability of W. chinensis to inhibit the cholinesterase activity and peroxidation of lipids suggest that the plant might be useful for the management of AD.

In the present study, the aerial parts of Achyranthes ferruginea underwent investigation of their in vitro antioxidant and free radical‐scavenging activities in cell‐free conditions, their phytoconstituents using gas chromatography‐mass spectrometry (GC‐MS), and their cytotoxic activity in HeLa cells. A. ferruginea was extracted with 80% methanol and successively fractionated with solvents to yield petroleum ether (PEF), chloroform (CHF), ethyl acetate (EAF), and aqueous (AQF) fractions. GC‐MS analysis revealed that CHF contained ten phytoconstituents, including different forms of octadecanoic acid methyl esters. The total antioxidant and ferric‐reducing antioxidant capacities of the extracts and the standard catechin (CA) were as follows: CA >CHF >PEF >CME (crude methanolic extract) >EAF >AQF, and CA >CHF >EAF >PEF >AQF >CME, respectively. CHF showed the highest DPPH‐free radical‐scavenging activity, with a median inhibitory concentration of 10.5 ± 0.28 µg/ml, which was slightly higher than that of the standard butylated hydroxytoluene (12.0 ± 0.09 µg/ml). In the hydroxyl radical‐scavenging assay, CHF showed identical scavenging activity (9.25 ± 0.73 µg/ml) when compared to CA (10.50 ± 1.06 µg/ml). Moreover, CHF showed strong cytotoxic activity (19.95 ± 1.18 µg/ml) in HeLa cells, which was alike to that of the standards vincristine sulfate and 5‐fluorouracil (15.84 ± 1.64 µg/ml and 12.59 ± 1.75 µg/ml, respectively). The in silico study revealed that identified compounds were significantly linked to the targets of various cancer cells and oxidative enzymes. However, online prediction by SwissADME, admetSAR, and PASS showed that it has drug‐like, nontoxic, and potential pharmacological actions., In this study, we found that the CHF of A. ferruginea has strong antioxidant and cytotoxic properties in different cell lines. GC‐MS quantitative phytochemical screening revealed that CHF contains 10 compounds which has known cytotoxic activity. Therefore, the obtained biological activity of A. ferruginea supports its use as a traditional medicine against different illnesses, and the plant can be considered a potential candidate for treating cancer.

Neurotoxicity is a serious health problem of patients chronically exposed to arsenic. There is no specific treatment of this problem. Oxidative stress has been implicated in the pathological process of neurotoxicity. Polyphenolics have proven antioxidant activity, thereby offering protection against oxidative stress. In this study, we have isolated the polyphenolics from

Aim/Objectives: Oxidative stress (OS) caused by the accumulation of free radicals in the body triggers many life-threatening diseases, including cancer. Plants are the rich source of safe and effective medicinal compounds like antioxidants that can prevent OS by scavenging free radicals. The aim of this study was to explore the chemical compositions of the methanolic extract of Leea aequata L. leaves possessed the highest antioxidant and cytotoxic activities.Methods and Materials: The Leea aequata leaves (LAL) was extracted with 80% methanol and the crude methanolic extract of LAL (CME) was successively fractionated with petroleum ether, chloroform, ethyl acetate and finally with water to get petroleum ether (PEF), chloroform (CHF), ethyl acetate (EAF) and aqueous (AQF) fraction, respectively. The antioxidant activity was evaluated by the in vitro standard spectrophotometric methods. The MTT colorimetric method was used to measure cytotoxic activity. Apoptosis was measured using fluorescein annexin V-FITC/PI staining method. GC-MS was used to investigate phytochemical compositions.Results: Among the fractions, the highest phenolic and flavonoid-rich fraction was EAF, which contained 267.05± 8.53 mg of gallic acid equivalent (GAE) and 152.98±1.96 mg of catechin equivalent (CAE)/gm of dried extract, respectively. The EAF was found to be the highest antioxidant and reducing power activities. Also, EAF had the strongest free radical scavenging activity with IC50 values of 5.11, 36.54 and 38.96 µg/mL for DPPH, hydroxyl and lipid peroxide free radicals, respectively. Moreover, EAF significantly reduced the HeLa cell proliferation and it was due to the induction of apoptosis of HeLa cells. Furthermore, GC-MS data revealed that EAF contained 17 compounds. Methyl esters of long chain fatty acid were the major chemical constituents. Interestingly, hexadecanoic acid, methyl ester; 9-octadecenoic acid (Z)-, methyl ester; 9,12-octadecadienoic acid, methyl ester (Z, Z) and phenol, 2,4-bis(1,1-dimethylethyl) are known to be antioxidant and cytotoxic. Antioxidant and anti-cancer activity were significantly correlated with the total content of phenolics and flavonoids, suggest that the fractions could be the good source of antioxidant and anti-cancer agents.Conclusion: The EAF of Leea aequata has strong polyphenolic content compared to the other fractions. The cytotoxic and antioxidant activity of Leea aequata were due to the presence of different bioactive compounds.

Increased awareness of the multiple roles of RNA molecules has led to the realization that, in addition to their structural and functional roles, RNAs can be drug targets for small molecular therapy. The aim of this study was to identify multivalent amikacin specific RNA aptamers that can be a new target sites for aminoglycoside antibiotics, including amikacin using the systemic evolution of ligands by exponential enrichment (SELEX) method. Amikacin, a member of the aminoglycoside group of antibiotics, binds to specific sites in bacterial 16S ribosomal RNAs (rRNAs) and interferes with protein synthesis, leading to cell death. Here, we used the SELEX method to isolate high affinity RNA fragments (aptamers) that bind to amikacin. After five rounds of SELEX selection, in which a linear N25 DNA template was used for the first selection cycle, the resulting RNA was cloned and sequenced. Among the 38 clones generated, five groups of sequences (groups A through E) containing nine conserved motifs were identified. The sequences of groups A and B were almost identical, indicating that the selected RNA was enriched. Subsequently, the Basic Local Alignment Search Tool program was used to search for the conserved motifs in bacterial 16S rRNA sequences. Strikingly, no sequence homology was observed, suggesting that the conserved sequences (motifs) identified in this study may be novel target sites for amikacin.

Ethnopharmacological relevance: Tabebuia pallida (Lindl.) Miers (T. pallida) is a well-known native Caribbean medicinal plant. The leaves and barks of T. pallida are used as traditional medicine in the form of herbal or medicinal tea to manage cancer, fever, and pain. Moreover, extracts from the leaves of T. pallida showed anticancer activity. However, the chemical profile and mechanism of anticancer activity of T. pallida leaves (TPL), stem bark (TPSB), root bark (TPRB) and flowers (TPF) remain unexplored. Aim of the study: The present study was designed to explore the regulation of apoptosis by T. pallida using Ehrlich Ascites Carcinoma (EAC) cultured cells and an EAC mouse model. LC-ESI-MS/MS was used for compositional analysis of T. pallida extracts. Materials and methods: Dried and powdered TPL, TPSB, TPRB and TPF were extracted with 80% methanol. Using cultured EAC cells and EAC-bearing mice with and without these extracts, anticancer activities were studied by assessing cytotoxicity and tumor cell growth inhibition, changes in life span of mice, and hematological and biochemical parameters. Apoptosis was analyzed by microscopy and expression of selected apoptosis-related genes (Bcl-2, Bcl-xL, NFκ-B, PARP-1, p53, Bax, caspase-3 and -8) using RT-PCR. LC-ESI-MS analysis was performed to identify the major compounds from active extracts. Computer aided analyses was undertaken to sort out the best-fit phytoconstituent of total ten isolated compounds of this plant for antioxidant and anticancer activity. Results: In EAC mice compared with untreated controls, the TPL extract exhibited the highest cancer cell toxicity with significant tumor cell growth inhibition (p < 0.001), reduced ascites by body weight (p < 0.01), increased the life span (p < 0.001), normalized blood parameters (RBC/WBC counts), and increased the levels of superoxide dismutase and catalase. TPL-treated EAC cells showed increased apoptotic characteristics of membrane blebbing, chromatin condensation and nuclear fragmentation, and caspase-3 activation, compared with untreated EAC cells. Moreover, annexin V-FITC and propidium iodide signals were greatly enhanced in response to TPL treatment, indicating apoptosis induction. Pro- and anti-apoptotic signaling after TPL treatment demonstrated up-regulated p53, Bax and PARP-1, and down-regulated NFκ-B, Bcl-2 and Bcl-xL expression, suggesting that TPL shifts the balance of pro- and anti-apoptotic genes towards cell death. LC-ESI-MS data of TPL showed a mixture of glycosides, lapachol, and quercetin antioxidant and its derivatives that were significantly linked to cancer cell targets. The compound, pelargonidin-3-O-glucoside was found to be most effective in computer aided models. Conclusions: In conclusion, the TPL extract of T. pallida possesses significant anticancer activity. The tumor suppressive mechanism is due to apoptosis induced by activation of antioxidant enzymes and caspases and mediated by a change in the balance of pro- and anti-apoptotic genes that promotes cell death.

Background Wedelia chinensis has been reported as a folk medicine for the treatment of different diseases including neurodegenerative disease. Although the plant has been studied well for diverse biological activities, the effect of this plant in neurological disorder is largely unknown. The present study was undertaken to evaluate the cholinesterase inhibitory and antioxidant potential of W. chinensis. Methods The extract and fractions of the plant were evaluated for acetylcholinesterase and butyrylcholinesterase inhibitory activity by modified Ellman method. The antioxidant activity was assessed in several in vitro models/assays such as reducing power, total antioxidant capacity, total phenolic and flavonoid content, scavenging of 2,2’-diphenyl-1-picrylhydrazyl (DPPH) free radical and hydroxyl radical, and inhibition of brain lipid peroxidation. Chromatographic and spectroscopic methods were used to isolate and identify the active compound from the extract. Results Among the extract and functions, aqueous fraction (AQF) and ethylacetate fraction (EAF) exhibited high inhibition against acetylcholinesterase (IC50: 40.02 ± 0.164 µg/ml and 57.76 ± 0.370 µg/ml) and butyrylcholinesterase (IC50: 31.79 ± 0.182 µg/ml and 48.41 ± 0.053 µg/ml). Similarly, the EAF and AQF had high content of phenolics and flavonoids and possess strong antioxidant activity in several antioxidant assays including DPPH and hydroxyl radical scavenging, reducing power and total antioxidant activity. They effectively inhibited the peroxidation of brain lipid in vitro with IC50 values of 45.20 ± 0.995 µg/ml and 25.53 ± 0.042 µg/ml, respectively. A significant correlation was observed between total flavonoids and antioxidant and cholinesterase inhibitory activity. Activity guided chromatographic separation led to the isolation of a major active compound from the EAF and its structure was elucidated as apigenin by spectral analysis. Conclusions The potential ability of W. chinensis to inhibit the cholinesterase activity and peroxidation of lipids suggest that the plant might be useful for the management of AD.

Objectives Plants have been used as traditional medicine (TM) since ancient times and TM remains an effective treatment option in the primary health care system in developing countries, including Bangladesh. There are several reasons to use plants as TM, which are cheaply and easily available and have a cultural heritage of their uses across generations. Leea, a genus of the Vitaceae family, possesses a large number of medicinal plants. In this review, the literature data on the traditional uses and pharmacological activities of Leea species and their phytochemicals are compiled. All the information was collected from the scientific databases. Results Leea species are endemic that have opened a promising research field to identify new leads against different diseases. Leea contains approximately 70 species, which are widely distributed throughout the Northern and Eastern Australia, South and Southeast Asia and parts of Africa. The Leea plants are used traditionally in different ailments such as fever, diarrhea, dysentery, joint pain, rheumatism, diabetes, bone fracture, body ache, wound, sexual disorders, and so on. The majority of the Leea species are the medicinal plants, which have anticancer, cytotoxic, antimicrobial, antidiabetic, hepatoprotective, cardiovascular, and CNS activity. Moreover, phytochemicals such as flavonoids, glycosides, phenols, terpenoids, steroids, volatile oils, alkaloids, proteins, quinine derivatives, tannins, saponins, and many other organic compounds have been reported in the Leea species (Leea indica, Leea macrophylla, Leea asiatica, Leea aequata, Leea rubra and Leea guineensis). The presence of phytochemicals and the in vitro and in vivo biological activities reported of these plants support their use as TM. Though original research articles related to the Leea genus are available, supportive reviews on phytochemicals and pharmacological activities remain scarce. Conclusion Leea species are used as TM in different ailments and have a real interest in their diverse pharmacological properties. Also, Leea species contain a remarkable number of bioactive compounds. This review has provided a comprehensive report on the plants of Leea genus to identify its therapeutic potential and future prospects for betterment research. However, chemical and biological investigations of several species of Leea genus remain unexplored. Therefore, further studies on these species are necessary, especially regarding pharmacological properties, isolation of the compounds and mechanism of action for the development of new drugs., Leea genus, traditional use, medicinal use, bioactive compounds, pharmacological activity

Targeting apoptosis is a promising approach to inhibit the abnormal cell proliferation of cancer progression. Existing anti-apoptotic drugs, many derived from chemical substances, have often failed to combat cancer development and progression. Therefore, identification of apoptosis-inducing anticancer agents from plant-derived sources has become a key aim in cancer research. The present study was designed to explore the regulation of apoptosis by Tabebuia pallida (T. pallida) using an Ehrlich Ascites Carcinoma (EAC) mouse model and compositional analysis by LC-ESI-MS/MS. Dried and powdered T. pallida leaves (TPL), stem bark (TPSB), root bark (TPRB) and flowers (TPF) were extracted with 80% methanol. Using cultured EAC cells and EAC-bearing mice with and without these extracts, anticancer activities were studied by assessing cytotoxicity and tumor cell growth inhibition, changes in life span of mice, and hematological and biochemical parameters. Apoptosis was analyzed by microscopy and expression of selected apoptosis-related genes (Bcl-2, Bcl-xL, NFκ-B, PARP-1, p53, Bax, caspase-3 and -8) using RT-PCR. LC-ESI-MS analysis was performed to identify the major compounds from the most active extracts. In EAC mice compared with untreated controls, the TPL extract exhibited the highest cytotoxicity with significant tumor cell growth inhibition (p< 0.001), reduced ascites by body weight (p< 0.01), increased the life span (pT. pallida possesses significant anticancer activity. The tumor suppressive mechanism is due to apoptosis induced by activation of antioxidant enzymes and caspases and mediated by a change in the balance of pro- and anti-apoptotic genes that promotes cell death.Graphical Abstract

Mistletoes are considered to be the potential medicinal herbs due to their rich traditional uses. Loranthus globosus is a Bangladeshi mango mistletoe that has been reported as folk medicine for various ailments and diseases. In an attempt to explore its effectiveness in Alzheimer’s disease (AD), we investigated the antioxidant and acetylcholinesterase inhibitory activity of L. globosus. We report that the crude methanol extract (CME) of the plant contains a good amount of polyphenolics and possesses antioxidant and cholinesterase inhibitory activity. Fractionation of CME with solvents of varying polarity revealed the highest activity and polyphenolic content in the ethylacetate fraction (EAF). Correlation analysis revealed a significant ( P < 0.05 ) association of polyphenolics with the antioxidant and cholinesterase inhibitory properties. Using column chromatography with diaion resin, the polyphenolics (EAF-PP) were isolated from the EAF that displayed the potent antioxidant and cholinesterase inhibitory activities. Kinetic analysis showed that EAF-PP exhibited a competitive type of inhibition. A total of thirty-six compounds including catechin and its different derivatives were identified in the EAF-PP by LC/MS analysis. Bioactivity-guided separation approach afforded the isolation of the two major active compounds catechin and catechin dimer from the EAF-PP. Hence, EAF-PP represents a potential source of antioxidants and cholinesterase inhibitors, which can be used in the management of AD.

Vanda roxburghii has been used in traditional medicine to treat nervous system disorders including Alzheimer’s disease (AD). We reported earlier a high acetylcholinesterase inhibitory and antioxidant activity in the chloroform fraction of this plant. Therefore, this study was designed to explore the compounds with acetylcholinesterase inhibitory and antioxidant activities from the chloroform fraction of Vanda roxburghii. Phytochemical investigation led to the isolation for the first time of a fatty acid ester: methyl linoleate (1), and three phenolics: syringaldehyde (2), vanillin (3), and dihydroconiferyl dihydro-p-coumarate (4) along with the previously reported compound gigantol (5). Among the isolates, vanillin (3) and dihydroconiferyl dihydro-p-coumarate (4) were found to significantly inhibit the activity of acetylcholinesterase, scavenge the free radicals, exhibit the reducing power and total antioxidant activity, and effectively reduce the peroxidation of lipid. Gigantol (5) and syringaldehyde (2), despite lacking the activity against acetylcholinesterase, exhibited antioxidant activity. Among the compounds, gigantol (5) appeared to be the most potent antioxidant. These findings revealed that V. roxburghii contained compounds with potential acetylcholinesterase inhibitory and antioxidant activity, which support its traditional use in the treatment of AD.

Alzheimer’s disease (AD) is a progressive neurodegenerative disorder of the elderly people. Cholinergic dysfunction and oxidative stress have been found to be related with the development of the disease. Typhonium trilobatum L. Scott has been used traditionally in folk medicine as a central nervous system stimulant. In this study, we have investigated the various extracts of T. trilobatum for acetylcholinesterase and antioxidant activities in vitro. All the tested extracts exhibited inhibition against acetylcholinesterase. Petroleum ether extract exhibited the highest inhibition with an IC50 of 255.26 g/ml. Likewise all the extracts were found to possess antioxidant activity. In reducing power assay, petroleum ether extract showed the highest reducing power with an absorbance of 0.874 at 0.1 mg/ml concentration and in DPPH radical scavenging assay, chloroform extract exhibited the highest scavenging activity with an IC50 of 619.54 µg/ml. Phytochemical analyses of the four extracts revealed that the ethyl acetate extract contained the highest amount of flavonoids and petroleum ether had the highest amount of phenolics. These results suggest that T. trilobatum has both antioxidant and cholinesterase inhibitory activities, which may be useful in reducing the risk of AD. Bangladesh Pharmaceutical Journal 22(1): 92-98, 2019

Background The marine invertebrate starfish was found to contain a novel α-N-acetylgalactosaminidase, α-GalNAcase II, which catalyzes removal of terminal α-N-acetylgalactosamine (α-GalNAc), in addition to a typical α-N-acetylgalactosaminidase, α-GalNAcase I, which catalyzes removal of terminal α-N-acetylgalactosamine (α-GalNAc) and, to a lesser extent, galactose. The interrelationship between α-GalNAcase I and α-GalNAcase II and the molecular basis of their differences in substrate specificity remain unknown. Results Chemical and structural comparisons between α-GalNAcase I and II using immunostaining, N-terminal amino acid sequencing and peptide analysis showed high homology to each other and also to other glycoside hydrolase family (GHF) 27 members. The amino acid sequence of peptides showed conserved residues at the active site as seen in typical α-GalNAcase. Some substitutions of conserved amino acid residues were found in α-GalNAcase II that were located near catalytic site. Among them G171 and A173, in place of C171 and W173, respectively in α-GalNAcase were identified to be responsible for lacking intrinsic α-galactosidase activity of α-GalNAcase II. Chemical modifications supported the presence of serine, aspartate and tryptophan as active site residues. Two tryptophan residues (W16 and W173) were involved in α-galactosidase activity, and one (W16) of them was involved in α-GalNAcase activity. Conclusions The results suggested that α-GalNAcase I and II are closely related with respect to primary and higher order structure and that their structural differences are responsible for difference in substrate specificities.

The objective of this study was to purify and characterize the alpha-N-acetylgalactosaminidase (?-GalNAcase) from hilsha fish, Hilsha ilisha. Digestive organ of hilsha fish was found to contain a large amount of ?-GalNAcase in compared with the other tissues examined. ?-GalNAcase was purified from the crude extract of hilsha fish by ammonium sulphate precipitation, Sephadex G-200 gel filtration, and SP-Sephadex C-50 column chromatography. The purified enzyme gave a single band on sodium dodecylsulphate-polyacrylamide gel electrophoresis and exhibited a molecular mass of 48 kDa. The final preparation of ?-GalNAcase showed 3.02% ?-galactosidase activity. The enzyme had an optimum pH of 4.0 and was found to be quiet heat stable at 37°C. Inhibition studies with metal ions demonstrated that the enzyme was highly inhibited by silver and mercury ions. Both N-acetylgalactosamine and galactose affect the enzyme activity. Kinetic studies with the enzyme showed that the KM value for p-nitrophenyl-?-N-acetylgalactosaminide substrate was 3.31 mM and the Vmax value was 35.04 unit/mg.

Two compounds (7-O-methylmearnsitrin (7-OM) and roseoside A (RA) were identified and characterized from the leaves of Leea aequata (L. aequata) L. The cytotoxicity of 7-OM and RA on HeLa cells was performed using MTT. The 7-OM and RA showed significant inhibition of HeLa cell proliferation with an IC50 of 22 and 20 µg/mL, respectively when compared with the standard vincristin sulphate (VS) (IC50 of 15 µg/mL). Moreover, the 7-OM and RA significantly inhibit other cancer cells (HEK-293, H228, and H3122) when compared with the VS and the cytotoxic activity of the compounds might show through the induction of apoptosis. Strikingly, annexin-V and PI signals could barely be detected in control cells, while strong fluorescence densities were observed in response to treatment indicating that these compounds have capacity to induce HeLa cell apoptosis. Our results suggest that the anticancer activity of 7-OM and RA was due to the induction of apoptosis.

The present study was designed to investigate the effects of combination of Nigella sativa oil and pioglitazone on long-term alloxan-induced diabetic rats. In short-term (two weeks) alloxan-induced diabetic rats, N. sativa oil (NSO) reduced significant amount of glucose in blood, TC, TG and LDL-C and increased significant amount of HDL-C compared to diabetic rats. However, pathological changes of pancreas’s Islets of Langerhans were observed after long-term (four weeks) induction of alloxan in rats. Administration of NSO recovered Langerhans cells from shrinkage whereas pioglitazone displayed slight recovery. But the combination therapy showed complete recovery of Langerhans cells as compared with diabetic rats. Combination of drugs significantly reduced the TC, TG and LDL-C level as well as increased significant amount of HDL-C level to the normal level. Combination also increased DPPH free radical scavenging activity compared with diabetic rats. The results suggest that treatment with combination therapy was more effective than mono-therapy for preventing diabetes as N. sativa oil potentiates the effects of pioglitazone on long term alloxan-induced diabetic rats. DOI: http://dx.doi.org/10.3329/bpj.v16i2.22296 Bangladesh Pharmaceutical Journal 16 (2): 143-151, 2013

Background Alzheimer's disease (AD) is a progressive neurodegenerative disorder clinically characterized by loss of memory and cognition. The effective therapeutic options for AD are limited and thus there is a demand for new drugs. Aegle marmelos (Linn.) (A. marmelos) leaves have been used in traditional medicine to promote intellect and enhance memory. In this study, we evaluated A. marmelos for its acetylcholinesterase (AChE) inhibitory activity and antioxidant property in vitro in the treatment of AD. Methods A crude methanol extract and four fractions (petroleum ether, chloroform, ethyl acetate and aqueous) were prepared from the leaves of A. marmelos. The preparations were assessed for AChE inhibitory activity by the Ellman method, and their antioxidant properties were assessed by several assays: reducing power, scavenging of 1,1-diphenyl-2-picrylhydrazyl free radical and hydroxyl radical, and inhibition of lipid peroxidation. Qualitative and quantitative analyses of endogenous substances in A. marmelos were performed by the standard phytochemical methods. Results Among the different extracts tested, the ethyl acetate fraction exhibited the highest inhibition of AChE activity. In the same way, ethyl acetate fraction showed the highest reducing activity and radical scavenging ability towards the 1,1-diphenyl-2-picrylhydrazyl (half maximal inhibitory concentration = 3.84 μg/mL) and hydroxyl free radicals (half maximal inhibitory concentration = 5.68 μg/mL). The antiradical activity of the ethyl acetate fraction appeared to be similar to that of the reference standard butylated hydroxytoluene and catechin used in this study. In addition, the ethyl acetate fraction displayed higher inhibition of brain lipid peroxidation. Phytochemical screening of different extractives of A. marmelos showed the presence of phenols and flavonoids, alkaloid, saponin, glycoside, tannin and steroids. Quantitative analysis revealed higher contents of phenolics (58.79-mg gallic acid equivalent/g dried extract) and flavonoids (375.73-mg gallic acid equivalent/g dried extract) in the ethyl acetate fraction. Conclusion The results suggest that the ethyl acetate fraction of A. marmelos is a significant source of polyphenolic compounds with potential AChE inhibitory property and antioxidant activity and, thus, may be useful in the treatment of AD.

The aim of this study was to investigate the inhibitory effect of Nigella sativa seed extract (abbreviated as NSS E) on adrenaline-induced dyslipidemia and left ventricular hypertrophy (LVH) in rats. Intraperitoneal injection of adrenaline for two weeks induced dyslipidemia whereas injection of adrenaline for four weeks induced both dyslipidemia and LVH significantly, compared with normal rats. Injection of NSS E with different doses (0.5, 1 and 1.5 mg/kg body weight, BW) on adrenaline-induced dyslipidemic rats (AIDRs) for two weeks significantly reduced TC, TG and LDL-C and increased HDL-C compared with AIDRs and the most effective dose was 1.5 mg/kg BW. Treatment with NSS E (1.5 mg/kg BW) on AIDRs for eight weeks, significant anti-dyslipidemic effect was observed. Moreover, NSS E significantly increased free radical scavenging activity and attenuated the LVH and cardiomyocyte size compared with AIDRs. The results suggested that the anti-dyslipidemic, antioxidative and inhibitory effects of NS SE on LVH were closely resembled to that of atorvastatin, a most effective lipid lowering agent. Therefore, NS SE might be used as a therapeutic alternative or as a combination with drug in the treatment of dyslipidemia and LVH. Keywords: Adrenaline; Dyslipidemia; LVH; NSS E; Atorvastatin. © 2013 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved. doi: http://dx.doi.org/10.3329/jsr.v5i2.12203 J. Sci. Res. 5 (2), 325-334 (2013) .

Diabetes associated dyslipidemia is one of the major causes of disability in western as well as in developing countries. The present study was designed to investigate the effect of ethanolic extract of Hibiscus rosa sinensis (EHBS) leaves on alloxan-induced diabetes with dyslipidemia in rats. Treatment of alloxan-induced diabetes with most effective observed dose (2.0 mg/kg body weight) of EHBS for 1 week significantly reduced glucose level, TC, TG and LDL-C, with the increase of HDL-C and weight of kidney, pancreas and liver when compared with diabetic rats. The observation was also made for consecutive 4 weeks to confirm the results obtained in one week model. Like one week, we got similar results when the treatment of alloxan-induced rats was done with the EHBS for 4 weeks. The results indicated that the EHBS leaves, in comparison with metformin, had profound hypoglycemic and hypolipidemic activities. DOI: http://dx.doi.org/10.3329/bpj.v16i1.14487 Bangladesh Pharmaceutical Journal 16(1): 27-31, 2013

Hyperlipidemia is one of the major causes of disability in western as well as in developing countries. The present study was designed to investigate the effect of the ethanolic leaf extract of a Bangladeshi medicinal plant Acacia nilotica (AN) on adrenaline-induced hyperlipidemia and cardiac remodeling in rats. The plant extract and commercial lipid lowering drug atorvastatine were administered in adrenaline-induced hyperlipidemic rats (AIHRs) through intraperitoneal route for one week at a dose of 30 mg and 0.04 mg per 150 gm body weight of rat, respectively. The AN extract showed a significant (P

The present study was designed to investigate the effects of combination drugs (metformin and atorvastatin) on long-term alloxan-induced diabetes with CVD in rats. In short-term alloxan-induced diabetic rats, metformin reduced significant amount of glucose in blood, but it had no significant effect on lipid profile. Atorvastatin significantly reduced TC, TG and LDL-C, whereas it increased significant amount of HDL-C. However, pathological changes of heart were not observed after short-term induction of alloxan in rats. In long-term induction of diabetes by alloxan, LV hypertrophy was observed and cardimyocyte size in rats was increased. Atorvastatin alone and in combination with metformin significantly reduced the LV hypertrophy, cardiomyocyte size, TC, TG and LDL-C level. They increased significant amount of HDL-C level and showed significant DPPH free radical scavenging activity. Present findings may suggest that treatment with combination therapy is more effective than mono-therapy for preventing diabetes with CVD in rats.© 2012 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.doi: http://dx.doi.org/10.3329/jsr.v4i3.9974 J. Sci. Res. 4 (3), 709-720 (2012)

not available DOI: http://dx.doi.org/10.3329/dujps.v13i2.21905 Dhaka Univ. J. Pharm. Sci. 13(2): 225-227, 2014 (December)

To induce neural differentiation of P19 cells, two different treatments, RA (retinoic acid) and cell aggregation, are required. However, there has been no report that RA treatment alone or cell aggregation alone could control alternative splicing regulation in P19 cells. Therefore, we focused on alternative splicing effects by neural induction (RA treatment and/or cell aggregation) in P19 cells. We analysed the splicing patterns of several genes, including 5-HT3R-A (5-hydroxytryptamine receptor), Actn1 (actinin alpha1), CUGBP2 (CUG-binding protein) and PTB (polypyrimidine track-binding protein), which showed different responses during the early neural induction of P19 cells. We show here that RA treatment alone changes the alternative splice mechanism of 5-HT3R-A. Cell aggregation alone controls alternative splicing regulation of Actn1. Both treatments (RA and cell aggregation) compensate and regulate the alternative splicing mechanism of CUGBP2. However, PTB is independent of RA and cell aggregation. Taken together, our results suggest that RA treatment and cell aggregation independently regulate the alternative splicing mechanism in the early stage of P19 cells during neural differentiation.

Background Antioxidants play an important role to protect damage caused by oxidative stress (OS). Plants having phenolic contents are reported to possess antioxidant properties. The present study was designed to investigate the antioxidant properties and phenolic contents (total phenols, flavonoids, flavonols and proanthrocyanidins) of methanolic extracts from Morus alba (locally named as Tut and commonly known as white mulberry) stem barks (TSB), root bark (TRB), leaves (TL) and fruits (TF) to make a statistical correlation between phenolic contents and antioxidant potential. Methods The antioxidant activities and phenolic contents of methanolic extractives were evaluated by in vitro standard method using spectrophotometer. The antioxidant activities were determined by total antioxidant capacity, DPPH (1,1-diphenyl-2-picrylhydrazine) radical scavenging assay, hydroxyl radical scavenging assay, ferrous reducing antioxidant capacity and lipid peroxidation inhibition assay methods. Results Among the extracts, TSB showed the highest antioxidant activity followed by TRB, TF and TL. Based on DPPH and hydroxyl radical scavenging activity, the TSB extract was the most effective one with IC50 37.75 and 58.90 μg/mL, followed by TRB, TF and TL with IC50 40.20 and 102.03; 175.01 and 114.63 and 220.23 and 234.63 μg/mL, respectively. The TSB extract had the most potent inhibitory activity against lipid peroxidation with IC50 145.31 μg/mL. In addition, the reducing capacity on ferrous ion was in the following order: TSB > TRB > TL > TF. The content of phenolics, flavonoids, flavonols and proanthocyanidins of TSB was found to be higher than other extractives. Conclusion The results indicate high correlation and regression (p-value ) between phenolic contents and antioxidant potentials of the extracts, hence the Tut plant could serve as effective free radical inhibitor or scavenger which may be a good candidate for pharmaceutical plant-based products. However, further exploration is necessary for effective use in both modern and traditional system of medicines.

Background CELF/Bruno-like proteins play multiple roles, including the regulation of alternative splicing and translation. These RNA-binding proteins contain two RNA recognition motif (RRM) domains at the N-terminus and another RRM at the C-terminus. CUGBP2 is a member of this family of proteins that possesses several alternatively spliced exons. Results The present study investigated the expression of exon 14, which is an alternatively spliced exon and encodes the first half of the third RRM of CUGBP2. The ratio of exon 14 skipping product (R3δ) to its inclusion was reduced in neuronal cells induced from P19 cells and in the brain. Although full length CUGBP2 and the CUGBP2 R3δ isoforms showed a similar effect on the inclusion of the smooth muscle (SM) exon of the ACTN1 gene, these isoforms showed an opposite effect on the skipping of exon 11 in the insulin receptor gene. In addition, examination of structural changes in these isoforms by molecular dynamics simulation and NMR spectrometry suggested that the third RRM of R3δ isoform was flexible and did not form an RRM structure. Conclusion Our results suggest that CUGBP2 regulates the splicing of ACTN1 and insulin receptor by different mechanisms. Alternative splicing of CUGBP2 exon 14 contributes to the regulation of the splicing of the insulin receptor. The present findings specifically show how alternative splicing events that result in three-dimensional structural changes in CUGBP2 can lead to changes in its biological activity.

Background The use of plants and their derived substances increases day by day for the discovery of therapeutic agents owing to their versatile applications. Current research is directed towards finding naturally-occurring antioxidants having anticancer properties from plant origin since oxidants play a crucial role in developing various human diseases. The present study was designed to investigate the antioxidant and anticancer properties of Sygygium fruticosum (Roxb.) (abbreviated as SF). Methods The dried coarse powder of seeds of SF was exhaustively extracted with methanol and the resulting crude methanolic extract (CME) was successively fractionated with petroleum ether, chloroform and ethyl acetate to get petroleum ether (PEF), chloroform (CHF), ethyl acetate (EAF) and lastly aqueous (AQF) fraction. The antioxidant activities were determined by several assays: total antioxidant capacity assay, DPPH free radical scavenging assay, hydroxyl radical scavenging assay, ferrous reducing antioxidant capacity and lipid peroxidation inhibition assay. The in vivo anticancer activity of SF was determined on Ehrlich’s Ascite cell (EAC) induced Swiss albino mice. Results All the extractives showed strong antioxidant activities related to the standard. The total antioxidant capacity (TAC) of the fractions was in the following order: EAF>AQF>CME>PEF>CHF. The TAC of EAF at 320 μg/mL was 2.60±0.005 which was significantly higher (p < 0.01) than that of standard catechin (1.37 ± 0.005). The ferrous reducing antioxidant capacity of the extracts was in the following order: EAF>AQF>CME>AA>CHF>PEF. In DPPH free radical scavenging assay, the IC50 value of EAF was 4.85 μg/mL, whereas that of BHT was 9.85 μg/mL. In hydroxyl radical scavenging assay and lipid peroxidation inhibition assay, the EAF showed the most potent inhibitory activity with IC50 of 43.3 and 68.11 μg/mL, respectively. The lipid peroxidation inhibition assay was positively correlated (p < 0 .001) with both DPPH free radical scavenging and hydroxyl radical scavenging assay. The total phenolic contents of SF were also positively correlated (p < 0 .001) with DPPH free radical scavenging, hydroxyl radical scavenging and lipid peroxidation inhibition assay. Based on antioxidant activity, EAF was selected for cytotoxic assay and it was found that EAF inhibited 67.36% (p < 0.01) cell growth at a dose of 50 mg/kg (ip) on day six of EAC cell incubation. Conclusions Our results suggest that EAF of seeds of SF possess significant antioxidant and moderate anticancer properties. Seeds of SF may therefore be a good source for natural antioxidants and a possible pharmaceutical supplement.

Background Research on natural products has gained a wide popularity due to the potential of discovering active compounds. The antioxidant properties contained in plants have been proposed as one of the mechanisms for the observed beneficial effect. Therefore, the present study investigated the antioxidant activity and total phenolic contents of various solvent extracts of Albizia procera leaves. Methods Antioxidant activity of the methanol extract and its derived fractions petroleum ether (APP), carbon tetrachloride (APC), dichloromethane (APD), ethyl acetate (APE), and residual aqueous fraction (APA) of the leaves of Albizia procera was performed by in vitro chemical analyses. Total phenolic content of the APM and other five fractions were also determined. APM and its derived fractions were also subjected to preliminary phytochemical screening test for various constituents. R esults Phytochemical screening revealed the presence of saponins, steroids, tannins, glycosides and flavonoids in the extracts. Amongst the extracts, APE showed the highest total phenolic content (449.18 ± 18.41mg of gallic acid equivalent/g of extract). In DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging test, the IC50 value of APM, APP, APC, APD, APE and APA was 43.43, 63.60, 166.18, 41.15, 11.79, and 63.06 μg/mL, respectively. Therefore, among the APM and its derived fractions, APE showed the highest antioxidant activity which is comparable to that of standard ascorbic acid (AA) (IC50 10.12 μg/mL). The total antioxidant capacity was found to be varied in different fractions. The reducing activity on ferrous ion was ranked as APE > APD > APM > APA > APC. C onclusion The above evidences suggest that APE of A. procera leaf is a potential source of natural antioxidant and can be used to prevent diseases associated with free radicals.