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Vitex peduncularis (Verbenaceae), a perennial tree, is locally utilized for possessing multifaceted pharmacological properties including analgesic, antimalarial, anti-angina, antidiabetic, antioxidant, anti-inflammatory and hepatoprotective. Hence, this study aims to evaluate their antioxidant, thrombolytic, cytotoxic and antibacterial activities from the methanolic crude extract and its various solvent fractions. Data from antioxidant and thrombolytic assay displayed that Kupchan partitioned chloroform soluble fraction revealed the maximum phenolic content (73.39 mg of GAE/g of extract), DPPH free radical scavenging activity (26.69 μg/ml) and thrombolytic activity (37.35%). In brine shrimp lethality evaluation, the LC50 values indicate that the most cytotoxic compound was found to be from ethyl acetate soluble fraction (LC50 6.73 μg/ml). Finally, antibacterial activity of different fractions showed that both chloroform and methanolic fraction possessed mild activity against the tested bacteria. The potential biological effects of the crude fractions have been demonstrated demanding future studies of the isolated compounds to assess these activities. Bangladesh J. Sci. Ind. Res. 57(4), 239-246, 2022

Cervico-Dorsal junction is a transitional zone of spinal column. 360-degree fixation of cervico-dorsal region in a single posterior approach is a difficult and challenging procedure accounting the spinal cord decompression, posterior vertebral body replacement and then posterior instrumentation. Here we have described a patient who presented with features of spastic paraparesis and lower motor palsy of right upper limb due to anexpansile bone mass on Rt side of cervico-dorsal region. He underwent neuronal decompression and 360-stabilisation in a single posterior approach. We review clinical and radiographic features of the patient; the procedureunderwent as well as current other treatment options with reference to the relevant literatures. Bang. J Neurosurgery 2022; 11(2): 122-127

Crinum asiaticum L. (Amaryllidaceae) is a perennial bulbous herb, locally utilized for possessing multifaceted pharmacological properties including anticancer, immune-stimulating, analgesic, antiviral, antimalarial, antibacterial, and antifungal, in addition to their popularity as an aesthetic plant. Separation of MeOH extract of C. asiaticum leaves yielded three known compounds as cycloneolitsol (1), hippeastrine (2) and β-sitosterol (3). Among these, compounds 1 and 2 were subjected to the cytotoxic assay and found that 1 decreased cell viability to 45% and 8% against HCT116 cells; 15% and 9% against DU145 cells; 63% and 23% against Huh7 cells at 100 µM and 200 µM concentrations, respectively. Similarly, 2 decreased cell viability to 10% and 7% against HCT116 cells; 25% and 15% against DU145 cells; 26% and 18% against Huh7 cells at 100 µM and 200 µM concentrations, respectively. When tested for TRAIL-resistance abrogating activity, 1 (100 µM) along with TRAIL (100 ng/mL) showed moderate activity in AGS cells producing 25% more inhibition than the agent alone. Whereas (20 and 30 µM) in combination with TRAIL (100 ng/mL) exhibited strong activity in abrogating TRAIL-resistance and caused 34 and 36% more inhibition in AGS cells, respectively. The in-silico studies of compounds 1 and 2 revealed high docking hits in the TRAIL and other cancer-associated proteins which indicates a good correlation with the cell-based assay. It is still recommended to conduct further investigations to understand their exact molecular mechanism.

Two new compounds, thannilignan 9-O-β-glucoside (1) and 2-(β-glucopyranosyl)-3-isoxazolin-5-one derivative (2), and seven known compounds were isolated from the methanol extract of Terminalia bellirica leaves, collected in Bangladesh. The structures of the compounds were elucidated using spectroscopic analysis. Among these isolated compounds, corilagin (3) was cytotoxic against human gastric adenocarcinoma cell line AGS at an IC

Mucuna pruriens is a tropical legume native to Africa, India and Bangladesh and is widely cultivated in tropical countries. In this study, a crude methanolic extract of the leaves of M. pruriens was investigated for its chemical constituents and to explore the phenolic and flavonoid content, antioxidant, cytotoxic and antimicrobial activities using established protocols. From the ethyl acetate soluble fraction of the crude methanol extract, three known compounds namely ferulic acid (1), 2-(5-methoxy-1-benzofuran-3-yl)-N-ethylethanamine (2) and stizolamine (3) were isolated and their structures were elucidated by the analysis of NMR spectral data. The crude extract was found to possess phenolic content of 216.16 μg/g whereas the concentration of flavonoid was found to 214.8 μg/g expressed in quercetin standard. Free radicals generated through DPPH were neutralized by crude methanolic extract and the IC50 value was obtained as 19.63 μg/ml. Regression analysis during brine shrimp lethality test enumerated LC50 value of crude methanolic extract at 10.72 μg/ml and was significant compared to the positive standard. The crude methanolic extract of leaf of M. pruriens did not show any significant antimicrobial activity against the organisms used in our test. Dhaka Univ. J. Pharm. Sci. 20(1): 103-109, 2021 (June)

Palm oil is an edible vegetable oil, extracted from the fruit of the Elaeis guineensis which is used for frying foods in most of the restaurants and confectionaries as well as for cosmetic preparations in industries. As the quality of palm oil in Bangladesh is deteriorating day by day, ten brands (S-1 to S-10) of commercially available palm oils were collected from different local markets, their physicochemical properties were tested and compared with the standard parameters stated by Bangladesh Standards and Testing Institution (BSTI). Results revealed that the acid value, free fatty acid value and relative density of all the palm oils (S-1 to S-10) were within the range of BSTI standard. However, the saponification value, peroxide value, iodine value, insoluble impurities and moisture content were much higher than the ranges of BSTI standard in all the samples. Moreover, lead content was higher than the standard value (>0.1 ppm) in brands S-1, S-4 and S-10. In addition, Copper and Iron contents were higher than the BSTI standards (0.1 and 1.5 ppm) in all the tested samples, whereas Cadmium content was below than the standard level (1.0 ppm). Bangladesh J. Sci. Ind. Res.55(4), 301-310, 2020

Methanolic extract of Curcuma amada leaves was investigated for isolation of secondary metabolites by successive chromatographic separation (VLC, column chromatography and TLC) which yielded several purified compounds. Among them the structures of β-sitosterol and stigmasterol were determined by analysis of high resolution 1H NMR spectroscopic data and co-TLC with authentic samples. The crude methanolic extract of C. amada leaves and its different fractionates i.e. petroleum ether (PESF), chloroform (CSF) and aqueous (AQSF) soluble fractions were evaluated for antibacterial, antioxidant, cytotoxic and thrombolytic activities. In antibacterial screening, the CSF exhibited the highest inhibition against bacterial growth having zone of inhibition 12 mm compared to the standard kanamycin where the zone of inhibition was observed at 18 mm against gram negative Vibrio mimicus. Significant free radical scavenging activity was also exhibited by CSF with the IC50 value of 103.09 μg/ml as compared to tert-butyl-1-hydroxytoluene (BHT) having IC50 31.88 μg/ml. In cytotoxicity study, the crude extract showed significant lethality towards brine shrimp having with the LC50 value of 6.540 μg/ml as compared to the standard vincristine sulfate (0.451μg/ml). In the study for thrombolytic property, different extracts of C. amada exhibited clot lysis ranging from 17.24 to 43.55% as compared to standard streptokinase (93.75 %). Dhaka Univ. J. Pharm. Sci. 19(1): 9-13, 2020 (June)

The present study was carried out to investigate phytochemical, antioxidant; antimicrobial, thrombolytic activity and estimate total phenolic, total flavonoid content of Pandanus odoratissimus (p.odoratissimus) leaves of methanol extract. In thrombolytic activity, aqueous soluble fraction (AQSF) exhibited highest percentage (46.58 %) of potential to lyse blood clot compared to standard drug streptokinase (69.52 %). In antimicrobial assay, dichloromethane soluble fraction (DCMSF) explored the highest diameter of clear zone of inhibition against both gram positive (19.60 ± 0.12 mm) and gram negative (20.00 ± 0.20 mm) bacteria compared to standard antibiotic, Kanamycin (50.00 ± 0.19). Levels of antioxidant were determined by DPPH assay followed by calculated IC50 values of different Kupchan extracts. The methyl soluble fraction (MSF) showed the lowest level of IC50 value (36.70 ± 0.32 µg/mL) in comparison to ascorbic acid (12.48 ± 0.09 µg/mL) while MSF disclosed the maximum level (62.19 ± 0.26 mg of GAE/g of extract) of total phenolic content in the extracts of P. odoratissimus. This study was conducted to validate the P. odoratissimus leaves used as a folk medicine such as, antioxidant, thrombolytic, and antimicrobial potential.

Adenoid cystic carcinoma (ACC) is a rare malignant tumor that can manifests as proptosis in adult population. They account for 1.6% of all orbital tumors. Despite their rarity, they are the second most frequent epithelial neoplasms occurring in the lacrimal gland after pleomorphic adenomas. This kind of tumors are commonly occur in the salivary glands but can metastasize to lung, breast ,brain and sinuses in hematogenous route.We describe a patient who presented with protrusion of right eyeball, developing over 8 years with history of intermittent watery discharge for 4 years. His magnetic resonance imaging showed a retrobulbarextraconal soft tissue lesion around the lacrimal fossa with invasion and erosion of the adjacent bone. The patient underwent right sided orbito-pterional craniotomy and gross total removal of tumor. Pathologic analysis showed neoplastic cells in a predominantly cribriform pattern with features of perineural invasion and diagnosed as a case adenoid cystic carcinoma of the lacrimal gland. We review the incidence, clinical features, radiographic and histopathologic features of these rare, aggressive malignancies along with current treatment options with reference to the relevant literatures. Bang. J Neurosurgery 2019; 9(1): 49-53

Structural damage inflicted to a wide variety of bioorganic compounds (DNA, protein, carbohydrates, and lipid) may occur as a consequence of oxidative damage which is naturally attributed to our daily lifestyle. A number of mechanisms are exploited to neutralize the reactive oxygen species. Medicinal plant can play a pivotal role of detoxifying the generated ROS. Leeamacrophylla (Leeaceae), a wild medicinal plant, has been taken into consideration of having antioxidant and cytotoxic properties. In this study, in vitro DPPH free radical scavenging activity, total phenolic content and total flavonoid content of methanol extract from the leaves of L. macrophylla were determined with using UV spectrophotometric method. Antioxidant activity of the crude extract was expressed as percentage of DPPH free radical inhibition and IC50 value (μg/ml). The IC50 value of L. macrophylla was found to be 152.40μg/ml. Compared to standard ascorbic acid (4.36 μg/ml), L. macrophylla leaf extract has moderate antioxidant property. The total phenolic content was 65.75 mg/g of dry weight of extract, expressed as gallic acid equivalents. The total flavonoid concentration was 59.8 mg/g, expressed as quercetin equivalents. In the brine shrimp lethality test, LC50value of crude methanolic extract obtained from the best-fit line slope was 3.06μg/ml which was significant comparing with control (vincristine sulphate). Above results suggested that the L. macrophylla can be regarded as a promising candidate for natural plant sources of antioxidants with high value.

This report describes the development of a target-protein-oriented natural-products-isolation (TPO-NAPI) method for Hedgehog inhibitors and the direct GLI1 inhibitor, 5′-O-methyl-3-hydroxyflemingin A (3), which inhibited hedgehog (Hh) signal transduction and diminished characteristics of cancer stem cells. Eight natural products (including three newly described products) that directly bind to GLI1 were rapidly obtained via the TPO-NAPI method developed using GLI1 protein-immobilized beads. 5′-O-Methyl-3-hydroxyflemingin A (3) inhibited Hh signaling (IC50 7.3 μM), leading to decreasing production of the Hh target proteins BCL2, PTCH1, and BMI1. 5′-O-Methyl-3-hydroxyflemingin A (3) was cytotoxic to Hh-related cancer cells. CD experiments revealed that 5′-O-methyl-3-hydroxyflemingin A (3) directly bound GLI1 (Kd = 7.7 μM). Moreover, 5′-O-methyl-3-hydroxyflemingin A (3) diminished cancer stem cell characters of Huh7 such as sphere formation and production of the cancer stem cell marker EpCAM. These results su...

Fractionation of the leaf extract from Murraya exotica led to the successful isolation of 12 compounds (1-12) with TRAIL-resistance-overcoming activity. Xanthinosin (1), 11α, 13-dihydroxanthinin (2), 11β, 13-dihydroxanthinosin (3), 4α, 11α, 13-trihydroxanthuminol (4), desacetylxanthanol (5), and lasidiol p-methoxybenzoate (6) were sesquiterpenes isolated from this plant for the first time, and 3 was isolated from natural sources for the first time. Among them, compounds 1 and 5 showed strong TRAIL-resistance-overcoming activity, but their mechanisms have already been revealed. Furthermore, dihydroxanthinin (2), 1, 5-dicaffeoylquinic acid (7), and (-) loliolide (8), which belong to different phytochemical groups, were investigated for their effects on increasing apoptosis induction to overcome TRAIL resistance using Western blot analysis. The results demonstrated that 2, 7, and 8 promoted TRAIL-induced apoptosis by increasing the expression of several proapoptotic markers, including cleaved caspases −3 and −8, and suppressing anti-apoptotic protein Bcl-2.

Natural products isolation using protein based methods is an attractive for obtaining bioactive compounds. To discover neural stem cell (NSC) differentiation activators, we isolated eight inhibitors of Hes1 dimer formation from Psidium guajava using the Hes1-Hes1 interaction fluorescent plate assay and one inhibitor from Terminalia chebula using the Hes1-immobilized beads method. Of the isolated compounds, gallic acid (8) and 4-O-(4”-O-galloyl-α-L-rhamnopyranosyl)ellagic acid (11) showed potent Hes1 dimer formation inhibitory activity, with IC50 values of 10.3 and 2.53 μM, respectively. Compound 11 accelerated the differentiation activity of C17.2 NSC cells dose dependently, increasing the number of neurons with a 125% increase (5 μM) compared to the control.

Tumor necrosis factor related apoptosis-inducing ligand (TRAIL) has emerged as a promising anticancer agent as it selectively kills cancer cells. However, TRAIL resistance limits its use as a therapeutic agent. An understanding the mechanisms responsible for TRAIL resistance and strategies to overcome it are important for its effective use as an anticancer agent. During our studies to screen natural products from medicinal plants, we identified a number of compounds with synergistic effects on TRAIL-induced apoptosis in tumor cells. This review describes our recent studies on the isolation of bioactive compounds with TRAIL-resistance overcoming activity.

Tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL) has emerged as a promising anticancer agent because of its ability to selectively kill tumor cells. But TRAIL-resistance is a major problem of its therapy. A search for compounds for abrogating TRAIL-resistance has, thus, become an important strategy for anticancer drug discovery. In search of bioactive natural products for overcoming TRAIL-resistance, we previously reported some compounds with TRAIL-resistance overcoming activity. Bioassay guided fractionation of Entada scandens led to the isolation of four compounds (1-4). Of the isolates, compounds 1 and 3 showed moderate TRAIL-resistance overcoming activity in TRAIL-resistant human gastric adenocarcinoma (AGS) cells.

Four alkaloids, voacangine (1), isovoacangine (2), coronaridine (3), and coronaridine hydroxyindolenine (4), were isolated from the MeOH extract of Tabernaemontana divaricata aerial parts by activity-guided fractionation for Wnt signal inhibitory activity. Compounds 1-4 exhibited TCF/β-catenin inhibitory activities with IC50 values of 11.5, 6.0, 5.8, and 7.3 μM, respectively. Of these, coronaridine (3) decreased β-catenin levels in SW480 colon cancer cells, while this decrease in β-catenin was not suppressed by a co-treatment with 3 and MG132, a proteasome inhibitor. These results suggested that the decrease observed in β-catenin levels by coronaridine (3) did not depend on a proteasomal degradation process. On the other hand, the treatment of SW480 cells with coronaridine (3) caused a decrease in β-catenin mRNA levels. Thus, coronaridine (3) may inhibit the Wnt signaling pathway by decreasing the mRNA expression of β-catenin.

The ability of TRAIL to selectively induce apoptosis in cancer cells while sparing normal cells makes it an attractive target for the development of new cancer therapy. In search of bioactive natural products for overcoming TRAIL-resistance from natural resources, we previously reported a number of active compounds. In our screening program on natural resources targeting overcoming TRAIL-resistance, activity-guided fractionations of the extract of Xanthium strumarium led to the isolation of five sesquiterpene compounds (1-5). 11α,13-dihydroxanthinin (2) and 11α,13-dihydroxanthuminol (3) were first isolated from natural resources and xanthinosin (1), desacetylxanthanol (4), and lasidiol p-methoxybenzoate (5) were known compounds. All compounds (1-5) showed potent TRAIL-resistance overcoming activity at 8, 20, 20, 16, and 16 μM, respectively, in TRAIL-resistant AGS cells. Compounds 1 and 5 enhanced the levels of apoptosis inducing proteins DR4, DR5, p53, CHOP, Bax, cleaved caspase-3, cleaved caspase-8, and cleaved caspase-9 and also decreased the levels of cell survival protein Bcl-2 in TRAIL-resistant AGS cells in a dose-dependent manner. Compound 1 also enhanced the levels of DR4 and DR5 proteins in a time-dependent manner. Thus, compounds 1 and 5 were found to induce both extrinsic and intrinsic apoptotic cell death. Compound 1 also exhibit TRAIL-resistance overcoming activity in DLD1, DU145, HeLa, and MCF7 cells but did not decrease viability in non-cancer HEK293 cells up to 8 μM.

The Wnt signal pathway modulates numerous biological processes, and its aberrant activation is related to various diseases. Therefore, inhibition of the Wnt signal may provide an effective (or efficient) strategy for these diseases. Cell-based luciferase assay targeting the Wnt signal (TOP assay) revealed that Hibiscus ficulneus extract inhibited the Wnt signal. The activity-guided isolation of the MeOH extract of H. ficulneus stems yielded four known (1-4) lignans along with myriceric acid (5). Compounds 1-4 potently inhibited the Wnt signal with TOPflash IC50 values of 1.0, 4.5, 6.3, and 1.9 μM, respectively. Compound 1 exhibited cytotoxicity against both Wnt-dependent (HCT116) and Wnt-independent (RKO) cells. Western blot analysis showed that 1 decreased the expression of full, cytosolic and nuclear β-catenin along with c-myc in STF/293 cells. Our results suggested that 1 may have inhibited the Wnt signal by decreasing β-catenin levels.

The inhibition of the hedgehog (Hh) signaling pathway has emerged as an attractive anti-cancer strategy. As part of our continuing search for natural inhibitors of the Hh/GLI1 signaling pathway, we isolated three alkaloids (1-3) from Crinum asiaticum. Compounds 1 and 3 showed potent Hh/GLI1-mediated transcriptional inhibitory activity and exhibited cytotoxicity against human pancreatic (PANC1) and prostate (DU145) cancer cells. Our data revealed that compounds 1 and 3 clearly inhibited the Hh signaling pathway by down-regulating the expression of GLI-related proteins (PTCH and BCL2) in DU145 cells.

Scopadulciol (1), a scopadulan-type diterpenoid, was isolated from Scoparia dulcis along with three other compounds (2-4) by an activity-guided approach using the TCF reporter (TOP) luciferase-based assay system. A fluorometric microculture cytotoxicity assay (FMCA) revealed that compound 1 was cytotoxic to AGS human gastric adenocarcinoma cells. The treatment of AGS cells with 1 decreased β-catenin levels and also inhibited its nuclear localization. The pretreatment of AGS cells with a proteasome inhibitor, either MG132 or epoxomicin, protected against the degradation of β-catenin induced by 1. The 1-induced degradation of β-catenin was also abrogated in the presence of pifithrin-α, an inhibitor of p53 transcriptional activity. Compound 1 inhibited TOP activity in AGS cells and downregulated the protein levels of cyclin D1, c-myc, and survivin. Compound 1 also sensitized AGS cells to tumor necrosis factor-related apoptosis ligand (TRAIL)-induced apoptosis by increasing the levels of the death receptors, DR4 and DR5, and decreasing the level of the antiapoptotic protein Bcl-2. Collectively, our results demonstrated that 1 induced the p53- and proteasome-dependent degradation of β-catenin, which resulted in the inhibition of TCF/β-catenin transcription in AGS cells. Furthermore, 1 enhanced apoptosis in TRAIL-resistant AGS when combined with TRAIL.

A B S T R A C T The Wnt signal regulates various biological processes, and its aberrant activation is associated with the development of diseases. Thus, inhibiting the Wnt signal provides a promising strategy to treat these diseases. Our cell-based luciferase assay system, which targets the Wnt signal (TOP assay), revealed that Azadirachta excelsa inhibited the Wnt signal. The activity-guided isolation of the MeOH fruit extract of A. excelsa provided one new (1) and seven known (2–8) limonoids. Their structures were elucidated based on their spectroscopic data, and their NMR data were compared with those in the literature. Compounds 3–6 potently inhibited the Wnt signal with IC50 values of 127 nM, 300 nM, 252 nM, and 121 nM, respectively. Compound 4 exhibited selective cytotoxicity against AGS and HCT116. Western blot analysis showed that 4 did not affect the level or localization of b-catenin, but downregulated the level of c-myc. Our results suggested that 4 may have inhibited the Wnt signal by affecting the components downstream of b-catenin.

Neurodegenerative diseases such as Alzheimer’s disease and Parkinson’s disease occur due to loss of the structure and function of neurons. For the potential treatment of neurodegenerative diseases, accelerators of neuronal differentiation of neural stem cells (NSCs) have been focused on and a cell-based assay system for measuring Notch signaling pathway activity was constructed. Using this assay system, eight compounds isolated from Calotropis gigantea were identified as inhibitors of the Notch signaling pathway. Hes1 and Hes5 are target genes of the Notch signaling pathway, and compound 1, called uscharin, decreased the protein levels of Hes1 and Hes5 in assay cells and MEB5 cells (mouse NSCs). Furthermore, uscharin (1) enhanced the differentiation of MEB5 cells into neurons. The mechanism of uscharin (1) for the Notch signaling inhibitory activity would be acceleration of the degradation of the Notch intracellular domain (NICD) in the MEB5 cells.

Wnt signaling plays important roles in proliferation, differentiation, development of cells, and various diseases. Activity-guided fractionation of the MeOH extract of the Ricinus communis stem led to the isolation of four compounds (1-4). The TCF/β-catenin transcription activities of 1 and 3 were 2.2 and 2.5 fold higher at 20 and 30μM, respectively. Cells treated with ricinine (1) had higher β-catenin and lower of p-β-catenin (ser 33, 37, 45, Thr 41) protein levels, whereas glycogen synthase kinase 3β (GSK3β) and casein kinase 1α (CK1α) protein levels remained unchanged. Cells treated with pyrvinium, an activator of CK1α, had lower β-catenin levels. However, the combined treatment of pyrvinium and 1 led to higher β-catenin levels than those in cells treated with pyrvinium alone, which suggested that 1 inhibited CK1α activity. Furthermore, 1 increased β-catenin protein levels in zebrafish embryos. These results indicated that 1 activated the Wnt signaling pathway by inhibiting CK1α.

Wnt signaling plays key roles in embryonic development and various human diseases. Activity-guided testing to isolate Wnt signaling inhibitors from the methanol extract of Calotropis gigantea (Asclepiadaceae) exudutes identified six Wnt inhibitory cardenolides (1-6), of which 1, 3, 5, and 6 exhibited potent TCF/β-catenin inhibitory activities (IC50 0.7-3.6 nM). Calotropin (1) inhibited Wnt signaling by decreasing both nuclear and cytosolic β-catenin in a dose-dependent manner, and promoted degradation of β-catenin by increasing the phosphorylation of β-catenin at Ser45 through casein kinase 1α (CK1α). Moreover, 1 significantly increased CK1α protein and mRNA levels. The results suggest that 1 inhibits the Wnt signaling pathway by increasing CK1α protein levels. To the best of our knowledge, calotropin is the first small molecule to increase CK1α levels.

TRAIL is a potent inducer of apoptosis in most cancer cells, but not in normal cells, and therefore has deserved intense interest as a promising agent for cancer therapy. In the search for bioactive natural products for overcoming TRAIL-resistance, we previously reported a number of active compounds. In our screening program on natural resources targeting overcoming TRAIL-resistance, activity-guided fractionation of the MeOH extract of Datura stramonium leaves led to the isolation of three alkaloids--scopolamine (1), trigonelline (2), and tyramine (3). Compounds 1, 2, and 3 exhibited TRAIL-resistance overcoming activity at 50, 150, and 100 µM, respectively in TRAIL-resistant AGS cells.

In a screening program for natural products that can overcome TRAIL resistance, a new eudesmane-type sesquiterpenoid (1), three new guaianolides, mehirugins A-C (2-4), and two known guaianolides (5 and 6) were isolated from a MeOH extract of Kandelia candel leaves. Compounds 1 and 3-6 in combination with TRAIL showed cytotoxic activity in sensitizing TRAIL-resistant human gastric adenocarcinoma cells.

The methanolic extract of Acanthus ilicifolius Linn. (Acanthaceae) leaves was assessed for its possible antinociceptive activity by using acetic acid-induced writhing, formalin and hot plate test. The oral administration of the MeOH extract at the doses of 250 and 500 mg/kg of body weight showed significant and dose dependent antinociceptive activity in all the three models used. This indicates the existence of both central and peripheral mechanism of antinociceptive action of the extract. All the experimental results suggest that methanolic extract of A. ilicifolius leaves contain constituents having antinociceptive properties and thus support its popular folkloric uses in the management of pain

The inhibition of the Hedgehog (Hh) signaling pathway has emerged as an anti-cancer strategy. Three flavonoid glycosides including 2 new compounds (1-2) were isolated from Excoecaria agallocha as Hedgehog/GLI1-mediated transcriptional inhibitors and exhibited cytotoxicity against human pancreatic (PANC1) and prostate (DU145) cancer cells. Our data revealed that compound 1 clearly inhibited the expression of GLI-related proteins (PTCH and BCL-2) and blocked the translocation of GLI1 transcription factors into the nucleus in PANC1. Deleting the Smoothened (Smo) function in PANC1 treated with 1 led to downregulation of the mRNA expression of Ptch. This study describes the first Hh signaling inhibitor which blocks GLI1 movement into the nucleus without interfering with Smo.

Bioassay guided separation of Sida acuta whole plants led to the isolation of an alkaloid, cryptolepine (1), along with two kaempferol glycosides (2–3). Compound 1 showed strong activity in overcoming TRAIL-resistance in human gastric adenocarcinoma (AGS) cells at 1.25, 2.5 and 5 μm. Combined treatment of 1 and TRAIL sensitized AGS cells to TRAIL-induced apoptosis at the aforementioned concentrations. Copyright © 2010 John Wiley & Sons, Ltd.

Fuligocandins A and B, cycloanthranilylproline derivatives isolated from the myxomycete Fuligo candida, were synthesized efficiently by a Meyer―Schuster rearrangement, which gave Z-isomer with high selectivity. The absolute stereochemistry at C-11a of the natural products was determined to be S by comparison of the optical rotation of the natural products with synthetic counterparts derived from L-proline. This report is the first total synthesis of optically active fuligocandin B.

As part of the search for new sources of mental health supplements, alcohol extracts of 11 Bangladeshi medicinal fruits and plants were investigated for neuropharmacological effects in mice and on ionotropic γ-aminobutyric acid receptors (GABAA receptors). The extracts of S. caseolaris, T. bellirica, S. cumini, and T. arjuna significantly potentiated the GABA-induced response of GABAA receptors expressed in Xenopus oocytes, though the extracts alone induced no response. In mice, administration of these extracts prolonged pentobarbital-induced sleeping time. Potentiation of GABAA receptor response reportedly generates anxiolytic, sedative, sleep-inducing and anesthetic activities in the human brain. Thus, these extracts may have potential regarding the development of a supplement with tranquilizing and sleepinducing effects that is beneficial for mental health.

SUMMARY The MeOH extract of seeds of Cerbera odollam Gaertn. (Apocynaceae) was screened for its antibacterial,cytotoxic and neuropharmacological activities. The extract showed moderate anti-bacterialactivity against Salmonella typhi, Streptococcus saprophyticus, and Streptococcus pyogenes. It exhibitedhigh level cytotoxicity against brine shrimp (LC 50 : 3 µg/ml). The extract potentiated pentobarbitalinduced sleeping time in mice which was further supported by the exploratory behavior test atdose of 25 mg/kg. The overall results tend to suggest the antibacterial, cytotoxic and CNSdepressant activities of the extract. Key words: Cerbera odollam; Antibacterial activity; Cytotoxic activity; CNS depressant activity INTRODUCTION Cerbera odollam Gaertner (pink-eyed cerbera, yellow-eyed cerbera, odollam tree), also sometimes calledCerbera manghas L, belongs to the notoriously poisonousApocynaceae family, which also includes theyellow oleanders (Thevetia peruviana and Thevetianerifolia) and common oleanders (Nerium oleanderand Nerium indicum). The C. odollam tree grows toa height of 6 - 15 m and has dark green fleshylanceolate leaves. The large white flowers have adelicate perfume, reminiscent of jasmine. Thefruit, when still green, looks like a small mango,with a green fibrous shell enclosing an ovoidkernel measuring approximately 2 cm × 1.5 cmand consisting of two cross-matching white fleshyhalves. On exposure to air, the white kernel turnsviolet, then dark grey, and ultimately brown orblack. The plant as a whole yields a milky whitelatex. The tree grows in coastal salt swamps andcreeks in south India (particularly abundantlynear the canals and backwaters of Kerala) andalong riverbanks in southern and central Vietnam,Cambodia, Sri Lanka, Bangladesh and Myanmar.In Bangladesh the plant is known as Dabur,Dhakur or Um-dabur. The seeds have a longhistory as an ordeal poison in Madagascar, due tothe highly toxic cardiac glycosides they contain.The seeds contain non-siccative oil, producing ashining flame with a pleasant nut-like odour. TheBurmese use it for lighting, as a cosmetic, ormixed with other oils as an insecticide or insect-repellent (Chopra et al., 1956). The bark and leavesof the plant are traditionally used as emetic andcathartic; kernels are used as emetic; fruit is usedas a cure for hydrophobia (Kirtikar and Basu,1987). Its bark and fruits are purgative and used