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Sonneratia caseolaris (L.) is a common mangrove plant which has significant medicinal value in traditional medicine. Ethanol extract from the fruits of S. caseolaris (SCE) was used in this project to explore its different pharmacological effects considering its traditional usage. In the castor oil-induced diarrheal method, SCE significantly lengthened the latency of the first defecation period up to 95.8 and 119.4 min as well as lowering stool count by 43.3% and 64.4% at the doses of 250 and 500 mg/kg, respectively. In evaluating the neuropharmacological effect using the open-field model, a significant central nervous system (CNS) depressant nature was observed after a reduction in the no. of squares crossed by mice at various time intervals. In evaluating the blood coagulation effect, SCE significantly reduced blood clotting time at 5.86, 5.52, and 5.01 min at 25, 50, and 100 mg/ml doses, respectively. In the assessment of the anthelmintic effect, SCE significantly killed Paramphistomum cervi ( P. cervi ) where the death times of the nematodes were 40.3, 36.8, and 29.9 min at 12.5, 25, and 50 mg/ml doses, respectively. The extract showed a very poor cytotoxic effect in brine shrimp lethality bioassay. In molecular docking analysis, maslinic acid, oleanolic acid, luteolin, luteolin 7- O - β -glucoside, myricetin, ellagic acid, and R-nyasol showed the best binding affinities with the selected proteins which might be the credible reasons for eliciting pharmacological responses. Among these seven compounds, only luteolin 7- O - β -glucoside had two violations in Lipinski's rule of five., Competing Interests: There is no point of conflict of interest among the authors., (Copyright © 2023 Pritam Kundu et al.)

In recent years, polymer-supported magnetic iron oxide nanoparticles (MIO-NPs) have gained a lot of attention in biomedical and healthcare applications due to their unique magnetic properties, low toxicity, cost-effectiveness, biocompatibility, and biodegradability. In this study, waste tissue papers (WTP) and sugarcane bagasse (SCB) were utilized to prepare magnetic iron oxide (MIO)-incorporated WTP/MIO and SCB/MIO nanocomposite particles (NCPs) based on in situ co-precipitation methods, and they were characterized using advanced spectroscopic techniques. In addition, their anti-oxidant and drug-delivery properties were investigated. Field emission scanning electron microscopy (FESEM) and X-ray diffraction (XRD) analyses revealed that the shapes of the MIO-NPs, SCB/MIO-NCPs, and WTP/MIO-NCPs were agglomerated and irregularly spherical with a crystallite size of 12.38 nm, 10.85 nm, and 11.47 nm, respectively. Vibrational sample magnetometry (VSM) analysis showed that both the NPs and the NCPs were paramagnetic. The free radical scavenging assay ascertained that the WTP/MIO-NCPs, SCB/MIO-NCPs, and MIO-NPs exhibited almost negligible antioxidant activity in comparison to ascorbic acid. The swelling capacities of the SCB/MIO-NCPs and WTP/MIO-NCPs were 155.0% and 159.5%, respectively, which were much higher than the swelling efficiencies of cellulose-SCB (58.3%) and cellulose-WTP (61.6%). The order of metronidazole drug loading after 3 days was: cellulose-SCB < cellulose-WTP < MIO-NPs < SCB/MIO-NCPs < WTP/MIO-NCPs, whereas the sequence of the drug-releasing rate after 240 min was: WTP/MIO-NCPs < SCB/MIO-NCPs < MIO-NPs < cellulose-WTP < cellulose-SCB. Overall, the results of this study showed that the incorporation of MIO-NPs in the cellulose matrix increased the swelling capacity, drug-loading capacity, and drug-releasing time. Therefore, cellulose/MIO-NCPs obtained from waste materials such as SCB and WTP can be used as a potential vehicle for medical applications, especially in a metronidazole drug delivery system.

Phytol (PYT) is a diterpene member of the long-chain unsaturated acyclic alcohols. PYT and some of its derivatives, including phytanic acid (PA), exert a wide range of biological effects. PYT is a valuable essential oil (EO) used as a fragrance and a potential candidate for a broad range of applications in the pharmaceutical and biotechnological industry. There is ample evidence that PA may play a crucial role in the development of pathophysiological states. Focusing on PYT and some of its most relevant derivatives, here we present a systematic review of reported biological activities, along with their underlying mechanism of action. Recent investigations with PYT demonstrated anxiolytic, metabolism-modulating, cytotoxic, antioxidant, autophagy- and apoptosis-inducing, antinociceptive, anti-inflammatory, immune-modulating, and antimicrobial effects. PPARs- and NF-κB-mediated activities are also discussed as mechanisms responsible for some of the bioactivities of PYT. The overall goal of this review is to discuss recent findings pertaining to PYT biological activities and its possible applications., (Copyright © 2018 Elsevier Ltd. All rights reserved.)

TRAIL is a potent and selective inducer of apoptosis in most cancer cells while sparing normal cells, which makes it an attractive target for the development of new cancer therapies. In a screening program on natural resources with the ability to abrogate TRAIL resistance, the bioassay-guided fractionation of Boesenbergia pandurata rhizomes resulted in the isolation of 17 pimarane diterpenes and a monoterpene. Among these, compounds 1-8, named boesenberols A-H, are new pimarane diterpenes. All compounds exhibited TRAIL-resistance-overcoming activity in TRAIL-resistant AGS cells. Subtoxic doses of the major compound 9 sensitized AGS cells to TRAIL-induced apoptosis by up-regulating apoptosis-inducing proteins, such as DR4, DR5, p53, Fas, CHOP, Bak, and cleaved caspases-3, -8, and -9, and down-regulating the levels of cell survival proteins, such as Bcl-2, c-FLIP, and GSK-3β, in TRAIL-resistant AGS cells. Furthermore, compound 9 did not decrease the viability of noncancerous (HEK293) cells at concentrations up to 30 μM.

Two new phenazine derivatives, aotaphenazine (1) and 5,10-dihydrophencomycin (2), were isolated from the ethyl acetate extract of Streptomyces sp. IFM 11694. In addition, the known 1-phenazinecarboxylic acid (3), phencomycin (4) and 1,6-phenazinedicarboxylic acid (5) were identified. The structures of the isolated compounds (1-5) were characterized by spectroscopic methods including NMR and mass spectrometry data. Compound 1 showed the ability to overcome tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) resistance at concentration of 12.5 μM. Aotaphenazine (1) enhanced the levels of apoptosis inducing proteins DR4, DR5, p53 and also decreased the levels of cell survival protein Bcl-2 in TRAIL-resistant human gastric adenocarcinoma (AGS) cells in a dose-dependent manner.

One new alkyl sulfonic acid derivative, sulfotanone (1), and the known panosialin wA (2) were isolated from the methanolic extract of mycelium of Streptomyces sp. 11694. The structure of the new compound (1) was established by a combination of spectroscopic techniques, including HRESIMS, IR, 1D and 2D NMR measurements. Compound 1 (40 µM) in combination with TRAIL showed synergistic activity in sensitizing TRAIL-resistance in human gastric adenocarcinoma cell lines.

Rocaglamides are bioactive natural compounds which have a cyclopenta[b]benzofuran core structure. The total synthesis of a reported natural product, 3'-hydroxymethylrocaglate (5), was achieved using [3 + 2] cycloaddition between 3-hydroxyflavone and methyl cinnamate. We also describe the synthesis of rocaglamide heterocycle derivatives and evaluate their Wnt signal inhibitory activities. Compounds 4, 5, 22a, 22b, 22c and 23c showed potent Wnt signal inhibitory activity.

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.

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., (Copyright © 2015 Elsevier Ltd. All rights reserved.)

Objective: To investigate analgesic, antidiarrhoeal and cytotoxic activities of the ethanol extract of Passiflora foetida L. (Passifloraceae) by three experimental methods., Methods: Analgesic activity of the ethanol extract of Passiflora foetida L. (EEPF) acetic acid-induced writhing inhibition in mice. The method of castor oil-induced diarrhoea in mice was utilized to evaluate antidiarrhoeal activity. The cytotoxic activity of EEPF was explored with a brine shrimp lethality bioassay., Results: The extract showed 68.75% and 30.00% inhibition of writhe at the doses of 500 and 250 mg/kg body weight, respectively. The extract increased the mean latent period prior to diarrhoeal onset to about 1.55 h and 1.17 h, and decreased the mean number of stools to 4.4 and 5.6 at the doses of 500 and 250 mg/kg body weight. The extract also demonstrated cytotoxic activity in the brine shrimp lethality assay, and the median lethal concentration for brine shrimp nauplii was 80 μg/mL., Conclusion: The results suggest that the plant extract has analgesic and antidiarrhoeal activities, supporting its uses in traditional medicine. The results also demonstrate that the plant extract possesses cytotoxic activities.

Context: Ageratum conyzoides Linn. (Asteraceae) is an annual herbaceous plant with a long history of traditional medicinal and agricultural uses; it is usually grown in the northeast part of Bangladesh., Objective: The ethanol extract of the plant leaves was evaluated for preliminary phytochemical screening with its antinociceptive and antioxidant activities., Materials and Methods: The preliminary phytochemical analysis was performed on the basis of standard procedures. The analgesic activity of the extract was investigated using the acetic acid-induced writhing method in mice. Five complementary tests such as DPPH free radical scavenging, nitric oxide (NO) scavenging, reducing power, Fe(++) ion chelating ability and total phenolic content were used for determining antioxidant activities., Results: The results of preliminary phytochemical analysis showed the presence of alkaloids, reducing sugars, saponins, gums, steroids, tannins and flavonoids. The extract possessed a significant dose-dependent DPPH free radical scavenging activity with an IC50 value of 18.91 μg/ml compared to ascorbic acid (IC50: 2.937 μg/ml) and butylated hydroxyanisole (IC50: 5.10 μg/ml). The IC50 value of the extract for NO scavenging (41.81 μg/ml) was also found to be significant compared to the IC50 value of ascorbic acid (37.93 μg/ml). Moreover, the extract showed reducing power activity and Fe(++) ion chelating ability. The total phenolic amount was also calculated as quite high (378.37 mg/g of gallic acid equivalents) in the crude ethanol extract., Discussion and Conclusion: Therefore, the obtained results tend to suggest the antinociceptive and antioxidant activities of the ethanol extract of the plant leaves and justify its use in folkloric remedies.

Objective: To evaluate the antinociceptive, anti-inflammatory and antidiarrheal activities of the ethanolic calyx extract of Hibiscus sabdariffa Linn. in mice., Methods: In the present study, the dried calyxes of H. sabdariffa were subjected to extraction with 95% ethanol and the extract was used to investigate the possible activities. Antinociceptive activity of the extract was evaluated by using the acetic acid-induced writhing test. The anti-inflammatory effect of the extract was tested by using the xylene-induced ear edema model mice. Castor oil-induced diarrheal model mice were used to evaluate the antidiarrheal activity of the extract., Results: In acetic acid-induced writhing test, the extract produced inhibited writhing in mice significantly compared with the blank control (P<0.01). The extract showed significant inhibition of ear edema formation in xylene-induced ear edema model mice in a dose-related manner compared with the blank control (P<0.01). The extract demonstrated a significant antidiarrheal activity against castor oil-induced diarrheal in mice in which it decreased the frequency of defecation and increased the mean latent period at the doses of 250 and 500 mg/kg body weight (P<0.01)., Conclusion: The above mentioned findings indicate that the calyx extract of H. sabdariffa possesses significant antinociceptive, anti-inflammatory and antidiarrheal activities that support its uses in traditional medicine.

Objectives: Urinary tract infection is the second most common clinical indication for empirical antibiotic treatment in primary and secondary health care settings. The incidence of diabetes mellitus throughout the world is increasing strikingly and in the long run, it has some major effects on the genitourinary system which makes diabetic patients more liable to urinary tract infection. This study is designed to reveal the distribution of uropathogens in diabetic patients according to age and sex, and corresponding resistance patterns., Methods: A six-month retrospective review of urine culture assay data from August 2009 to January 2010 from randomly selected 85 patients who suffered from both urinary tract infection and diabetes was conducted. Relevant information was retrieved and analyzed statistically using Microsoft® Excel 2002 software., Results: The study showed that females are more vulnerable to pathogenic attack than males throughout a wide age distribution. In terms of pathogenic distribution, Escherichia coli was the highest followed by Streptococcus sp., Acinetobacter, Klebsiella pneumoniae and few others. Though Meropenem showed no resistance with E. coli, Acinetobacter and Klebsiella pneumoniae, in the case of Streptococcus sp. it exhibited resistance of 25%. Amikacin exhibited only 3% resistance with E. coli, whereas no resistance with Acinetobacter and Klebsiella pneumoniae, and most interestingly showed 75% resistance with Streptococcus sp. Gentamicin exhibited no resistance with Acinetobacter while 26.9%, 50% and 87.5% resistance with E. coli, Klebsiella pneumoniae and Streptococcus sp. respectively. Hence, Nitrofurantoin exhibited less resistance 11.9% compared to 12.5% resistance with E. coli and Streptococcus sp. Nitrofurantoin was highly prone to resistance with Acinetobacter and Klebsiella pneumoniae (100%, 50% respectively). Cephalosporins (cephradine, cefixime, ceftriaxone, cefepime etc.) showed moderate resistance (avg. 50%), whereas amoxicillin and ciprofloxacin showed the highest resistance in all these cases., Conclusion: Pathogens are mostly resistant to antibiotics including amoxicillin, ciprofloxacin, cephalosporins and nitrofurantoin, with few exceptions including gentamicin, amikacin and meropenem.

Background: Toxicokinetics and recovery studies of dicamba dimethyl amine salt (DDAS) were conducted to obtain more information about its toxicity and tissue retention in farm animals., Results: The minimum oral toxic dose level of DDAS was determined as 1400 mg kg(-1) body weight. In the toxicokinetic study, blood DDAS concentration of 55.6 +/- 0.59 microg mL(-1) (mean +/- standard error) was detected at 0.08 h, which peaked to 102.3 +/- 5.03 microg mL(-1) at 0.25 h, and declined to a minimum of 4.1 +/- 0.06 microg mL(-1) at 36 h. In recovery studies, DDAS concentration in urine began to increase significantly (P < 0.05) from 12 h, peaked at 24 h and declined from 48 h onwards. Maximum excretion through faeces was at 24 h and was complete by 144 h. The residual level in tissues decreased significantly (P < 0.05) on day 7 as compared to day 4. In histopathological studies, cellular alterations in lungs, liver, kidney, adrenal gland and spleen were found., Conclusion: DDAS persists in the body for a shorter period and its major excretory route is through urine. DDAS has lower affinity to accumulate in tissues, and intensity of cellular alterations is not severe after single-dose oral administration., ((c) 2009 Society of Chemical Industry.)