Synthesis of rocaglamide derivatives and evaluation of their Wnt signal inhibitory activities.

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.

Antinociceptive and antioxidant potential of the crude ethanol extract of the leaves of Ageratum conyzoides grown in Bangladesh.

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.

Synthesis of Magnetic Iron Oxide-Incorporated Cellulose Composite Particles: An Investigation on Antioxidant Properties and Drug Delivery Applications.

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.

Exploration of In Vivo and In Vitro Biological Effects of Sonneratia caseolaris (L.) Fruits Supported by Molecular Docking and ADMET Study.

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-ß-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-ß-glucoside had two violations in Lipinski's rule of five.

Antinociceptive, anti-inflammatory and antidiarrheal activities of ethanolic calyx extract of Hibiscus sabdariffa Linn. (Malvaceae) in mice.

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.

Phytol: A review of biomedical activities.

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.

Medicinal potential of Passiflora foetida L. plant extracts: biological and pharmacological activities.

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.