Current Bioactive Compounds - Volume 21, Issue 9, 2025

Momordica dioica belongs to the family Cucurbitaceae and is generally known as teasle gourd or spiny gourd. This plant is highly significant for its active phytoconstituents bearing several pharmacological activities.

This study aims to evaluate the anthelmintic activity of biosynthesized Silver nanoparticles of Momordica dioica fruit extract against Pheretima Posthuma.

Momordica dioica silver nanoparticles were prepared by green synthesis and were characterized using spectroscopic methods like UV-visible, FTIR, and Scanning Electron Microscopy (SEM) techniques. The prepared silver nanoparticles were investigated for the targeted activity using Albendazole as standard and normal saline as the control.

The UV-visible spectrophotometer showed absorbance in the range of 424 nm. FTIR revealed the presence of functional groups of both extract and nanoparticles. The spherical shape of the AgNPs and their size ranges below 100 nm by SEM. The in-vitro anthelmintic activity showed the paralysis and mortality rate of the worms for the fruit extract, and silver nanoparticles were found to be 45.03 ± 0.1, 60.13 ± 0.1, and 12.35 ± 0.04, 22.34 ± 0.02 by One way ANOVA (p <0.0001).

The fruit extract converted to silver nanoparticles had better anthelmintic activity compared to the fruit extract. The paralysis and death time were reduced 4 to 5 times, which showed the improved effect of the silver nanoparticles of Momordica dioica extract.

The current method of controlling malaria vectors using synthetic chemicals has caused serious problems for human health and the environment. Hence, a need for alternative, cheap, readily available, and acceptable mosquito control methods.

To evaluate the bioinsecticidal efficacy of Ocimum gratissimum and Mesosphaerum suaveolens against Anopheles gambiae using the bioassay method.

Oil extracts in 5 ml, 25 ml, and 75 ml serially diluted twice in 100 ml of olive oil formed 0.05%, 0.25%, and 0.75%, while 1 m in 100 ml formed 1%. Olive oil only served as a control. Twenty-five female Anopheles mosquitoes, aged 2-4 days, were blown into tubes containing filter paper-coated essential oils of various concentrations in quadruplicates.

Over 50% mortality was recorded in mosquitoes exposed to 0.75% and 1% O. gratissimum compared to others (p <0.05). Knockdown time (KDT) was higher in mosquitoes exposed to 1% O. gratissimum compared to others (p <0.05). Generalized linear regressions showed that the essential oils of O. gratissimum and M. suaveolens contributed 4% (f² = 0.042) and 14% (f² = 0.167) to the variability of mortality with time. KDT50 (9.34 - 131.5 minutes) and KDT95 (77.6 - 275 minutes) of O. gratissimum as well as KDT50 (162.8 - 233.6 minutes) and KDT95 (302.8 - 415 minutes) of M. suaveolens were recorded. Stigmastane; 4,22-Stigmastadiene-3-one (Area: 45.88%) in O. gratissimum and gamma-Sitosterol (16.02%) in M. suaveolens were identified by Gas Chromatogram as the highest dose of chemical compounds.

The low bioinsecticidal activities of these plant extracts could be attributed to the low occurrence of terpenoids and alkaloids.

According to WHO, Alzheimer’s disease was estimated at 74.4 million cases in 2023, which will increase by 152.8 million cases in 2050. The therapeutic options available in the market for the treatment of AD are only capable of reducing the symptoms of dementia but not preventing progressive degeneration. Memantine is a non-competitive NMDAR antagonist used for the treatment of patients with moderate-to-severe AD, but it has a high toxicity profile. To counter this, the Memantine Schiff base derivatives were designed as simple and low-toxicity compounds.

Molecular docking was performed against the targeted enzymes Acetylcholinesterase and Butyrylcholinesterase using AUTODOCK 1.5.7 software. A series of novel Memantine derivatives of Schiff base were synthesized by condensing Memantine with various aryl aldehydes and screened for their in vitro -cholinesterase inhibitory activity towards Acetylcholinesterase (AChE) and Butyrylcholinesterase (BChE) by Ellman’s method.

Among the designed compounds, compounds LMV and LMC showed maximum binding scores of -10.35 kcal/mol and -10.12 kcal/mol, respectively, than the standard Donepezil (-8.78 kcal/mol) against Acetylcholinesterase. The compounds LMONB and LMDMB produced significant binding scores of -9.31 kcal/mol and -9.11 kcal/mol, respectively, compared to the standard Donepezil (-7.57 kcal/mol) against Butyrylcholinesterase. Also, compounds LMV (30.9 ± 2.13 μM) and LMDMB (13.51 ± 1.12 μM) showed potent inhibitory activity against the AChE and BChE. These compounds possess drug-like characteristics and are also capable of crossing the Blood-brain Barrier (BBB).

The studied compounds LMV and LMDMB, being non-toxic, obey Lipinski’s rule of 5 and are potential inhibitors against targeted enzymes, which may be promising clinical candidates for treating Alzheimer’s disease.

Present study deals to access the antidepressant activity of Etlingera elatior leaves extract in rodent.

Etlingera elatior is a species of herbaceous perennial plant in the family Zingiberaceae; native to Indonesia, Thailand, Malaysia and New Guinea. Depression is one of the most common mental disorders affecting humans, pathological basis of which is not fully understood. The current antidepressant drugs have several adverse effects including their effects on cognition. Therefore, natural product are being evaluated for their antidepressant activities.

In this study, Etlingera elatior leaf extracts are being evaluated for antidepressant activity in rodent models. A wide range of synthetic medicines that can be used to treat depression which may exerts various side effects such as dry mouth, gastrointestinal problems, nausea, respiratory problems, cardiac arrhythmias, drowsiness, anxiety etc. Hence, it becomes essential to discover new anti-depressant drug with more potency, efficacy and safety profile than those of marketed synthetic drugs.

Using the forced swimming test, the tail suspension test, mouse 5-HTP-induced head twitches and estimation of brain lipid peroxidation modelsthe antidepressant efficacy of Etlingera elatior ethanolic extract was examined. Imipramine was used as reference standards.

According to our study, Etlingera elatior significantly (p 0.01) reduced immobility in tail suspension, forced swimming, and 5-HTP-induced head twitches in mice with depression that were comparable to imipramine.

Based on the results obtained we can conclude that Etlingera elatior leaves extract possess significant antidepressant activity. The antidepressant effectiveness of Etlingera elatior leaves extract can be confirmed in the future by adding more models, and attempts can also be made to isolate and characterise the phytoconstituents responsible for the pharmacological action.

A preliminary biological evaluation of ten synthesized analogs, 5a-5j {[5-(E)-benzylidene amino]-1,3,4-thiadiazol-2-yl} cyclohexane-1,2,3,5-tetrol, revealed promising results, positioning these compounds as potential lead candidates for further optimization and preclinical exploration in cancer therapy. Incorporating the 1,3,4-thiadiazol moiety into the structure of the produced analogs considerably improved their anticancer activities, revealing the compound's high potential for cancer treatment. Spectroscopic approaches and structural analysis, such as elemental analysis, IR, ¹H NMR, ¹³C NMR, and MS, were crucial for properly establishing the molecular structures of these analogs and evaluating their anticancer activity. These methodologies laid a solid platform for rationally developing new anticancer medications with increased efficacy and fewer adverse effects. Furthermore, computational tools like molecular docking, ADMET prediction, and drug-likeness evaluation have accelerated the drug development by finding the most promising lead candidates for preclinical and clinical trials. This technique not only saves time and costs, but also raises the chances of producing successful anticancer drugs.

The main aim of the current study is to develop, synthesize, in-silico, in-vitro potentials of {5-[(E)-benzylidene amino]-1,3,4-thiadiazol-2-yl} cyclohexane-1,2,3,5-tetrol for a possible anticancer drug to improve their efficiency and selectivity against cancer cells, computational approaches aided in the rational design of these chemicals. Spectroscopic methods verified the chemical structures of the target compounds. The structures show the presence of 1,3,4-thiadiazol also responsible for anticancer activity. The 10 analogs were synthesized and showed encouraging anticancer efficacy in preliminary biological evaluation, suggesting they might be suitable lead candidates for more optimization and preclinical exploration.

{5-[(E)-benzylidene amino]-1,3,4-thiadiazol-2-yl} cyclohexane-1,2,3,5-tetrol derivatives 5a-5j showed optimum IC50 values in in vitro activity by SRB assay using MCF-7 as a strain, the few selected analogs.

The study synthesized cyclohexane-1,2,3,5-tetrol analogs and evaluated their potential for cancer therapy. The compounds showed promising cytotoxic activity against various cancer cell lines, with 5c, 5f, 5g, and 5j showing the most potent anti-proliferative effects. These compounds induce apoptosis via mitochondrial dysfunction and cell cycle arrest. Further preclinical investigations are needed to establish their therapeutic potential.