Current Bioactive Compounds - Volume 21, Issue 1, 2025

Biosurfactants are very important amphiphile compounds due to their interesting advantages such as low toxicity, biodegradability and also their many biological properties.

In the present study, antimicrobial and anti-imflammatory activities were evaluated to determine the biological proprieties of biosurfactant BLA 2906 produced by Alcaligenes aquatilis YGD 2906 using different assays. Screening and optimization component concentrations in the medium were investigated using PBD and SRM to increase surfactant yield in term emulsification activity value (E24%).

The halos of antifungal activity presented a mean value of 12.33 mm to 17.67 mm. For antibacterial activity, the diameter varied from 10.33 to 12.67 mm with a very important anti-inflammatory activity using a protein denaturation method that showed a maximum inhibition of 92.79%.

These results suggest that BLA 2906 may be used as a new therapeutic and anti-inflammatory agent. The PBD selected 7 significant components out of the 14 screened. The RSM resulted in the production in terms of emulsification activity of 68.37% in the optimized medium.

Nimodipine is a highly lipophilic anti-hypertensive drug having 13% oral bioavailability (log P 3.41). Nimodipine is a prominent calcium channel blocker that must be given intravenously for an extended period of time (1-2 weeks) in order to treat cerebral vasospasm. It might be possible to substitute a sustained-release biodegradable formulation for the ongoing intravenous infusion used in this traditional therapy.

The primary goal of this study was to formulate and evaluate the potentiality of ethosomes to deliver nimodipine, a potent water-insoluble anti-hypertensive drug, through the deeper layers of the skin. The greatest challenge for drug formulation is its poor oral bioavailability and solubility.

Nimodipine-loaded ethosomal gel was developed for transdermal drug delivery to increase solubility and skin penetration and to promote oral bioavailability. Central composite design employing a thin-film hydration method was used to prepare and optimize ethosomes. A better dispersion medium for nimodipine's preparation in ethosomes was selected based on the effect. The design consisted of independent variables as lipid (X1), ethanol (X2), and sonication time (X3). Concentrations were manipulated to examine the effects on three responses, namely the %entrapment efficiency (Y1), vesicle size (Y2), and %cumulative drug release (Y3). Surface morphology and other in vitro tests were used to identify ethosomes containing nimodipine. The preparation of ethosomal gel formulations began with incorporating a single ethosomal formulation (F4) into various concentrations of gelling agents. These studies performed physicochemical characterization, compatibility testing, and in vitro drug release tests on ethosomal gels. In vivo studies involving hypertensive rats were conducted after skin permeation, and ex vivo studies were performed. In order to assess the drug's permeability and deposition, we employed the abdomen skin of rats.

The optimal process parameters resulted in ethosomes with 89.9 ± 0.19 percent entrapment efficiency, a vesicle size of 102.37 ± 5.84 nm, and a cumulative drug release of 98.3 ± 0.13%. pH and drug content measurements were consistent with the homogeneous ethosomal gels. Viscosity was found to increase with the spreadability. The ethosomal gel formulation (G2) met the regulatory standards regarding appearance, spreadability, viscosity, and in vitro release studies. Compared to pure nimodipine, ethosomal suspension (F4) and ethosomal gel (G2) formulations had higher ex vivo permeation, steady-state flux, and drug retention. Rats' mean arterial pressure (146.11 ± 0.84 mmHg) was significantly lower (p < 0.01) after after two hours of the experiment than it had been (p < 0.001) (98.88 ± 0.63 mmHg) after six hours.

To summarize, ethosomal gels have been found to be lipid carriers that enhance skin permeation and extend the anti-hypertensive effect of nimodipine. Compared to plain gel, ex vivo drug permeation through rat abdominal skin in ethosomal gel was enhanced. Gel-based ethosomal transdermal drug delivery formulations of nimodipine can be used to achieve a faster rate and extend the duration of drug delivery by more than 24 hours.

By condensing 2-aminothiazole and phenacyl bromide, a novel
catalyst-free synthetic approach for the synthesis of imidazo[2,1-b]thiazole derivatives has been
developed.

In this work, aloe vera/water (3:2) is used as a reusable, environmentally benign, green-promoting media to synthesize desired products. This method enables the synthesis of a diverse range of aryl-substituted imidazo[2,1-b]thiazoles.

This solvent system demonstrates remarkable efficiency and offers numerous advantages, including shorter reaction times, the absence of side product formation, cost-effectiveness, excellent atom efficiency, straightforward operation, and high yields.

We successfully developed a green protocol for the environmentally benign synthesis of imidazo[2,1-b]thiazole derivatives using aloe vera water as green-promoting media.

The constant increase in global onion production escalates the 
generation of onion peel waste. For instance, globally, >50 lakh tons of onion waste are generated annually.

Its objectionable odor precludes its use in agriculture or disposal as landfilling presents environmental issues. Previous studies show that two major flavonoids, quercetin and its
glycosides (spiraeoside), have been identified in abundance in onion waste. By utilizing the
spiraeoside (quercetin-4ʹ-glucoside), a rapid synthesis of pachypodol (quercetin-3,3′,7-trimethyl ether, and a rare flavonol), an essential Ayurvedic product, has been developed and achieved. Pachypodol and analogs were studied for their ability to inhibit matrix metalloproteinase-2 and 
-9 (MMP-2 & 9) activity. Amongst the compounds tested, pachypodol significantly inhibited MMP-2 activity.

In-silico docking studies suggest that, unlike most known MMP inhibitors, pachypodol interacts selectively with MMP-2 through the residues Ile222, Tyr223, and Thr227 in a zinc-independent manner.

The experimental studies also prove that pachypodol inhibits the MMP-2 enzyme in a zinc-independent way.

The study addresses the underexplored realm of cytotoxicity evaluation involving binary mixtures of Passiflora caerulea leaf extracts and Titanium nanoparticles (TiO2NPs). The focus lies on understanding the combined effects of these components on cancer cells (A549, U937, and HeLa).

In vitro cytotoxicity assessments were employed to evaluate the toxicity of P. caerulea leaf extracts, TiO2NPs, and their combination. The study utilized MTT, NRU, and LDH assays to measure cellular viability. Additionally, reactive oxygen species (ROS) and glutathione levels were assessed alongside the aforementioned assays.

The toxicity percentage exhibited dose-dependent behavior for P. caerulea leaf extracts, TiO2NPs, and their combination. Interestingly, when P. caerulea leaf extract and TiO2NPs were combined, the reduction in cell viability was noticeably more than when the exposures were made separately. Moreover, the production of ROS was higher in the combined toxicity scenario, and a more pronounced decrease in glutathione levels was observed compared to individual exposures.

The findings suggest that the combined effects of P. caerulea leaf extract and TiO2NPs induce greater cytotoxicity compared to their impacts. This underscores the potential for synergistic cytotoxicity in combined exposure scenarios, warranting further exploration of combined effects in future studies.

The encapsulation technique is an effective method for coating bioactive molecules and protecting them against various technological treatment conditions during production processing.

The aim of this study was to optimize the encapsulation conditions of phenolic compounds extracted from Malabar nut (Justicia adhatoda L.) leaves by alginate emulsion-gelation approach using response surface methodology.

The ionotropic gelation method was used to encapsulate the phenolic compounds of Malabar nut (Justicia adhatoda L.) leaves. The optimization of this phenolic compounds encapsulation was carried out using response surface methodology through Box˗Behnken design. Four parameters with three levels (-1, 0, +1) were chosen including sodium alginate concentration
(2 - 3 - 4%), calcium chloride concentration (4 - 6 - 8%), plant extract-alginate solution ratio (0.02 - 0.11 - 0.2 mg/ml), and gelation time (5 - 12.5 - 20 min). Total phenolic and flavonoid contents encapsulation efficiency was assessed. Likewise, the antioxidant activity was evaluated using ferric-reducing power (FRP) and free radical scavenging activity (DPPH).

The results of response surface methodology analysis using Box˗Behnken design showed that the optimal encapsulation conditions were 3.11% for alginate concentration, 5.74% for calcium chloride concentration, 0.1 mg/ml for the plant extract-alginate solution ratio, and 10.80 min for gelation time. Under these conditions, the optimum values of total phenolic and flavonoid encapsulation efficiency were 86.17% and 75.69%, respectively, 126.75 mg AAE/100 g for ferric reducing power and 97.29% for DPPH. The experimental and prediction results have expressed a high significant level for all responses.

The method revealed the validity of elaborated models through response surface methodology optimization processes for phenolic antioxidants encapsulation of Malabar nut
(Justicia adhatoda L.) leaves extract.