Efficacy Of Bioactive Compounds Research Articles

Trimethyl Lock Based Tools for Drug Delivery and Cell Imaging - Synthesis and Properties.

Trimethyl lock (TML) systems have become increasingly important in medicinal and bioorganic chemistry, particularly for their roles in the targeted delivery of therapeutic agents and as integral components in fluorogenic probes for cellular imaging. The simplicity and efficiency of their synthesis have established TML systems as versatile platforms for the controlled release of active molecules under particular physiological conditions. This review consolidates recent advancements in the application of TML systems, with a focus on their use in drug delivery, cellular imaging, and other areas where precise molecular release is crucial. Additionally, we discuss the synthetic strategies employed to construct TML-based conjugates, underscoring their potential to enhance the specificity and efficacy of bioactive compounds in various biomedical applications.

Streptomyces as a promising biological control agents for plant pathogens.

Plant diseases caused by pathogenic microorganisms in agriculture present a considerable obstacle, resulting in approximately 30-40% crop damage. The use of conventional techniques to manage these microorganisms, i.e., applying chemical pesticides and antimicrobials, has been discovered to have adverse effects on human health and the environment. Furthermore, these methods have contributed to the emergence of resistance among phytopathogens. Consequently, it has become imperative to investigate natural alternatives to address this issue. The Streptomyces genus of gram-positive bacteria is a potentially viable natural alternative that has been extensively researched due to its capacity to generate diverse antimicrobial compounds, such as metabolites and organic compounds. Scientists globally use diverse approaches and methodologies to extract new bioactive compounds from these bacteria. The efficacy of bioactive compounds in mitigating various phytopathogens that pose a significant threat to crops and plants has been demonstrated. Hence, the Streptomyces genus exhibits potential as a biological control agent for combating plant pathogens. This review article aims to provide further insight into the Streptomyces genus as a source of antimicrobial compounds that can potentially be a biological control against plant pathogens. The investigation of various bioactive compounds synthesized by this genus can enhance our comprehension of their prospective utilization in agriculture.

Efficacy of Bioactive Compounds in the Regulation of Metabolism and Pathophysiology in Cardiovascular Diseases.

An imbalance in reactive oxygen species (ROS) homeostasis can wreak damage to metabolic and physiological processes which can eventually lead to an advancement in cardiovascular diseases (CVD). Mitochondrial dysfunction is considered as a key source of ROS. The purpose of the current review is to concisely discuss the role of bioactive compounds in the modulation of cardiovascular metabolism and their potential application in the management of cardiovascular diseases. Recently, it has been shown that bioactive compounds exhibit immunomodulatory function by regulating inflammatory pathways and ROS homeostasis. It has also been reported that bioactive compounds regulate mitochondria dynamics, thus modulating the autophagy and energy metabolism in the cells. In the present article, we have discussed the roles of different bioactive compounds in the modulation of different inflammatory drivers. The functional properties of bioactive compounds in mitochondrial dynamics and its impact on cardiac disease protection have been briefly summarized. Furthermore, we have also discussed various aspects of bioactive compounds with respect to metabolism, immune modulation, circadian rhythm, and its impact on CVD's pathophysiology.

Morelloflavone as Potential Anticancer Agent Against MCF-7 Breast Cancer Cell Lines: In vitro and In silico Studies

Background: Breast cancer is most commonly reported to contribute to people's death. Nowadays, cancer treatment is focused on investigating anticancer drugs from natural compounds. Various methods, including in vitro, in vivo, and in silico methods, are used to assess the potential of anticancer compounds. The efficacy of bioactive compounds from medicinal plant origin lies in their affordability and minimized side effects. The Garcinia genus contains bioactive compounds, such as xanthones, benzophenones, triterpenes, biflavonoids, and benzoquinones. Purpose: The study aimed at investigating an active compound that can inhibit cancer cell growth and proteins that contribute to cancer cell growth, such as Caspase-9, TNF-α, ER-α, and HER-2. Methods: This study is divided into three steps. The first step is the isolation of the active compound from G. cymosa. The second step is an assessment of cytotoxic activity against MCF-7 cell by using MTT assay, and the last one is an investigation of the molecular mechanism of an active compound against Caspase-9, TNF-α, ER-α, and HER-2 by using in silico studies utilizing various programs, such as PyRx 0.8, PYMOL, and Discovery Studio. Results: Morelloflavone from G. cymosa stem barks has exhibited anticancer activity (55.84 μg/mL) eight times lower than doxorubicin (6.99 μg/mL), but it can block the activity of Caspase-9, TNF-α, ER- α, and HER-2. The binding affinity of morelloflavone is the strongest of all ligands. Conclusion: The natural flavonoid, morelloflavone, may be a new lead candidate for anticancer agent inhibiting action mechanism of Caspase-9, TNF-α, ER-α, and HER-2, respectively.

Design of nanoemulgel using Argania spinosa microfibrillated cellulose and natural emulsifiers foreseeing melanogenesis enhancement

Nanotechnology is a route of choice that improves administration and efficacy of bioactive compounds. In this study, nanoemulgels were prepared using microfibrillated cellulose from Argania spinosa shell (AS-MFC) and Argan shell (ASE) or Argan press cake extracts (APC) as natural emulsifiers. Oil-in-water (O/W) nanoemulsions were prepared using different natural emulsifiers or synthetic emulsifiers and presented a nano size (d3,2 < 140 nm). Following that, the nanoemulsions were incorporated within AS-MFC matrix and rheological properties confirmed a shear thinning behavior. Confocal micrographs of nanoemulgels confirmed the dispersion of nanoemulsions in the AS-MFC network without affecting the nanoemulsions stability. Finally, in vitro bioassay on B16F10 using ASE or APC nanoemulsions was conducted. This study confirmed cell permeation in B16F10 cells of formulated nanoemulsions and the upregulation of melanin content up to 30% more that the untreated cells. This study designed novel MFC nanoemulgel with high potential application in healthcare and cosmetic field.

Efficacy of bioactive compounds and their association with different cowpea cultivars against their major stored pest.

Stored grain insects are controlled with fumigant insecticides which can select resistant insect populations and cause environmental and applicator contamination. Thus, resistant cultivars and chemical constituents of essential oils are an alternative to the almost exclusive use of these insecticides. The effects of the combination of cowpea cultivars Vigna unguiculata (L.) Walp. with chemical constituents of essential oils against Callosobruchus maculatus were determined. Four cowpea cultivars: BRS Tracuateua, BR 17 Gurgueia, Epace 10 and Sempre Verde (insect rearing) untreated were used in the experiments and combined with chemical constituents of essential oil: eugenol, geraniol and trans-anethole. The biological parameters observed were: total egg number and eggs per grain, egg viability (%), insects emerged and insects per grain, immature stage viability (%), instantaneous rate of growth (ri), insect dry weight (mg), grain weight loss (%) and egg-adult period. When comparing all biological parameters, the cultivars BRS Tracuateua and BR 17 Gurgueia were harmful to C. maculatus. In the toxicity tests, the results showed that LC30 and LC50 of the chemical constituents ranged from 54.77 to 103.48 ppm and 60.99 to 125.18 ppm, respectively. In most of the biological parameters, LC50 had adverse effects significantly higher than LC30 and BR 17 Gurgueia treated were harmful to C. maculatus. Overall, the findings showed that BR 17 Gurgueia combined with eugenol and geraniol more significantly affected the biological parameters of C. maculatus than when associated with trans-anethole, reducing egg number, insects emerged and egg viability. © 2020 Society of Chemical Industry.

Characterization of the interaction of diosgenin with human serum albumin and α1-acid glycoprotein using biophysical and bioinformatic tools

Diosgenin (DIO), a steroidal sapogenin with high therapeutic potential, has been shown to exhibit a myriad of pharmacologically significant properties and is commonly used as a template for synthesizing steroidal drugs. The efficacy of bioactive compounds as a potential drug depends mainly upon their interaction with proteins in the circulatory system. Therefore, the interaction of DIO with the major carrier proteins in humans, i.e. human serum albumin (HSA) and α 1 -acid glycoprotein (AAG), was characterized using multispectroscopic and molecular docking techniques. Analysis of fluorescence enhancement data showed intermediate binding affinity for both DIO–HSA and DIO–AAG interactions. Circular dichroism spectral results revealed minimal conformational alterations in HSA upon DIO binding, but the effect on AAG was more significant. Competitive ligand displacement results suggested that DIO does not bind strongly to the main drug binding sites of HSA. However, DIO was found to favor binding to subdomain IB of HSA based on molecular docking data. For AAG, the binding location of DIO was determined for the two variants of AAG (A and F1*S variants) using molecular docking. For variant A, the binding site was situated in lobes I and II of the central binding pocket of the protein, while in variant F1*S, DIO was docked to a cleft on the protein surface. Hydrophobic interactions and van der Waals forces were mainly responsible for complexation between DIO and both proteins. Additionally, there was involvement of hydrogen bonding between DIO and both variants of AAG, but not between DIO and HSA. • AAG binds to DIO with slightly stronger affinity than HSA. • Hydrophobic forces are mainly responsible for DIO binding to both proteins. • DIO binds to HSA at subdomain IB. • DIO binds to variant F1*S of AAG at a cleft at the surface. • DIO binds to variant A of AAG at the central cavity.

Breast Cancer Resistance Protein and Multidrug Resistance Protein 2 Determine the Disposition of Esculetin-7-O-Glucuronide and 4-Methylesculetin-7-O-Glucuronide.

Esculetin (ET)-7-O-glucuronide (ET-G) and 4-methylesculetin (4-ME)-7-O-glucuronide (4-ME-G) are the main glucuronide of ET and 4-ME, respectively. The disposition mediated by efflux transporters for glucuronide has significant influence on the pharmacokinetic profile and efficacy of bioactive compounds. In the current study, transporter gene knockout mice and Caco-2 cells were used to explore the effects of breast cancer resistance protein (BCRP) and multidrug resistance-associated protein 2 (MRP2) on the disposition of ET-G and 4-ME-G. After oral or i.v. administration of ET and 4-ME, the area under the plasma concentration-time curve from time 0 to the last data point or infinity values of ET, 4-ME, and their glucuronides (ET-G and 4-ME-G) were remarkably and significantly increased in most Bcrp1-/- and Mrp2-/- mice compared with those in wild-type FVB mice (P < 0.05). These results were accompanied with a significant increase of maximum plasma concentration values (P < 0.05). In Caco-2 monolayers, the efflux and clearance rates of ET-G and 4-ME-G were markedly reduced by the BCRP inhibitor Ko143 and MRP2 inhibitor MK571 on the apical side (P < 0.05). In an intestinal perfusion study, the excretion of ET-G was significantly decreased in perfusate and increased in plasma in Bcrp1-/- mice compared with those in wild-type FVB mice (P < 0.05). The 4-ME-G concentration was also decreased in the bile in transporter gene knockout mice. ET and 4-ME showed good permeability in both Caco-2 monolayers [apparent permeability (Papp ) ≥ 0.59 × 10-5 cm/s] and duodenum (Papp ≥ 1.81). In conclusion, BCRP and MRP2 are involved in excreting ET-G and 4-ME-G. ET and 4-ME are most likely absorbed via passive diffusion in the intestines.

Radical Scavenging and Antiproliferative Effects of Cordycepin-Rich Ethanol Extract from Brown Rice-Cultivated Cordyceps militaris (Ascomycetes) Mycelium on Breast Cancer Cell Lines.

The yield and efficacy of bioactive compounds from Cordyceps militaris fruiting bodies and its fermented grains usually vary with the strainused. In this study, we compared the antiproliferative, apoptotic, and antioxidative properties of ethanolic extracts of fruiting bodies and solid-stated fermented rice (FRE) from two wild-type strains of C. militaris applied to human breast cancer cell lines. We observed that FRE of the Zhangzhou strain (FRE-Z) produced a high level of cordycepin and exhibited comprehensive in vitro antioxidant activity against the oxidation of 2,2-diphenyl-1-picrylhydrazyl, superoxide, and hydroxyl radicals and low-density lipoprotein. Only FRE-Z exhibited dose-dependent inhibition of cell proliferation in MCF-7 (0.7 mg/mL) and MDA-MB-231 cells (1 mg/mL) after culturing for 24 h. The antiproliferative effects of FRE-Z were associated with an early stage of apoptosis induction at 4 h of treatment with 0.5 mg/mL FRE-Z in MCF-7 cells. The antiproliferative effect was determined to occur through p53 activation but not through the release of mitochondrial apoptosis-inducing factor or caspase-9 activation for an initial culture period of 16 h. In addition to a transient increase in cellular antioxidant enzyme, Cu/Zn superoxide dismutase was identified in MCF-7 cells after 2 h of treatment with FRE-Z. Therefore, FRE-Z, which exhibits various dose- and exposure time-dependent activities, has potential application in breast cancer chemoprevention.

Efficacy of bioactive compounds from Curcuma longa L. against mosquito larvae

AbstractTo identify larvicidal compounds from the ethanolic extracts of Curcuma longa root, the active compounds were isolated using activity‐guided fractionation with column chromatography and identified based on nuclear magnetic resonance (NMR) and mass spectrometry (MS) data. The dipping method was used to determine the larvicidal activities of each compound against 4th‐instar larvae of Culex pipiens pallens. Two compounds were isolated and identified, ar‐turmerone and 8‐hydroxyl‐ar‐turmerone. The two compounds exhibited larvicidal activities against the 4th‐instar larvae of C. pipiens pallens after 24 hr of treatment with LC50 values of 138.86 and 257.68 ppm, respectively. The larvicidal activities of ar‐turmerone and 8‐hydroxyl‐ar‐turmerone against C. pipiens pallens are reported herein for the first time. The elucidation of the structure of these phytochemicals and their insecticidal activities are important for assessing the potential of this plant as a botanical insecticide.

Production of novel vitamin D3 loaded lipid nanocapsules for milk fortification

ABSTRACTLipid nanoparticles are carriers to improve stability, solubility, and efficacy of bioactive compounds. In this paper, novel vitamin D3 loaded lipid nanocapsules (LNC) were produced by phase inversion method. The produced nanocapsules were characterised by particle size, polydispersity index, zeta potential, encapsulation efficiency, and encapsulation load. LNC showed sizes in the range of 31.43 to 36.66 nm. Optimum LNC formulation was selected for further analysis (such as morphological study, analysis of chemical structure, release study, and sensory evaluation). Transmission electron microscopy revealed that particles had approximately spherical shape. The Fourier transform infrared spectra indicated that no adverse reactions occurred between vitamin D3 and lipid nanocapsules. About 9.6% of vitamin released in gastric simulated solution (pH: 1.2), which indicated that LNC can protect vitamin against acidic conditions. Sensory evaluation revealed the potential application of produced vitamin D3 loaded LNC for development of fortified milk.

Efficacy of Bioactive Compounds of Sponges to Prevent Biofilm Formation on Medical Implants

Bacterial biofilms are surface-attached communities of microorganisms that are protected by an extracellular matrix of biomolecules. In the biofilm state, bacteria are significantly more resistant to external assault, including attack by antibiotics. In their native environment, bacterial biofilms underpin costly biofouling that wreaks havoc on shipping, utilities, and offshore industry. Within a host environment, they are insensitive to antiseptics and basic host immune responses. It is estimated that up to 80% of all microbial infections are biofilm-based. Biofilm infections of indwelling medical devices are of particular concern, since once the device is colonized, infection is almost impossible to eliminate. Importantly, we discuss several sets of compounds derived from marine sponges that we are developing in our labs to address the persistent biofilm problem. Marine bioactive compound synthesis of natural products and their analogues-including our marine sponge-derived compounds and initial adjuvant activity and toxicological screening of our novel anti-biofilm compounds.

Efficacy of bioactive compounds from extra virgin olive oil to modulate atherosclerosis development

As olive oil is the main source of calories in the Mediterranean diet, a great deal of research has been devoted to characterizing its role in atherosclerosis. Virgin olive oil is an oily matrix that contains hydrocarbons, mainly squalene; triterpenes such as uvaol, erythrodiol, oleanolic, and maslinic acid; phytosterols; and a wide range of phenolic compounds comprising simple phenols, flavonoids, secoiridoids, and lignans. In this review, we analyze the studies dealing with atherosclerosis and olive oil in several species. A protective role of virgin olive oil against atherosclerosis has been shown in ApoE-deficient mice and hamsters. In the former animal, sex, dose, and dietary cholesterol are modulators of the outcome. Contradictory findings have been reported for rabbits, a circumstance that could be due to the profusion of experimental designs, differing in terms of doses and animal strains, as well as sources of olive oils. This role has yet to be fully validated in humans. Minor components of olive oil have been shown to be involved in atherosclerosis protection. Nevertheless, evidence of the potential of isolated compounds or the right combination of them to achieve the antiatherosclerotic effect of virgin olive oil is inconclusive and will undoubtedly require further experimental support.

Efficacy of bioactive compounds from Curcuma aromatica against mosquito larvae

With the development of resistance to conventionally used synthetic insecticides, vector management has become acutely problematic. Hence more attention has been focused on botanicals. Therefore our present study was aimed to evaluate the efficacy of extracts from rhizomes of Curcuma aromatica against the larvae of filariasis vector mosquitoes, Culex quinquefasciatus employing standard WHO procedure at Mysore. The soxhlet extraction was carried out using non-polar organic solvent, petroleum ether. The efficacy of petroleum ether extract seemed to be effective with LC 50 and LC 90 values of 11.42 and 18.00 ppm respectively. Bioassay-guided fractionation through flash chromatography lead to the isolation of two larvicidal compounds namely 9-oxoneoprocurcumenol and neoprocurcumenol. Between the two, 9-oxoneoprocurcumenol exerted significant toxicity ( P < 0.01) on mosquito larvae with LC 50 value of 5.81 ppm and LC 90 being 9.99 ppm compared to neoprocurcumenol with 13.69 and 23.92 ppm of LC 50 and LC 90 values respectively. From the results, C. aromatica could be considered as one of the powerful candidate to bring about useful botanicals so as to prevent the resurgence of mosquito vectors.