Phytocompounds and lipid-based drug delivery system for neurodegenerative diseases

Across the annals of time,organic molecules sourced from nature have found innumerable uses within the realms of healthcare,pharmaceuticals,and the study of living organisms.This abundant source of natural compounds has exhibited immense promise in the cure of diverse ailments,mainly neurodegenerative diseases owing to their minimum toxic and adverse effects.However,different challenges exist with phytocompounds from plants such as poor permeation,poor solubility(water/lipid),unsteadiness under extremely acidic pH conditions,and lack of targeting specificity.Furthermore,as a result of the existence of blood-brain barrier membrane and inconvenient pharmacokinetics characteristics of phytocompounds,their passage into the brain is constrained.In order to address this issue and augment the transportation of medications into the brain at a therapeutically effective level,it is imperative to formulate an innovative and pragmatic strategy.Many papers have shown that nanoformulations containing phytocompounds(resveratrol,quercetin,ferulic acid,curcumin,berberine,etc.)effectively improved many neurodegenerative diseases such as Parkinson’s,Alzheimer’s and Huntington’s diseases.This study provides an overview of phytocompounds that are used in nanosized lipid drug delivery systems.These systems are categorized according to lipid types and preparation techniques used in the formulation.Some studies regarding these systems and phytocompounds are also summarized.

Delineating the role of phytocompounds against anti-bacterial drug resistance–An update

Antibacterial resistance developed by bacteria due to the unlimited use of antibiotics has posed a challenge for human civilization.This kind of problem is not limited to India only,but it is a global concern.Nowadays,many treatments and medicines for bacterial diseases have been developed.However,they possess some drawbacks.Therefore,the alternative medicine has been used to target the drug resistant mechanisms and such medicines have less side effects which is becoming necessary.Natural products have traditionally or historically been of importance for the development of antibacterial agents and are also known to overcome bacterial drug resistance by directly targeting the drug resistance mechanisms in bacteria.In recent years,researchers have also focused on new drug discovery from plant-based research.They have looked on various phytocompounds as antibacterial agents.In the current review,we report various classes of secondary metabolites such as phenolic compounds,flavonoids,alkaloids,saponins,terpenes,quinones,and some essential oils that have been used as an antibacterial agent.In addition,we also discuss several mechanisms behind bacterial multi-drug resistance that are used during bacterial pathogenesis.

Emerging nanoformulation strategies for phytocompounds and applications from drug delivery to phototherapy to imaging

Over thousands of years,natural bioactive compounds derived from plants(bioactive phytocompounds,BPCs)have been used worldwide to address human health issues.Today,they are a significant resource for drug discovery in the development of modern medicines.Although many BPCs have promising biological activities,most of them cannot be effectively utilized in drugs for therapeutic applications because of their inherent limitations of low solubility,structural instability,short half-life,poor bioavailability,and non-specific distribution to organs.Researchers have utilized emerging nanoformulation(NF)technologies to overcome these limitations as they have demonstrated great potential to improve the solubility,stability,and pharmacokinetic and pharmacodynamic characteristics of BPCs.This review exemplifies NF strategies for resolving the issues associated with BPCs and summarizes recent advances in their preclinical and clinical applications for imaging and therapy.This review also highlights how innovative NF technologies play a leading role in next-generation BPC-based drug development for extended therapeutic applications.Finally,this review discusses the opportunities to take BPCs with meaningful clinical impact from bench to bedside and extend the patent life of BPC-based medicines with new formulations or application to new adjacent diseases beyond the primary drug indications.

Apple as a Source of Dietary Phytonutrients: Bioavailability and Evidence of Protective Effects against Human Cardiovascular Disease

The dietary consumption of fruit and vegetable is associated with a lower incidence of degenerative diseases such as cardiovascular disease. Most recent interest has focused on the bioactive phenolic compounds in vegetable products. All varieties of apple contain several antioxidants and polyphenols that possess many biological activities, such as antioxidant and anti-inflammation properties. The review describes the nutritional properties of apples and their derivatives, with a particular attention to polyphenol compounds. Moreover, the health benefits of apples and the potential molecular mechanisms against cardiovascular disease are reviewed.

Novel ligand-based docking; molecular dynamic simulations;and absorption, distribution, metabolism, and excretion approach to analyzing potential acetylcholinesterase inhibitors for Alzheimer's disease

Acetylcholinesterase(AChE) plays an important role in Alzheimer's disease(AD). The excessive activity of AChE causes various neuronal problems, particularly dementia and neuronal cell deaths. Generally, antiAChE drugs induce some serious neuronal side effects in humans. Therefore, this study sought to identify alternative drug molecules from natural products with fewer side effects than those of conventional drugs for treating AD. To achieve this, we developed computational methods for predicting drug and target binding affinities using the Schrodinger suite. The target and ligand molecules were retrieved from established databases. The target enzyme has 539 amino acid residues in its sequence alignment. Ligand molecules of 20 bioactive molecules were obtained from different kinds of plants, after which we performed critical analyses such as molecular docking; molecular dynamic(MD) simulations; and absorption, distribution, metabolism, and excretion(ADME) analysis. In the docking studies, the natural compound rutin showed a superior docking score of à 12.335 with a good binding energy value ofà73.313 kcal/mol. Based on these findings, rutin and the target complex was used to perform MD simulations to analyze rutin stability at 30 ns. In conclusion, our study demonstrates that rutin is a superior drug candidate for AD. Therefore, we propose that this molecule is worth further investigation using in vitro studies.

Acknowledging the use of botanicals to treat diabetic foot ulcer during the 21st century:A systematic review

BACKGROUND Diabetic foot ulcer(DFU) is a serious health issue of diabetes mellitus that affects innumerable people worldwide. Management and treatment of this complication are challenging, especially for those whose immune system is weak.AIM To discuss the plants and their parts used to heal DFU, along with the mode of their administration in diabetic patients.METHODS The original articles on “the plants for the treatment of DFU” studied in clinical cases only were obtained from various bibliographic databases using different keywords.RESULTS The search resulted in 22 clinical cases records with 20 medicinal plants belonging to 17 families on 1553 subjects. The fruits and leaves were the most preferentially used parts for DFU treatment, regardless of whether they were being administered orally or applied topically. Of the 20 medicinal plants, 19 reported their effectiveness in increasing angiogenesis, epithelialization, and granulation, thus hastening the wound-healing process. The efficacy of these botanicals might be attributed to their major bioactive compounds, such as actinidin and ascorbic acid(in Actinidia deliciosa), 7-O-(β-D-glucopyranosyl)-galactin(in Ageratina pichinchensis), omega-3-fatty acid(in Linum usitatissimum), isoquercetin(in Melilotus officinalis), anthocyanins(in Myrtus communis), and plantamajoside(in Plantago major).CONCLUSION The validation of mechanisms of action underlying these phytocompounds contributing to the management of DFU can aid in our better understanding of creating efficient treatment options for DFU and its associated problems.

Analysis of phytochemical profile of Terminalia arjuna bark extract with antioxidative and antimicrobial properties

Objective:To investigate phytochemical screening,antimicrobial activity and qualitative thin layer chromatographic separation of flavonoid components,antioxidant activity and total flavonoid compound of Terminalia arjuna.Methods:For phytochemical screening,some common and available standard tests were done.Antimicrobial bioassay was done through agar well diffusion method.Detection of antioxidant activity and flavonoid compounds were done through thin layer chromatography.Total antioxidant activity was measured by 2,2-diphenyl-1-picrylhydrazyl(DPPH)in colorimetric method.Aluminum chloride colorimetric method was used for total flavonoid determination.Results:Phytochemical screening showed the active compounds presence in high concentration,such as phytosterol,lactones,flavonoids,phenolic compounds and tannins and glycosides.The anlimicrobial activity of extract showed that greater inhibition zone against Gram negative bacteria than Gram positive bacteria.This methanolic extract showed a promising antioxidant activity,as absorption of DPPH redicles decreased in DPPH free radical scavenging assay.Flavonoids components having antioxidant property present in the methanol extract at a level of199.00 mg quercetin equivalent/g of dried methanol extract in colorimetric method.Conclusions:The Terminalia arjuna bark extract revealed the presence of bio-active constituents which are known to exhibit medicinal as well as physiological activities.

Camellia sinensis mediated synthesis and characterization of nanoparticles and applications to control Gram-negative ESBL producing antibiotic resistant bacterial pathogens

Camellia sinensis(tea),has numerous pharmacotherapeutic benefits.The majority of its phytocompounds exhibit antibacterial properties,which are effective in treating a range of bacterial diseases,including Urinary Tract Infections(UTI).In-silico research examined the ability of the major C.sinensis phytocompounds to inhibit bacterial enzymes.Molecular docking was performed to explore the efficiency of tea phytoconstituents by evaluating their binding affinity and existence of different interactions between the bacterial proteins/enzymes and the tea phytoconstituents,to inhibit key enzymes associated with bacterial infections.Camellia sinensis silver nanoparticles(CsAgNps)were synthesized by using the biogenesis method,which comes under the bottom-up approach.The characterization results confirmed the charge,size and shape of the synthesized CsAgNps.Characterization data revealed the existence of functional groups which are responsible for the stability and effectivity of the nanoparticles.Toxicity studies were carried out to determine its safety at various dosage levels.In in vitro condition,CsAgNps synthesized from fresh tea leaves extract showed antibacterial properties even against antibiotic-resistant bacteria(ARB).In-vitro studies of this biosynthesized CsAgNps confirmed the bacteriostatic and bactericidal properties by using agar well diffusion,MIC and MBC methods at various concentrations of the synthesized CsAgNps.This proved that CsAgNps can inhibit bacterial growth against these three Gram-negative extended spectrum beta lactamase(ESBL)producers and hence it can serve as an alternative to antibiotics.