Recent Advances in Biomedical Applications of Mannans and Xylans.

Plant-based phytochemicals, including flavonoids, alkaloids, tannins, saponins, and other metabolites, have attracted considerable attention due to their central role in synthesizing nanomaterials with various biomedical applications. Hemicelluloses are the second most abundant among naturally occurring heteropolymers, accounting for one-third of all plant constituents. In particular, xylans, mannans, and arabinoxylans are structured polysaccharides derived from hemicellulose. Mannans and xylans are characterized by their linear configuration of ß-1,4-linked mannose and xylose units, respectively. At the same time, arabinoxylan is a copolymer of arabinose and xylose found predominantly in secondary cell walls of seeds, dicotyledons, grasses, and cereal tissues. Their widespread use in tissue engineering, drug delivery, and gene delivery is based on their properties, such as cell adhesiveness, cost-effectiveness, high biocompatibility, biodegradability, and low immunogenicity. Moreover, it can be easily functionalized, which expands their potential applications and provides them with structural diversity. This review comprehensively addresses recent advances in the field of biomedical applications. It explores the potential prospects for exploiting the capabilities of mannans and xylans in drug delivery, gene delivery, and tissue engineering.

Novel vesicular bilosomal delivery systems for dermal/transdermal applications.

The application of therapeutically active molecules through the dermal/transdermal route into the skin has evolved as an attractive formulation strategy in comparison to oral delivery systems for the treatment of various disease conditions. However, the delivery of drugs across the skin is limited due to poor permeability. Dermal/transdermal delivery is associated with ease of accessibility, enhanced safety, better patient compliance, and reduced variability in plasma drug concentrations. It has the ability to bypass the first-pass metabolism, which ultimately results in steady and sustained drug levels in the systemic circulation. Vesicular drug delivery systems, including bilosomes, have gained significant interest due to their colloidal nature, improved drug solubility, absorption, and bioavailability with prolonged circulation time for a large number of new drug molecules. Bilosomes are novel lipid vesicular nanocarriers comprising bile salts, such as deoxycholic acid, sodium cholate, deoxycholate, taurocholate, glycocholate or sorbitan tristearate. These bilosomes are associated with high flexibility, deformability, and elasticity attributed to their bile acid component. These carriers are advantageous in terms of improved skin permeation, increased dermal and epidermal drug concentration, and enhanced local action with reduced systemic absorption of the drug, resulting in reduced side effects. The present article provides a comprehensive overview of the biopharmaceutical aspects of dermal/transdermal bilosome delivery systems, their composition, formulation techniques, characterization methods, and applications.

Ivermectin: A Critical Review on Characteristics, Properties, and Analytical Methods.

BACKGROUND: Ivermectin is one of the first, safe, broad-spectrum avermectin class of antiparasitic agent, widely used to control parasitic growth in livestock. Ivermectin being highly lipophilic accumulates in fat tissues, causing its long-term existence in the body. Accordingly, ivermectin residues are observed in various animal products such as milk and meat presenting several health hazards. Therefore, monitoring of ivermectin residue levels in the various food products of animal origin is greatly important to ensure the safety of consumers. This review could be of significant importance in the area of ivermectin analytical method development studies. OBJECTIVE: In this context, objective of the present work is to provide a critical review of analytical methods in the literature for detection and quantification of ivermectin in pharmaceutical formulations, and biological materials including animal tissues. METHODS: The data from analysis of accessible literature within the time span of 1980 to 2022 was selected. RESULTS: Several analytical methods based on HPLC-fluorescence detector, UV-diode array detector, HPLC-tandem mass spectrometry (MS/MS), ultra-performance liquid chromatography-MS/MS, and capillary electrophoresis techniques have been utilized for the simultaneous determination of ivermectin singly or in the presence of other drugs with realistic retention times. Several derivatization strategies were used to introduce a fluorophore followed by extraction into organic phase to remove the matrix interferences and enhance the sensitivity by pre-concentration. Methods such as HPLC linked to MS/MS were developed to lower the detection limit and quantification limit, with no requirement for derivatization. CONCLUSION: More simple, selective, fast, sensitive, and green chemistry-oriented methods for ivermectin analysis need to be developed. Novel analytical devices based on pulsed electrochemical methods, voltammetry, and amperometry can be developed for real-time analysis of ivermectin, in addition to biosensors based on nanotechnology including quantum dots and nanoparticles, etc. HIGHLIGHTS: Various methods are described in the review including HPLC techniques with UV or visible spectrophotometric, fluorescence, and mass spectrometric detection, capillary electrophoresis, and immunological methods.

A Review on Recent Advances in Mannose-Functionalized Targeted Nanocarrier Delivery Systems in Cancer and Infective Therapeutics.

Unmodified nanocarriers used in the chemotherapy of cancers and various infectious diseases exhibit prolonged blood circulation time, prevent enzymatic degradation and increase chemical stability of encapsulated therapeutics. However, off-target effect and lack of specificity associated with unmodified nanoparticles (NPs) limit their applications in the health care system. Mannose (Man) receptors with significant overexpression on antigen-presenting cells and macrophages are among the most admired targets for cancer and anti-infective therapeutics. Therefore, development of Man functionalized nanocarriers targeting Man receptors, for target specific drug delivery in the chemotherapy have been extensively studied. Present review expounds diverse Man-conjugated NPs with their potential for targeted drug delivery, improved biodistribution profiles and localization. Additionally, the review gives detailed account of the interactions of mannosylated NPs with various biological systems and their characterization not discussed in earlier published reports is discussed.

Current Overview of Cyclodextrin Inclusion Complexes of Volatile Oils and their Constituents.

BACKGROUND: Volatile oils and their constituents have been considered major bioactive natural compounds due to their wide therapeutic and biological activities in pharmaceuticals in human healthcare. However, due to their poor solubility, their applications are limited. The inclusion complexation of volatile oils and their volatile constituents with cyclodextrins has emerged as a promising approach for the improvement of aqueous solubility, bioavailability, and stability. OBJECTIVE: The present review summarizes various research investigations highlighting the complexation of volatile oils and their constituents with cyclodextrins and their derivatives. Additionally, we present an overview of patents published between 1998-2021 to highlight the significance of including volatile oil in cyclodextrins. METHODS: The selection of articles for the current review was carried out by using keywords 'Cyclodextrin', 'Essential oil', 'Inclusion Complex', 'Encapsulation' and 'Essential oils/ volatile oils constituents' in certain specific databases, such as Elsevier (Science Direct), Pubmed Medical subject headings (MeSH) and Medline. RESULTS: A total of 199 studies published were included in the review. In vitro and in vivo studies revealed the efficacy of EOs and their VCs complexed with various types of CD compared to free forms. CONCLUSION: This review shows the impact of cyclodextrin complexation on the solubility, bioavailability, stability, and biological activities of volatile oils and their constituents.

miRNA and antisense oligonucleotide-based α-synuclein targeting as disease-modifying therapeutics in Parkinson's disease.

α-synuclein is the synaptic protein majorly involved in neuronal dysfunction and death and it is well known for the last two decades as a hallmark of Parkinson's disease. Alpha-synuclein is involved in neurodegeneration mediated through various neurotoxic pathways, majorly including autophagy or lysosomal dysregulation, mitochondrial disruption, synaptic dysfunction, and oxidative stress. Moreover, the alpha-synuclein aggregation has been associated with the development of several neurodegenerative conditions such as various forms of Parkinson's disease. The recent discovery in oligonucleotide chemistry has developed potential alpha-synuclein targeting molecules for the treatment of neurodegenerative diseases. The present review article focuses on recent advances in the applications of oligonucleotides acting via alpha-synuclein targeting mechanisms and their implication in combating Parkinson's disease. Moreover, the article emphasizes the potential of miRNAs, and antisense oligonucleotides and the challenges associated with their use in the therapeutical management of Parkinson's disease.

Antimicrobial Nanomaterials for Food Packaging.

Food packaging plays a key role in offering safe and quality food products to consumers by providing protection and extending shelf life. Food packaging is a multifaceted field based on food science and engineering, microbiology, and chemistry, all of which have contributed significantly to maintaining physicochemical attributes such as color, flavor, moisture content, and texture of foods and their raw materials, in addition to ensuring freedom from oxidation and microbial deterioration. Antimicrobial food packaging systems, in addition to their function as conventional food packaging, are designed to arrest microbial growth on food surfaces, thereby enhancing food stability and quality. Nanomaterials with unique physiochemical and antibacterial properties are widely explored in food packaging as preservatives and antimicrobials, to extend the shelf life of packed food products. Various nanomaterials that are used in food packaging include nanocomposites composing nanoparticles such as silver, copper, gold, titanium dioxide, magnesium oxide, zinc oxide, mesoporous silica and graphene-based inorganic nanoparticles; gelatin; alginate; cellulose; chitosan-based polymeric nanoparticles; lipid nanoparticles; nanoemulsion; nanoliposomes; nanosponges; and nanofibers. Antimicrobial nanomaterial-based packaging systems are fabricated to exhibit greater efficiency against microbial contaminants. Recently, smart food packaging systems indicating the presence of spoilage and pathogenic microorganisms have been investigated by various research groups. The present review summarizes recent updates on various nanomaterials used in the field of food packaging technology, with potential applications as antimicrobial, antioxidant equipped with technology conferring smart functions and mechanisms in food packaging.

Complexation of phytochemicals with cyclodextrins and their derivatives- an update.

Bioactive phytochemicals from natural source have gained tremendous interest over several decades due to their wide and diverse therapeutic activities playing key role as functional food supplements, pharmaceutical and nutraceutical products. Nevertheless, their application as therapeutically active moieties and formulation into novel drug delivery systems are hindered due to major drawbacks such as poor solubility, bioavailability and dissolution rate and instability contributing to reduction in bioactivity. These drawbacks can be effectively overcome by their complexation with different cyclodextrins. Present article discusses complexation of phytochemicals varying from flavonoids, phenolics, triterpenes, and tropolone with different natural and synthetic cyclodextrins. Moreover, the article summarizes complexation methods, complexation efficiency, stability, stability constants and enhancement in rate and extent of dissolution, bioavailability, solubility, in vivo and in vitro activities of reported complexed phytochemicals. Additionally, the article presents update of published patent details comprising of complexed phytochemicals of therapeutic significance. Thus, phytochemical cyclodextrin complexes have tremendous potential for transformation into drug delivery systems as substantiated by significant outcome of research findings.

Nanoparticles-Attractive Carriers of Antimicrobial Essential Oils.

Microbial pathogens are the most prevalent cause of chronic infections and fatalities around the world. Antimicrobial agents including antibiotics have been frequently utilized in the treatment of infections due to their exceptional outcomes. However, their widespread use has resulted in the emergence of multidrug-resistant strains of bacteria, fungi, viruses, and parasites. Furthermore, due to inherent resistance to antimicrobial drugs and the host defence system, the advent of new infectious diseases, chronic infections, and the occurrence of biofilms pose a tougher challenge to the current treatment line. Essential oils (EOs) and their biologically and structurally diverse constituents provide a distinctive, inexhaustible, and novel source of antibacterial, antiviral, antifungal, and antiparasitic agents. However, due to their volatile nature, chemical susceptibility, and poor solubility, their development as antimicrobials is limited. Nanoparticles composed of biodegradable polymeric and inorganic materials have been studied extensively to overcome these limitations. Nanoparticles are being investigated as nanocarriers for antimicrobial delivery, antimicrobial coatings for food products, implantable devices, and medicinal materials in dressings and packaging materials due to their intrinsic capacity to overcome microbial resistance. Essential oil-loaded nanoparticles may offer the potential benefits of synergism in antimicrobial activity, high loading capacity, increased solubility, decreased volatility, chemical stability, and enhancement of the bioavailability and shelf life of EOs and their constituents. This review focuses on the potentiation of the antimicrobial activity of essential oils and their constituents in nanoparticulate delivery systems for a wide range of applications, such as food preservation, packaging, and alternative treatments for infectious diseases.

Role of KSP Inhibitors as Anti-cancer Therapeutics: An Update.

Regardless of the growing discovery of anticancer treatments targeting cancer-specific pathways, cytotoxic therapy still maintained its abundant clinical significance because tumours harbor a greater population of actively dividing cells than normal tissues. Conventional anti-mitotic agents or microtubule poisons acting on the major mitotic spindle protein tubulin have been effectively used in clinical settings for cancer chemotherapy over the last three decades. However, the use of these drugs is associated with limited clinical utility due to serious side effects such as debilitating and dose-limiting peripheral neuropathy, myelosuppression, drug resistance, and allergic reactions. Therefore, research initiatives have been undertaken to develop novel microtubule motor proteins inhibitors that can potentially circumvent the limitations associated with conventional microtubule poisons. Kinesin spindle proteins (KSP) belonging to the kinesin-5 family play a crucial role during mitosis and unregulated cell proliferation. Evidence from preclinical studies and different phases of clinical trials have presented kinesin spindle protein as a promising target for cancer therapeutics. Kinesin spindle protein inhibitors causing mitosis disruption without interfering with microtubule dynamics in non-dividing cells offer a potential therapeutic alternative for the management of several major cancer types and are devoid of side effects associated with classical anti-mitotic drugs. This review summarizes recent data highlighting progress in the discovery of targeted KSP inhibitors and presents the development of scaffolds, structure-activity relationships, and outcomes of biological and enzyme inhibition studies. We reviewed the recent literature reports published over the last decade, using various electronic database searches such as PubMed, Embase, Medline, Web of Science, and Google Scholar. Clinical trial data till 2021 was retrieved from ClinicalTrial.gov. Major chemical classes developed as selective KSP inhibitors include dihydropyrimidines, ß-carbolines, carbazoles, benzimidazoles, fused aryl derivatives, pyrimidines, fused pyrimidines, quinazolines, quinolones, thiadiazolines, spiropyran, and azobenzenes. Drugs such as filanesib, litronesib, ispinesib have entered clinical trials; the most advanced phase explored is Phase II. KSP inhibitors have exhibited promising results; however, continued exploration is greatly required to establish the clinical potential of KSP inhibitors.

Fatty Acid Biosynthesis: An Updated Review on KAS Inhibitors.

Since the early twentieth century, with the isolation of penicillin and streptomycin in the 1940s, the modern era of anti-infective drug development has gained momentum. Due to the enormous success of early drug discovery, many infectious diseases were successfully prevented and eradicated. However, this initial hope was wrongheaded, and pathogens evolved as a significant threat to human health. Drug resistance develops as a result of natural selection's relentless pressure, necessitating the identification of new drug targets and the creation of chemotherapeutics that bypass existing drug resistance mechanisms. Fatty acid biosynthesis (FAS) is a crucial metabolic mechanism for bacteria during their growth and development. Several crucial enzymes involved in this biosynthetic pathway have been identified as potential targets for new antibacterial agents. In Escherichia coli (E. coli), this pathway has been extensively investigated. The present review focuses on progress in the development of Kas A, Kas B, and Fab H inhibitors as mono-therapeutic antibiotics.

A Status Update on Pharmaceutical Analytical Methods of Aminoglycoside Antibiotic: Amikacin.

Amikacin (AMK) is one of the commonly used aminoglycoside antibiotics, introduced for clinical use in patients suffering from bacterial infections especially life-threatening gram-negative infections. Due to lack of chromophore in the molecule, the detection of AMK during analysis is a challenge. Thus, pre and post-column derivatization techniques are generally used for AMK estimation. This review focuses on different analytical methods used for detection and quantification of AMK in pure or fixed dose combination pharmaceutical formulations and biological samples. Various reported methods described in the literature include high-performance liquid chromatography techniques, pulsed electrochemical detection techniques, Chemiluminescence techniques, Capillary electrophoresis and immunological methods. High-performance-liquid-chromatography based methods with UV/Vis spectrophotometric, fluorescence and mass spectrometric detection are the most prevailing methods employed for the analysis of AMK. This review could be of significant importance in the area of future AMK analytical method development studies.

An insight into cytotoxic activity of flavonoids and sesquiterpenoids from selected plants of Asteraceae species.

Cancer continues to be a disease that is difficult to cure and the current therapeutic regimen is associated with severe side effects and the issue of emerging drug resistance. According to the World Health Organization fact sheet 2017, cancer is the second major cause of morbidity and death and a 70% rise in new cases is expected over the next 20 years. The quest for new anticancer chemical entities is a thrust area identified by many government agencies and industry research and development groups. Nature-derived entities have played a very important role in therapeutics especially cancer Asteraceae is a large family consisting of around 1700 genera and more than 24,000 species. Several genera belonging to this family have ethnopharmacological uses such as cytotoxicity, antidiabetic, hepatoprotective and antioxidant. This review highlights the cytotoxic potential of structurally novel flavonoids and sesquiterpenes isolated from some selected species of Asteraceae plants native to Asia, Europe, parts of Africa and America. The existing literature suggests that sesquiterpenes and flavonoids from various species of Asteraceae represent a viable class of secondary metabolites with strong cytotoxic potential. These have demonstrated potent activity in cell cycle arrest, inhibition of neoangiogenesis and induction of apoptosis. The sesquiterpenoids exhibiting potent cytotoxic activity were found to contain an α- methylene-butyrolactone conjugated with an exomethylene group and the flavonoids obtained from various plant species of Blumea suggest that a dihydroxy ring system present in structure is essential for activity. Most of the published literature contains in vitro data of extracts/secondary metabolites with very few in vivo studies. Additionally, there is dearth of knowledge on mechanisms of cytotoxic activity and molecular targets impacted by the active secondary metabolites. This review hopes to fuel interest in researchers to take up detailed investigations on these scaffolds that could contribute significantly as potential leads in anticancer drug development.

Role of natural products in alleviation of rheumatoid arthritis-A review.

Rheumatoid arthritis (RHA) is one of the most prevalent complex, chronic, inflammatory diseases, manifested by elevated oxidative stress and inflammatory biomarkers. Prolonged administration of NSAIDs, steroids, and DMARDs, used in the treatment of RHA, is associated with deleterious side effects. This necessitates the urge of new and safe approaches for RHA management, based on the complementary and alternative system of medicine. Documented evidences have suggested that supplementation with nutritional, dietary, and herbal components; can play a crucial role as an adjuvant, in the alleviation of the RHA symptoms, through their influence on the pathological inflammatory processes. Dietary phenolic compounds, flavonoids, carotenoids, and alkaloids with their ability to modulate prooxidant and pro-inflammatory pathways, have been effective in delaying the arthritic disease progression. Moreover, in scientific explorations, herbs containing phenolic compounds, alkaloids, carotenoids flavonoids, spices such as ginger, turmeric, Ayurvedic formulations, different diets such as Mediterranean diet, vegan diet, beverages, and oils such as sesame oil, rice bran oil, vitamins, and probiotics are proven to modulate the action of inflammatory molecules, involved in RHA pathology. Subsequently, the purpose of this review article is to summarize various in vitro, in vivo, and clinical studies in RHA, which have documented remarkable insights into the anti-inflammatory, antioxidant, analgesic, and immunomodulatory, bone erosion preventing properties of dietary, nutritional, and herbal components with the focus on their molecular level mechanisms involved in RHA. Even though major findings were derived from in vitro studies, several in vivo and clinical studies have established the use of diet, herbal, and nutritional management in RHA treatment. PRACTICAL APPLICATIONS: Thickening of the synovial membrane, bone erosion, and cartilage destruction is known to trigger rheumatoid arthritis causing inflammation and pain in bone joints. Continuous intake of NSAIDs, steroids, and DMARD therapy are associated with detrimental side effects. These side effects can be overcome by the use of dietary, nutritional, and herbal interventions based on the complementary and alternative therapy. This concept portrays the food components and other natural components having the potential to promote health, improve general well-being, and reduce the risk of RHA.

Current insights on clinical efficacy of roflumilast for treatment of COPD, asthma and ACOS.

Phosphodiesterase-4 inhibitors (PDE4) are of great interest for the treatment of airway inflammatory diseases due to its broad anti-inflammatory effects. Roflumilast is a selective PDE4 inhibitor that inhibits pulmonary and systemic inflammation and rallies symptoms in airway diseases. Asthma and COPD are common chronic airway inflammatory diseases having incompletely illustrious pathophysiology and clinical manifestations. Recently, the condition called Asthma- COPD Overlap (ACO) has been evolved having the overlapping symptoms of both diseases. The newly discovered PDE4 inhibitor, roflumilast has exposed its potential in the treatment of Asthma, COPD and ACOS. Its mechanism of action in airway inflammatory diseases are said to be exerts by elevating intracellular cAMP and shows its anti-inflammatory action. Roflumilast, a promising therapeutic approach in inflammatory airway diseases, has many significant outcomes. In this review, we have provided various promising clinical evidences of roflumilast in COPD and asthma. However, there is no published clinical evidence to date for the role of roflumilast in ACOS. Nevertheless, there are therapeutic mechanisms that provide a reference for clinical application for ACOS.

A Critical Review on Anticancer Mechanisms of Natural Flavonoid Puerarin.

Cancer is one of the prominent global causes of death and the foremost worldwide health concern. Despite unprecedented progress in cancer chemoprevention, a vast number of cancers, however, remain an undefeatable challenge for treatment modalities. Immense therapeutic activities of puerarin contribute to its use in various health disorders. In this review, we explored the potential molecular mechanisms and targets of puerarin, proving its potential as a novel anticancer agent, for future cancer therapy and chemoprevention. Several mechanisms account for anticancer activity of puerarin which includes downregulation of NF-kB signalling pathway, mTOR signalling pathway, PI3K and BCl-2 proteins and upregulation of miR-16, caspase proteins, c- Jun N terminal kinase and extracellular signal-regulated kinase 1/2. These alterations result in inhibition of cancer cell proliferation and/or induction of apoptosis. Understanding the molecular mechanisms involved in chemotherapy and chemoprevention could aid in the more pronounced exploration of puerarin in effective cancer treatment.

Current overview on the clinical update of Bcl-2 anti-apoptotic inhibitors for cancer therapy.

Apoptosis is one of the major mechanisms exhibited in response to cell death and induction of apoptosis in tumour cells signifies a potential target for cancer therapy. Bcl-2 family proteins play a key role in regulation of the apoptotic pathway. Bcl-2 overexpression is commonly associated with various cancers including breast cancer, prostate cancer, B-cell lymphomas and colorectal adenocarcinomas etc. Thus, Bcl-2 is a novel anti-cancer target attracting medicinal chemists across the globe. Research investigations underlying Bcl-2 target have resulted in the generation of small molecule inhibitors, named as 'BH3-mimetics' (Bcl-2 homology 3 mimetics). These drugs display binding to pro-survival Bcl-2 proteins resulting in actuation of apoptosis of cancer cells. The first BH3 mimetics discovered as an outcome of structure-based drug design and Nuclear Magnetic Resonance (NMR)-based screening was ABT-263, an N-acylsulfonamide analogue. Thrombocytopenia a major dose-limiting toxicity, associated with ABT-263 had provoked the invention of a highly selective Bcl-2 inhibitor venetoclax. Several Bcl-2 inhibitors as small molecules are under clinical development and the results indicated that these molecules alone or in combination could be of potential application in cancer therapy. This review summarizes an up to date knowledge of the available small molecule inhibitors, their discovery, synthesis, current clinical and pre-clinical status.

Design and Development of Novel 2-(Morpholinyl)-N-substituted Phenylquinazolin-4-amines as Selective COX-II Inhibitor.

BACKGROUND: A novel series of 2-(Morpholin-4-yl)-N-phenylquinazolin-4- amine derivatives were synthesized and confirmed with spectral and elemental techniques. METHODS: The compounds were tested for analgesic and anti-inflammatory activity by various pain models in rodents whereas the selectivity towards COX-2 receptor is determined by in vitro assay. RESULTS: Screening results of compounds exhibited comparable biological activity with that of standard compound Indomethacin used for study. Compound 5d was found to be significantly potent with respect to its anti-inflammatory and analgesic activity with substantial COX-II selectivity. CONCLUSION: In silico analysis by molecular docking and 3D-QSAR studies justifies activity profile of compound 5d, suggesting that it may have potential for further evaluation and development as lead molecule for therapy in pain management.

Bone Health and Natural Products- An Insight.

Bone metabolism involves a complex balance between matrix deposition, mineralization, and resorption. Numerous evidences have revealed that dietary components and phytoconstituents can influence these processes, through inhibition of bone resorption, thus exhibiting beneficial effects on the skeleton. Various traditional herbal formulae in ayurvedic and Chinese medicine have shown demonstrable benefits in pharmacological models of osteoporosis. The present review discusses normal bone metabolism and disorders caused by bone disruption, with particular reference to osteoporosis and current therapeutic treatment. Furthermore the effects of constituents from natural products on bone tissue are explained, with relevant evidences of efficacy in various experimental models.

Mycobacterial siderophore: A review on chemistry and biology of siderophore and its potential as a target for tuberculosis.

Mycobacterium tuberculosis (MTB), the causative agent of tuberculosis is known to secrete low molecular mass compounds called siderophores especially under low iron conditions to chelate iron from host environment. Iron is essential for growth and other essential processes to sustain life of the bacterium in the host. Hence targeting siderophore is considered to be an alternative approach to prevent further virulence of bacterium into the host. This review article presents classification of siderophores, their role in transporting iron into the tubercular cell, biosynthesis of mycobactins, viability of siderophore as a therapeutic target and also focuses on overview on various approaches to target siderophore. The approaches encompass mutation effect on genes involved in siderophore recycling, synthetic as well as natural compounds that can inhibit further spread of bacterium by targeting siderophore.