Bioactive substances of cyanobacteria and microalgae: Sources, metabolism, and anticancer mechanism insights.

Cyanobacteria and microalgae contain various phytochemicals, including bioactive components in the form of secondary metabolites, namely flavonoids, phenolic acids, terpenoids, and tannins, with remarkable anticancer effects. This review highlights the recent advances in bioactive compounds, with potential anticancer activity, produced by cyanobacteria and microalgae. Previous in vitro investigations showed that many of these bioactive compounds exhibit potent effects against different human cancer types, such as leukemia and breast cancers. Multiple mechanisms implicated in the antitumor effect of these compounds were elucidated, including their ability to target cellular, subcellular, and molecular checkpoints linked to cancer development and promotion. Recent findings have highlighted various mechanisms of action of bioactive compounds produced by cyanobacteria and microalgae, including induction of autophagy and apoptosis, inhibition of telomerase and protein kinases, as well as modulation of epigenetic modifications. In vivo investigations have demonstrated a potent anti-angiogenesis effect on solid tumors, as well as a reduction in tumor volume. Some of these compounds were examined in clinical investigations for certain types of cancers, making them potent candidates/scaffolds for antitumor drug development.

Draft Genome Sequences of Four Plant Growth-Promoting Rhizobacteria Isolated from Saffron (Crocus sativus L.) Rhizosphere in Morocco.

We report the draft genome sequences of plant growth-promoting Rahnella perminowiae strain S11P1, Variovorax sp. strain S12S4, and Pseudomonas sp. strains S11A4 and S11P7, which were isolated from saffron (Crocus sativus L.) rhizosphere. Several genes were predicted to be involved in auxin production, phosphate solubilization, and other specialized functions in plant growth and defense.

Mechanisms, Anti-Quorum-Sensing Actions, and Clinical Trials of Medicinal Plant Bioactive Compounds against Bacteria: A Comprehensive Review.

Bacterial strains have developed an ability to resist antibiotics via numerous mechanisms. Recently, researchers conducted several studies to identify natural bioactive compounds, particularly secondary metabolites of medicinal plants, such as terpenoids, flavonoids, and phenolic acids, as antibacterial agents. These molecules exert several mechanisms of action at different structural, cellular, and molecular levels, which could make them candidates or lead compounds for developing natural antibiotics. Research findings revealed that these bioactive compounds can inhibit the synthesis of DNA and proteins, block oxidative respiration, increase membrane permeability, and decrease membrane integrity. Furthermore, recent investigations showed that some bacterial strains resist these different mechanisms of antibacterial agents. Researchers demonstrated that this resistance to antibiotics is linked to a microbial cell-to-cell communication system called quorum sensing (QS). Consequently, inhibition of QS or quorum quenching is a promising strategy to not only overcome the resistance problems but also to treat infections. In this respect, various bioactive molecules, including terpenoids, flavonoids, and phenolic acids, exhibit numerous anti-QS mechanisms via the inhibition of auto-inducer releases, sequestration of QS-mediated molecules, and deregulation of QS gene expression. However, clinical applications of these molecules have not been fully covered, which limits their use against infectious diseases. Accordingly, the aim of the present work was to discuss the role of the QS system in bacteria and its involvement in virulence and resistance to antibiotics. In addition, the present review summarizes the most recent and relevant literature pertaining to the anti-quorum sensing of secondary metabolites and its relationship to antibacterial activity.

Genetic diversity, antimicrobial, nutritional, and phytochemical properties of Chenopodium album: A comprehensive review.

Chenopodium album L., is a medicinal plant widely cultivated in Europe, North America, Iran, South Africa, Australia, South America, and Asia. This species is commonly used in folk medicine to treat many diseases such as cancer, viral infections, parasitic diseases, gastrointestinal disorders, as well as bacterial and fungal infections. The present review was carried out to highlight previous studies on C. album, including its botanical description, geographical distribution, genetic diversity, ecological variability, ethnomedicinal use, bioactive compounds, pharmacological properties, and toxicology. The data collected on C. album was generated using various scientific research databases such as SciFinder, PubMed, Google Scholar, SpringerLink, ScienceDirect, Web of Science, Scopus, and Wiley Online. In this review, the data presented focus on C. album to elucidate its ethnomedicinal use, pharmacological activities, and chemical composition in order to investigate the possible therapeutic pathways of the plant. Analysis of the findings showed that C. album has a capital power in various therapeutic uses such as antibacterial, antifungal, antiviral, antiparasitic, antipruritic, anticancer, antiulcer, antirheumatic, antidiabetic, antihyperlipidemic, antioxidant, and anti-inflammatory as well as other biological functions. Indeed, data on the chemical composition of the extracts and essential oils of this plant revealed its richness in secondary metabolites. The results of this paper prove that the pharmacological properties of C. album confirm its traditional importance in the international traditional pharmacopeia. This species notably exhibits various biological activities; antibacterial, antifungal, and antioxidant effects. However, toxicological investigations and pharmacokinetic validation are necessary in order to identify a possible toxicity of this plant for future clinical trials and to validate its bioavailability.

Is the rhizosphere a source of applicable multi-beneficial microorganisms for plant enhancement?

The plant faces different pedological and climatic challenges that influence its growth and enhancement. While, plant-microbes interactions throught the rhizosphere offer several privileges to this hotspot in the service of plant, by attracting multi-beneficial mutualistic and symbiotic microorganisms as plant growth-promoting bacteria (PGPB), archaea, mycorrhizal fungi, endophytic fungi, and others…). Currently, numerous investigations showed the beneficial effects of these microbes on growth and plant health. Indeed, rhizospheric microorganisms offer to host plants the essential assimilable nutrients, stimulate the growth and development of host plants, and induce antibiotics production. They also attributed to host plants numerous phenotypes involved in the increase the resistance to abiotic and biotic stresses. The investigations and the studies on the rhizosphere can offer a way to find a biological and sustainable solution to confront these environmental problems. Therefore, the interactions between microbes and plants may lead to interesting biotechnological applications on plant improvement and the adaptation in different climates to obtain a biological sustainable agricultures without the use of chemical fertilizers.

A review on transcriptomic and metabolomic responses of plants to nanopollution.

Nanoparticles (NPs) are tiny substances that can exist in the soil with different forms at different concentrations. In general, they present enormous effects on the growth, physiology, and molecular responses in plants. Indeed, they can penetrate the roots, stem, and leaves via different ways like stomata, plasmodesmata, xylem, and phloem and through transporter proteins like aquaporins. Once entered the plants, NPs induce reactive oxygen species (ROS) formation, and the plants respond to ROS by stimulates the production of antioxidants and antioxidant enzymes as well as the production of various primary and secondary metabolites like flavonoids and phenolic compounds. In addition, NPs have significantly affected the distribution of mineral profiles in plants. NPs considerably affect plant growth and yield in a dose-dependent fashion. At higher concentrations, they induced potent cytotoxicity and genotoxicity and thus reduced the growth and development of plants in turn decrease the yield. NPs exert potent changes in the transcriptome and metabolome pattern of plants to counteract the ROS imposed by NPs. This review depicts the overview of transcriptomic and metabolomic responses of plants towards nanopollution.

Conventional Medicinal Uses, Phytoconstituents, and Biological Activities of Euphorbia officinarum L.: A Systematic Review.

The Moroccan endemic plant Euphorbia officinarum is a traditional medicinal plant, known locally as "Daghmus." Plants in the genus Euphorbia are well known for the chemical diversity of their diterpenoids and isoprenoid constituents, which perform many activities such as cytotoxic, antimicrobial, and anti-inflammatory activities, as well as different biological properties, that cannot be overlooked. The effect of bioactive compounds (antiviral, antidiabetic, anticancer, and antioxidant). Euphorbia officinarum is an important conventional medicine for the treatment of various conditions, including skin and ophthalmological diseases. It is also used against human pathogens (intestinal parasites). E. officinarum latex is the major part of the plant used for conventional medicine and synthesizing new bioactive compounds. The characterization and isolation of its components are necessary to exploiting and enhancing its therapeutic potential. However, to the best of our knowledge, no review is available to date. In order to have and define a research question, we adopt a strategy by considering the items of the PRISMA checklist. Therefore, this review aims to cover E. officinarum taxonomy, botanical description, distribution, conventional uses, and phytochemical compounds of this plant, including the biological activities of compounds isolated and of these semisynthesized compounds. This article provides a foundation for any further studies from this plant.

Plant-microbial interaction: The mechanism and the application of microbial elicitor induced secondary metabolites biosynthesis in medicinal plants.

Plants and microbes interact with each other via different chemical signaling pathways. At the risophere level, the microbes can secrete molecules, called elicitors, which act on their receptors located in plant cells. The so-called elicitor molecules as well as their actions differ according to the mcirobes and induce different bilogical responses in plants such as the synthesis of secondary metabolites. Microbial compounds induced phenotype changes in plants are known as elicitors and signaling pathways which integrate elicitor's signals in plants are called elicitation. In this review, the impact of microbial elicitors on the synthesis and the secretion of secondary metabolites in plants was highlighted. Moreover, biological properties of these bioactive compounds were also highlighted and discussed. Indeed, several bacteria, fungi, and viruses release elicitors which bind to plant cell receptors and mediate signaling pathways involved in secondary metabolites synthesis. Different phytochemical classes such as terpenoids, phenolic acids and flavonoids were synthesized and/or increased in medicinal plants via the action of microbial elicitors. Moreover, these compounds compounds exhibit numerous biological activities and can therefore be explored in drugs discovery.

Phytochemical properties, biological activities and medicinal use of Centaurium erythraea Rafn.

ETHNOPHARMACOLOGICAL RELEVANCE: Centaurium erythraea is an important medicinal plant in many countries, e.g. Morocco, Algeria, Italy, Spain, Portugal, and countries of Balkan Peninsula. It is used in folk medicine to treat various illnesses. It is also used as an antiapoplectic, anticoagulant, anticholagogue, antipneumonic, hematocathartic, and as a hypotensive agent. AIM OF THE REVIEW: In this review, previous reports on the taxonomy, botanical description, geographic distribution, ethnomedicinal applications, phytochemistry, pharmacological properties, and toxicity of Centaurium erythraea were critically summarized. MATERIALS AND METHODS: Scientific search engines including PubMed, ScienceDirect, SpringerLink, Web of Science, Scopus, Wiley Online, SciFinder, and Google Scholar were consulted to collect data on C. erythraea. The data presented in this work summarized the main reports on C. erythraea phytochemical compounds, ethnomedicinal uses, and pharmacological activities. RESULTS: C. erythraea is used in traditional medicine to treat various diseases such as diabetes, fever, rhinitis, stomach ailments, urinary tract infections, dyspeptic complaints, loss of appetite, and hemorrhoids, and as diuretic. The essential oils and extracts of C. erythraea exhibited numerous biological properties such as antibacterial, antioxidant, antifungal, antileishmanial, anticancer, antidiabetic, anti-inflammatory, insecticidal, diuretic, gastroprotective, hepatoprotective, dermatoprotective, neuroprotective, and inhibitory agent for larval development. Phytochemical characterization of C. erythraea revealed the presence of several classes of secondary metabolites such as xanthonoids, terpenoids, flavonoids, phenolic acids, and fatty acids. CONCLUSIONS: Ethnomedicinal studies demonstrated the use of C. erythraea for the treatment of various disorders. Pharmacological reports showed that C. erythraea especially its aerial parts and roots exhibited potent, and beneficial activities. These findings confirmed the link between the traditional medicinal use and the results of the scientific biological experiments. Considering these results, further investigation using diverse in vivo pharmacological assays are strongly recommended to validate the results of its traditional use. Toxicological tests and pharmacokinetic studies are also required to validate the safety and efficacy of C. erythraea and its bioactive contents.

Traditional use, phytochemistry, toxicology, and pharmacology of Origanum majorana L.

ETHNOPHARMACOLOGICAL RELEVANCE: Origanum majorana L., is an aromatic and medicinal plant distributed in different parts of Mediterranean countries. This species is widely used in traditional medicine for the treatment of many diseases such as allergies, hypertension, respiratory infections, diabetes, stomach pain, and intestinal antispasmodic. AIM OF THE REVIEW: This work reports previous studies on O. majorana concerning its taxonomy, botanical description, geographical distribution, traditional use, bioactive compounds, toxicology, and biological effects. MATERIALS AND METHODS: Different scientific data bases such as Web of Science, Scopus, Wiley Online, SciFinder, Google Scholar, PubMed, ScienceDirect, and SpringerLink were consulted to collect data about O. majorana. The presented data emphasis bioactive compounds, traditional uses, toxicological investigations, and biological activities of O. majorana. RESULTS: The findings of this work marked an important correlation between the traditional use of O. majorana as an anti-allergic, antihypertensive, anti-diabetic agent, and its biological effects. Indeed, pharmacological investigations showed that essential oils and extracts from O. majorana exhibit different biological properties, particularly; antibacterial, antifungal, antioxidant, antiparasitic, antidiabetic, anticancer, nephrotoxicity protective, anti-inflammatory, analgesic and anti-pyretic, hepatoprotective, and antimutagenic effects. Toxicological evaluation confirmed the safety and innocuity of this species and supported its medicinal uses. Several bioactive compounds belonging to different chemical family such as terpenoids, flavonoids, and phenolic acids were also identified in O. majorana. CONCLUSIONS: The results suggest that the pharmacological properties of O. majorana confirm its traditional uses. Indeed, O. majorana essential oils showed remarkable antimicrobial, antioxidant, anticancer, anti-inflammatory, antimutagenic, nephroprotective, and hepatoprotective activities. However, further investigations regarding the evaluation of molecular mechanisms of identified compounds against human cancer cell lines, inflammatory process, and microbial infections are needed to validate pharmacodynamic targets. The toxicological investigation of O. Majorana confirmed its safety and therefore encouraged pharmacokinetic evaluation tests to validate its bioavailability.

Phytochemical and biological activities of Pinus halepensis mill., and their ethnomedicinal use.

ETHNOPHARMACOLOGICAL RELEVANCE: Pinus halepensis Mill., is a Mediterranean medicinal plant with numerous traditional applications such as anti-scarring, antiseptic, astringent, antifungal, and anti-tuberculosis. It is used against diarrhea, wounds, rheumatism, cough, gastrointestinal illnesses, hypertension, and hemorrhoids. AIM OF THE REVIEW: We critically summarized previous reports on the botanical, taxonomical, ecological, geographical distribution, phytochemical, and pharmacological results of P. halepensis Mill. MATERIALS AND METHODS: To gather data on P. halepensis Mill., different scientific search engines were consulted such as Google Scholar, Scopus, Wiley Online, Scifinder, Web of Science, ScienceDirect, SpringerLink, PubMed. The collected data on P. halepensis Mill., were organised according to ethnomedicinal use, phytochemistry, and pharmacology. RESULTS: Ethnomedicinal studies indicated that P. halepensis Mill., is used as a protective remedy against respiratory and digestive disorders, arterial hypertension, microbial infections. These medicinal uses vary based on the part used and regions. The extracts and essential oils of P. halepensis Mill., demonstrated several biological effects including antimicrobial, antidiabetic anti-inflammatory, cytotoxic, antiparasitic, and hepatoprotective. Traditional uses and biological effects of P. halepensis Mill., were attributed to the numerous molecules that belong to different chemical classes such as terpenoids, phenolic acids, flavonoids, fatty acids and steroids, aldehydes and ketones. CONCLUSIONS: In vitro and in vivo investigations of P. halepensis Mill., extracts and essential oils showed interesting pharmacological activities supporting the traditional use of this species. Previous reports indicated that P. halepensis Mill., extracts and their constituents exhibited potent antibacterial, antifungal, antioxidant, protective, anticoagulant, anti-hemolytic, and anti-inflammatory effects. Further investigation is needed to reveal the full biological spectra of P. halepensis Mill., extracts and essential oils (using in vivo models) and to validate their industrial applications as a food additive. However, in-depth studies are required to investigate the biological properties and molecular mechanisms of P. halepensis Mill., secondary metabolites in the management of diabetes mellitus and the prevention of the neurodegenerative disorders development such as Alzheimer's and Parkinson's disease. Studies exploring pharmacological effects of P. halepensis Mill., bioactive components such as the antimicrobial, anti-inflammatory, and antiparasitic drugs are required to validate the clinical use of these molecules. The safety of P. halepensis Mill., and its bioactive compounds should be also investigated by carrying out further pharmacokinetic and toxicological experiments.

Origanum compactum Benth., from traditional use to biotechnological applications.

Origanum compactum Benth., is a Moroccan medicinal plant known by its local name as Zaatar. In Morocco, it has various traditional applications such as the use to treat diabetes, metabolic disorders, digestive, and respiratory problems. In this review, we critically highlighted current investigations on the ethnopharmacological studies, the phytochemistry, pharmacological investigations, biotechnological applications, and future perspective of O. compactum. A bibliometric electronic search in worldwide accepted scientific databases such as ScienceDirect, PubMed, SpringerLink, Web of Science, Scopus, Wiley Online, and Google Scholar was carried out to gather on O. compactum. Chemical analysis using GC-MS and/or HPLC allowed the identification of several bioactive compounds such as terpenoids and phenolic acids. Furthermore, O. compactum extracts and essential oils have been tested for various biological activities such as antibacterial, antioxidant, antiparasitic, antifungal, and anticancer effects. Moreover, an alignment between traditional use and biological effects was demonstrated, in particular for the antimicrobial activity. These properties are related to O. compactum bioactive components, especially the volatile compounds such as thymol and carvacrol. The pharmacological mechanisms involve several cellular and molecular targeted actions. Moreover, the biological potential of this species had led some laboratories to apply the biotechnological tools for its regeneration. PRACTICAL APPLICATIONS: Origanum compactum is applied as traditional drug against different illnesses and for food preservation. Scientific investigations proved the application of O. compactum essential oils in food industries as antioxidants and antimicrobials. These volatile compounds could be applied also in pharmaceutical industries, in particular as antibacterial, antifungal, and antileishmanial drugs. Moreover, further investigations concerning toxicological evidences and pharmacokinetic as well as pharmacodynamic mechanistic targets and clinical trials could develop anticancer, antimalaria and anti-inflammatory, and antidiabetic drugs. Finally, the results of the findings of these purposes encourage other research groups to carry out further investigations on the pharmacological properties of O. compactum.

Ethnomedicinal use, phytochemistry, pharmacology, and toxicology of Ajuga iva (L.,) schreb.

ETHNOPHARMACOLOGICAL RELEVANCE: Ajuga iva (L.,) Schreb (A. iva). is a medicinal plant commonly used in Africa to treat several diseases such as diabetes, rheumatism, allergy, cancer, renal, metabolic disorders, cardiovascular disorders, digestive, and respiratory disorders. AIM OF THE REVIEW: We highlighted previous reports on A. iva including its ethnopharmacological uses, the chemistry of its secondary metabolites, in vitro and in vivo pharmacological properties, and toxicological evidence. MATERIALS AND METHODS: The data on A. iva were gathered using scientific research databases such as ScienceDirect, PubMed, SpringerLink, Web of Science, Scopus Wiley Online, and Google Scholar. In this review, studies focused on A. iva and its phytopharmacological activities were explored. RESULTS: A. iva is used by many North African folk medicine practitioners especially against diabetes and immunological diseases. Our analysis of the previous reports confirmed the scientific evidence of A. iva ethnomedicinal uses, especially the antidiabetic and anti-hypercholesterolemia activity. However, there was no clear correlation between previous pharmacological reports on A. iva and its other ethnomedicinal uses in the treatment of rheumatism, allergy, metabolic, digestive, and respiratory disorders. The extracts and isolated compounds from A. iva exhibited numerous in vitro and in vivo pharmacological activities such as antidiabetic, antioxidant, antimicrobial, anti-hypercholesterolemia, insecticide, and litholitic effects. Chemical characterization using GC-MS, HPLC, and NMR revealed the presence of many chemical compounds such as 20-hydroxyecdysone, cyasterone, ajugasterone, apigenin dihexoside, apigenin, carvacrol, ecdysterone, palmitic acid in different parts of A. iva. These compounds belong to different classes of chemical compounds such as steroids, flavonoids, fatty acids, and terpenoids. CONCLUSIONS: A. iva extracts especially from the leaves showed significant antidiabetic, antioxidant, anti-hypercholesterolemia, and analgesic effects. Future studies are required to validate the results of clinical trials on A. iva antidiabetic, anti-hypercholesterolemia, antioxidant/anti-inflammatory, antimicrobial, and analgesic properties. Toxicological validation and pharmacokinetics investigation are necessary to validate the efficacy and safety A. iva extracts and its secondary metabolites. An in-depth investigation is needed to reveal the biological activity of A. iva active compounds in preventing the development of cancer and neurodegenerative disorders such as Alzheimer's and Parkinson's diseases.

GC-MS Analysis, Antioxidant and Antimicrobial Activities of Achillea Odorata Subsp. Pectinata and Ruta Montana Essential Oils and Their Potential Use as Food Preservatives.

In order to discover new natural resources with biological properties, the chemical composition, the antioxidant and antimicrobial activities, and the potential use as food preservative of essential oils of Moroccan Achillea odorata subsp. pectinata (AOpEO) and Ruta montana (RMEO) were studied. Gas chromatography-mass spectrometry (GC-MS) analysis revealed the presence of 21 and 25 compounds in AOpEO and RMEO, respectively. The results showed that the major compounds of AOpEO are camphor (45.01%), bornyl acetate (15.07%), borneol (11.33%), ß-eudesmol (4.74%), camphene (3.58%), and 1.8-cineole (eucalyptol) (2.96%), whereas 2-undecanone (63.97%), camphor (3.82%) and cyclopropanecarboxylic acid (3.66%) were the main components of RMEO. The antioxidant activities were evaluated by diphenylpicrylhydraziyl radical (DPPH) and reducing power assays. The antimicrobial activities of essential oils were tested against bacterial strains and food contaminant yeast using agar disc diffusion and microdilution methods. A significant antimicrobial activity of AOpEO was observed against Bacillus subtilis, Proteus mirabilis and Candida albicans, compared to RMEO. The efficacy of AOpEO was also evaluated in model food systems (cabbage and barley) artificially inoculated during storage. The results found that the adding of a minimal inhibitory concentration (MIC) and 4× MIC were potent in decreasing the Proteus mirabilis growth in food model systems. Our findings suggested that AOpEO may be potentially used as an alternative food preservative.

Ethnomedicinal use, phytochemistry, pharmacology, and food benefits of Thymus capitatus.

ETHNOPHARMACOLOGICAL RELEVANCE: Thymus capitatusHoffm. et Link. is an endemic medicinal plant to the Mediterranean region. It is used in folk medicine to treat various diseases including diabetes, flu, cough, flatulence, dermatitis, indigestion, respiratory disorders, asthma, rheumatic, diarrhea, and influenza. It is also used as antiseptic, analgesic, stimulant, and sedative. AIM OF THE REVIEW: In this review, previous reports on T. capitatusconcerningits taxonomy, botanical description, geographical distribution, ethnomedicinal use, phytochemistry, pharmacological properties, and food benefits were critically summarized. MATERIALS AND METHODS: Scientificsearch engines including PubMed, ScienceDirect, SpringerLink, Web of Science, Scopus, Wiley Online, Scifnder, and Google Scholar were consulted to gather data on T. capitatus. The data presented in this work summarize T. capitatus phytochemical compounds, ethnomedicinaluses, pharmacological properties, and food value. RESULTS: In traditional medicine, T. capitatusis used to treat various illnesses including diabetes, dermatitis, and diarrhea. The essential oils and extracts of T. capitatus exhibited several biological properties such as antibacterial, antioxidant, antifungal, antiparasitic, hypoglycemic, anticancer, antiviral, and hepatoprotective effects. T. capitatus possesses high nutritional value and its essential oil showed promising activity in food preservation. Phytochemical characterization of T. capitatus revealed the presence of several classes of secondary metabolites such as terpenoids, flavonoids, and phenolic acids. CONCLUSIONS: Ethnomedicinal surveys indicated the use of T. capitatus for the treatment of various disorders. Pharmacological reports showed that T. capitatus especially its essential oils, exhibited potent antimicrobial, antioxidant, antidiabetic and hepatoprotective effects. These findings confirmed the link between traditional medicinal use and scientific biological results. Moreover, T. capitatus exhibited a potent food preservative effect which justifies its use in traditional medicine as a food additive. In light of these findings, further studies to validate the industrial applications of T. capitatus essential oils as a food additive are required. Further investigations on the in vivo pharmacological properties of T. capitatus are strongly recommended to validate the results of its clinical uses as an antimicrobial, hepatoprotective, and antiviral agent. Toxicological tests and pharmacokinetic investigations are also needed to validate the safety and efficacy ofT. capitatus and its bioactive compounds.

Pharmacological Properties of Chalcones: A Review of Preclinical Including Molecular Mechanisms and Clinical Evidence.

Chalcones are among the leading bioactive flavonoids with a therapeutic potential implicated to an array of bioactivities investigated by a series of preclinical and clinical studies. In this article, different scientific databases were searched to retrieve studies depicting the biological activities of chalcones and their derivatives. This review comprehensively describes preclinical studies on chalcones and their derivatives describing their immense significance as antidiabetic, anticancer, anti-inflammatory, antimicrobial, antioxidant, antiparasitic, psychoactive, and neuroprotective agents. Besides, clinical trials revealed their use in the treatment of chronic venous insufficiency, skin conditions, and cancer. Bioavailability studies on chalcones and derivatives indicate possible hindrance and improvement in relation to its nutraceutical and pharmaceutical applications. Multifaceted and complex underlying mechanisms of chalcone actions demonstrated their ability to modulate a number of cancer cell lines, to inhibit a number of pathological microorganisms and parasites, and to control a number of signaling molecules and cascades related to disease modification. Clinical studies on chalcones revealed general absence of adverse effects besides reducing the clinical signs and symptoms with decent bioavailability. Further studies are needed to elucidate their structure activity, toxicity concerns, cellular basis of mode of action, and interactions with other molecules.