Structure and Activity of Pentacyclic Triterpenes Codrugs. A Review

2021 ◽  
Vol 21 ◽  
Author(s):  
Justyna Żwawiak ◽  
Anna Pawełczyk ◽  
Dorota Olender ◽  
Lucjusz Zaprutko
Keyword(s):  
Biological Activities ◽  
Anticancer Activities ◽  
Drug Molecule ◽  
Pentacyclic Triterpene ◽  
Formation Pathway ◽  
Chemical Systems ◽  
Drug Molecules ◽  
Wide Range ◽  
Anti Hiv ◽  
Structure And Activity

: Triterpenes are a wide and important group of compounds that have several promising pharmacological properties, such as hepatoprotective, anti-inflammatory, anti-HIV, antioxidant, or anticancer activities. Such potent substances can be successfully incorporated in more complex chemical systems e.g. codrugs or pro-drugs that have better pharmacological profile. The codrug is connected with a drug formation pathway to chemically cohere at least two drug molecules to improve positive therapeutic efficiency or decrease side effects. The codrug can be cleaved in the organism to generate effective compounds previously used as substrates. This article presents an overview of codrugs that consist of pentacyclic triterpene moiety that is chosen as a basic codrug moiety due to their wide range of vital activities and another drug molecule fragment. It was found that triterpenoid codrugs are characterized by a wide range of biological activities. However, most of them have anticancer potency.

Synthesis and characterization of a new series of thiadiazole derivatives as potential anticancer agents

2020 ◽  
Vol 26 (1) ◽  
pp. 6-13 ◽  
Author(s):  
Ulviye Acar Çevik ◽  
Derya Osmaniye ◽  
Serkan Levent ◽  
Begüm Nurpelin Sağlik ◽  
Betül Kaya Çavuşoğlu ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Chemotherapeutic Agents ◽  
Anticancer Activities ◽  
Normal Tissues ◽  
H Nmr ◽  
Wide Range ◽  
Thiadiazole Derivatives ◽  
Low Efficiency

AbstractCancer is one of the most common causes of death in the world. Despite the importance of combating cancer in healthcare systems and research centers, toxicity in normal tissues and the low efficiency of anticancer drugs are major problems in chemotherapy. Nowadays the aim of many medical research projects is to discover new safer and more effective anticancer agents. 1,3,4-Thiadiazole compounds are important fragments in medicinal chemistry because of their wide range of biological activities, including anticancer activities. The aim of this study was to determine the capacity of newly synthesized 1,3,4-thiadiazole compounds as chemotherapeutic agents. The structures of the obtained compounds were elucidated using 1H-NMR, 13C-NMR and mass spectrometry. Although the thiadiazole derivatives did not prove to be significantly cytotoxic to the tumour tissue cultures, compound 4i showed activity against the C6 rat brain cancer cell line (IC50 0.097 mM) at the tested concentrations.

Development and characterization of electrospun curcumin-loaded antimicrobial nanofibrous membranes

2020 ◽  
pp. 004051752092551
Author(s):  
Javeed A Awan ◽  
Saif Ur Rehman ◽  
Muhammad Kashif Bangash ◽  
Fiaz Hussain ◽  
Jean-Noël Jaubert
Keyword(s):  
Biological Activities ◽  
Research Work ◽  
Medical Applications ◽  
Electrospinning Technique ◽  
Naturally Occurring ◽  
Wide Range ◽  
Nanofibrous Membranes ◽  
Antimicrobial Barrier ◽  
Anti Hiv

Curcumin is a naturally occurring hydrophobic polyphenol compound. It exhibits a wide range of biological activities such as antibacterial, anti-inflammatory, anti-carcinogenic, antifungal, anti-HIV, and antimicrobial activity. In this research work, antimicrobial curcumin nanofibrous membranes are produce by an electrospinning technique using the Eudragit RS 100 (C19H34ClNO6) polymer solution enriched with curcumin. The morphology and chemistry of the membrane are analyzed using scanning electron microscopy (SEM) and Fourier transform infrared (FTIR) spectroscopy. Kirby Bauer disk diffusion tests are carried out to examine the antibacterial effectiveness of the membrane. Experimental results show that the nanofibers produced are of uniform thickness morphology and curcumin is successfully incorporated into the nanofibrous mat, while no chemical bonding was observed between curcumin and the polymer. The antimicrobial curcumin nanofibrous membranes can be effectively applied as antimicrobial barrier in a wide variety of medical applications such as wound healing, scaffolds, and tissue engineering.

Indazole as a Privileged Scaffold: The Derivatives and their Therapeutic Applications

2020 ◽  
Vol 20 ◽  
Author(s):  
Jinling Qin ◽  
Weyland Cheng ◽  
Yong-Tao Duan ◽  
Hua Yang ◽  
Yongfang Yao
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Vital Role ◽  
Drug Molecules ◽  
Structure Activity ◽  
Privileged Scaffold ◽  
Future Direction ◽  
Relationship Of ◽  
Anti Hiv ◽  
Clinical Drug

Background: Heterocyclic compounds, also called heterocycles, are a major class of organic chemicalcompound that plays a vital role in the metabolism of all living cells. The heterocyclic compound, indazole, has attracted more attention in recent years and is widely present in numerous commercially available drugs. Indazole-containing derivatives, representing one of the most important heterocycles in drug molecules, are endowed with a broad range of biological properties. Methods: A literature search was conducted in PubMed, Google Scholar and Web of Science regarding articles related to indazole and its therapeutic application. Results: The mechanism and structure-activity relationship of indazole and its derivatives were described. Based on their versatile biological activities, the compounds were divided into six groups: anti-inflammatory, antibacterial, anti-HIV, antiarrhythmic, antifungal and antitumour. At least 43 indazole-based therapeutic agents were found to be used in clinical application or clinical trials. Conclusion: This review is a guide for pharmacologists who are in search of valid preclinical/clinical drug compoundswhere the progress of approved marketed drugs containing indazole scaffold is examined from 1966 to the present day. Future direction involves more diverse bioactive moieties with indazole scaffold and greater insights into its mechanism.

Bioactive Heterocyclic Compounds as Potential Therapeutics in the Treatment of Gliomas: A Review

2021 ◽  
Vol 21 ◽  
Author(s):  
Reyaz Hassan ◽  
Roohi Mohi-ud-din ◽  
Mohammad Ovais Dar ◽  
Abdul Jalil Shah ◽  
Prince Ahad Mir ◽  
...  
Keyword(s):  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Anticancer Activities ◽  
Tumour Heterogeneity ◽  
Cancer Cell Death ◽  
Wide Range ◽  
Heterocyclic Derivatives ◽  
Current Therapies ◽  
Terminal Prognosis ◽  
Potential Therapeutics

: Cancer is one of the most alarming diseases, with an estimation of 9.6 million deaths in 2018. Glioma occurs in glial cells surrounding nerve cells. The majority of the patients with gliomas have a terminal prognosis, and the ailment has significant sway on patients and their families, be it physical, psychological, or economic wellbeing. As Glioma exhibits, both intra and inter tumour heterogeneity with multidrug resistance and current therapies are ineffective. So the development of safer anti gliomas agents is the need of hour. Bioactive heterocyclic compounds, eithernatural or synthetic,are of potential interest since they have been active against different targets with a wide range of biological activities, including anticancer activities. In addition, they can cross the biological barriers and thus interfere with various signalling pathways to induce cancer cell death. All these advantages make bioactive natural compounds prospective candidates in the management of glioma. In this review, we assessed various bioactive heterocyclic compounds, such as jaceosidin, hispudlin, luteolin, silibinin, cannabidiol, tetrahydrocannabinol, didemnin B, thymoquinone, paclitaxel, doxorubicin, and cucurbitacins for their potential anti-glioma activity. Also, different kinds of chemical reactions to obtain various heterocyclic derivatives, e.g. indole, indazole, benzimidazole, benzoquinone, quinoline, quinazoline, pyrimidine, and triazine, are listed.

scholarly journals An Update on Pharmacological Potential of Boswellic Acids against Chronic Diseases

2019 ◽  
Vol 20 (17) ◽  
pp. 4101 ◽  
Author(s):  
Nand Kishor Roy ◽  
Dey Parama ◽  
Kishore Banik ◽  
Devivasha Bordoloi ◽  
Amrita Khwairakpam Devi ◽  
...  
Keyword(s):  
Chronic Diseases ◽  
Biological Activities ◽  
Boswellic Acid ◽  
Pentacyclic Triterpene ◽  
Boswellia Serrata ◽  
Wide Range ◽  
Molecular Mechanism Of Action ◽  
Inflammatory Bowel ◽  
Pharmacological Potential ◽  
Significant Attention

Natural compounds, in recent years, have attracted significant attention for their use in the prevention and treatment of diverse chronic diseases as they are devoid of major toxicities. Boswellic acid (BA), a series of pentacyclic triterpene molecules, is isolated from the gum resin of Boswellia serrata and Boswellia carteri. It proved to be one such agent that has exhibited efficacy against various chronic diseases like arthritis, diabetes, asthma, cancer, inflammatory bowel disease, Parkinson’s disease, Alzheimer’s, etc. The molecular targets attributed to its wide range of biological activities include transcription factors, kinases, enzymes, receptors, growth factors, etc. The present review is an attempt to demonstrate the diverse pharmacological uses of BA, along with its underlying molecular mechanism of action against different ailments. Further, this review also discusses the roadblocks associated with the pharmacokinetics and bioavailability of this promising compound and strategies to overcome those limitations for developing it as an effective drug for the clinical management of chronic diseases.

scholarly journals Antibacterial, Antiviral, Antioxidant, and Anticancer Activities of Postbiotics: A review of Mechanisms and Therapeutic Perspectives

2021 ◽  
Vol 12 (2) ◽  
pp. 2629-2645
Keyword(s):  
Human Health ◽  
Fermentation Process ◽  
Biological Activities ◽  
Scientific Evidence ◽  
Food Allergies ◽  
Live Cells ◽  
Anticancer Activities ◽  
Wide Range ◽  
Anti Cancer ◽  
Improve Health

Several scientific evidence has shown the advantageous effects of probiotic-derived metabolites on human health. Postbiotics are a wide range of bioactive compounds derived from probiotics through a fermentation process and/or produced in pure forms in laboratory scales. These compounds have native biological activities that have been extensively studied in recent years. Immunomodulation, antimicrobial, anti-cancer, antioxidant, anti-diabetic, and reduction of food allergies compose the most important biological roles of postbiotics. In terms of safety, it has been confirmed that postbiotics, as potential substitute elements, might be superior to their parent live cells. Also, due to their appropriate economic, technological, and clinical features, they could be employed as favorable apparatuses in the food and drug industry to improve health benefits. This review comprehensively discusses the concept of postbiotics and their characteristics, emphasizing their potential antibacterial, antiviral, antioxidant, and anticancer activities.

scholarly journals Bioactive Phytochemicals: Efficient Synthesis of Optically Active Substituted Flav-3-enes and Flav-3-en-3-o-R Derivatives

2017 ◽  
Vol 2017 ◽  
pp. 1-11
Author(s):  
Matthew Chilaka Achilonu ◽  
Moosa Mahmood Sedibe ◽  
Karabo Shale
Keyword(s):  
Good Yield ◽  
Biological Activities ◽  
Optically Active ◽  
Synthetic Chemistry ◽  
Efficient Synthesis ◽  
Anticancer Activities ◽  
Wide Range ◽  
Significant Interest ◽  
Bioactive Phytochemicals ◽  
Pharmacological Profiles

The structural core of flavene (2-phenyl-2H-chromene) is commonly found in plant flavonoids, which exhibit a wide range of biological activities and diverse pharmacological profiles (e.g., antioxidant and anticancer activities). Flavonoids have attracted significant interest in medicinal and synthetic chemistry. Substituted flav-3-ene 13 was exclusively synthesized by the stereoselective elimination of the O-mesyl moiety on C-3 of 5,7,3′,4′-tetramethoxyflavan-3-mesylate 12 with 1,8-diazabicyclo[5.4.0]undec-7-ene. The reaction of 5,7,3′,4′-tetramethoxyflavan-3-one 15 with ytterbium trifluoromethanesulfonate in methanol afforded a novel 3-O-substituted flav-3-ene derivative (3,5,7,3′,4′-pentamethoxyflav-3-ene) 17. The reduction of 4-(1,3,5-trihydroxybenzene)-5,7,3′,4′-tetra-O-benzylflavan-3-one 19b with hydrogen afforded a new compound: 3-hydroxy-4-(1,3,5-trihydroxybenzene)-5,7,3′,4′-tetrahydroxyflavan-3-en-3-ol 21 in good yield (95%), while the acetylation of 19a and 21 afforded the expected novel flav-3-en-3-acetoxy derivatives 20 (92%) and 22 (90%), respectively.

scholarly journals Therapeutic Potential of Hydrazones as Anti-Inflammatory Agents

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Anu Kajal ◽  
Suman Bala ◽  
Neha Sharma ◽  
Sunil Kamboj ◽  
Vipin Saini
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Chemical Properties ◽  
Basic Structure ◽  
Active Centers ◽  
Carbon And Nitrogen ◽  
Wide Range ◽  
Anti Inflammatory ◽  
Physical And Chemical ◽  
Anti Hiv

Hydrazones are a special class of organic compounds in the Schiff base family. Hydrazones constitute a versatile compound of organic class having basic structure (R1R2C=NNR3R4). The active centers of hydrazone, that is, carbon and nitrogen, are mainly responsible for the physical and chemical properties of the hydrazones and, due to the reactivity toward electrophiles and nucleophiles, hydrazones are used for the synthesis of organic compound such as heterocyclic compounds with a variety of biological activities. Hydrazones and their derivatives are known to exhibit a wide range of interesting biological activities like antioxidant, anti-inflammatory, anticonvulsant, analgesic, antimicrobial, anticancer, antiprotozoal, antioxidant, antiparasitic, antiplatelet, cardioprotective, anthelmintic, antidiabetic, antitubercular, trypanocidal, anti-HIV, and so forth. The present review summarizes the efficiency of hydrazones as potent anti-inflammatory agents.

scholarly journals A Review of the Ethnomedicinal Uses, Biological Activities, and Triterpenoids of Euphorbia Species

Molecules ◽  
2020 ◽  
Vol 25 (17) ◽  
pp. 4019
Author(s):  
Douglas Kemboi ◽  
Xolani Peter ◽  
Moses Langat ◽  
Jacqueline Tembu
Keyword(s):  
Drug Discovery ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Structural Diversity ◽  
Pharmacological Properties ◽  
Anticancer Activities ◽  
Sensory Disorders ◽  
Wide Range ◽  
Ethnomedicinal Uses

The genus Euphorbia is one of the largest genera in the spurge family, with diversity in range, distribution, and morphology. The plant species in this genus are widely used in traditional medicine for the treatment of diseases, ranging from respirational infections, body and skin irritations, digestion complaints, inflammatory infections, body pain, microbial illness, snake or scorpion bites, pregnancy, as well as sensory disorders. Their successes have been attributed to the presence of diverse phytochemicals like polycyclic and macrocyclic diterpenes with various pharmacological properties. As a result, Euphorbia diterpenes are of interest to chemists and biochemists with regard to drug discovery from natural products due to their diverse therapeutic applications as well as their great structural diversity. Other chemical constituents such as triterpenoids have also been reported to possess various pharmacological properties, thus supporting the traditional uses of the Euphorbia species. These triterpenoids can provide potential leads that can be developed into pharmaceutical compounds for a wide range of medicinal applications. However, there are scattered scientific reports about the anticancer activities of these constituents. Harnessing such information could provide a database of bioactive pharmacopeia or targeted scaffolds for drug discovery. Therefore, this review presents an updated and comprehensive summary of the ethnomedicinal uses, phytochemistry, and the anticancer activities of the triterpenoids of Euphorbia species. Most of the reported triterpenoids in this review belong to tirucallane, cycloartanes, lupane, oleanane, ursane, and taraxane subclass. Their anticancer activities varied distinctly with the majority of them exhibiting significant cytotoxic and anticancer activities in vitro. It is, therefore, envisaged that the report on Euphorbia triterpenoids with interesting anticancer activities will form a database of potential leads or scaffolds that could be advanced into the clinical trials with regard to drug discovery.

scholarly journals Marine Natural Products from Tunicates and Their Associated Microbes

Marine Drugs ◽  
2021 ◽  
Vol 19 (6) ◽  
pp. 308
Author(s):  
Chatragadda Ramesh ◽  
Bhushan Rao Tulasi ◽  
Mohanraju Raju ◽  
Narsinh Thakur ◽  
Laurent Dufossé
Keyword(s):  
Natural Products ◽  
Marine Natural Products ◽  
Biological Activities ◽  
Biological Properties ◽  
Anticancer Activities ◽  
Microbial Association ◽  
Wide Range ◽  
Microbial Groups ◽  
Global Oceans

Marine tunicates are identified as a potential source of marine natural products (MNPs), demonstrating a wide range of biological properties, like antimicrobial and anticancer activities. The symbiotic relationship between tunicates and specific microbial groups has revealed the acquisition of microbial compounds by tunicates for defensive purpose. For instance, yellow pigmented compounds, “tambjamines”, produced by the tunicate, Sigillina signifera (Sluiter, 1909), primarily originated from their bacterial symbionts, which are involved in their chemical defense function, indicating the ecological role of symbiotic microbial association with tunicates. This review has garnered comprehensive literature on MNPs produced by tunicates and their symbiotic microbionts. Various sections covered in this review include tunicates’ ecological functions, biological activities, such as antimicrobial, antitumor, and anticancer activities, metabolic origins, utilization of invasive tunicates, and research gaps. Apart from the literature content, 20 different chemical databases were explored to identify tunicates-derived MNPs. In addition, the management and exploitation of tunicate resources in the global oceans are detailed for their ecological and biotechnological implications.

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