scholarly journals Carboxyxanthones: Bioactive Agents and Molecular Scaffold for Synthesis of Analogues and Derivatives

Molecules ◽  
2019 ◽  
Vol 24 (1) ◽  
pp. 180 ◽  
Author(s):  
João Ribeiro ◽  
Cláudia Veloso ◽  
Carla Fernandes ◽  
Maria Elizabeth Tiritan ◽  
Madalena M. M. Pinto
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Building Blocks ◽  
Phase Iii ◽  
Pharmacological Activities ◽  
Molecular Scaffold ◽  
Xanthone Derivatives ◽  
Phase Iii Clinical Trials ◽  
Bioactive Agents ◽  
Tumor Agent

Xanthones represent a structurally diverse group of compounds with a broad range of biological and pharmacological activities, depending on the nature and position of various substituents in the dibenzo-γ-pyrone scaffold. Among the large number of natural and synthetic xanthone derivatives, carboxyxanthones are very interesting bioactive compounds as well as important chemical substrates for molecular modifications to obtain new derivatives. A remarkable example is 5,6-dimethylxanthone-4-acetic acid (DMXAA), a simple carboxyxanthone derivative, originally developed as an anti-tumor agent and the first of its class to enter phase III clinical trials. From DMXAA new bioactive analogues and derivatives were also described. In this review, a literature survey covering the report on carboxyxanthone derivatives is presented, emphasizing their biological activities as well as their application as suitable building blocks to obtain new bioactive derivatives. The data assembled in this review intends to highlight the therapeutic potential of carboxyxanthone derivatives and guide the design for new bioactive xanthone derivatives.

scholarly journals Flavonoid-Inspired Vascular Disrupting Agents: Exploring Flavone-8-Acetic Acid and Derivatives in the New Century

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4228
Author(s):  
Silvia Gobbi ◽  
Federica Belluti ◽  
Angela Rampa ◽  
Alessandra Bisi
Keyword(s):  
Acetic Acid ◽  
Biological Activities ◽  
Phase Iii ◽  
Innate Immune Responses ◽  
Lead Compounds ◽  
Phase Iii Clinical Trials ◽  
Molecular Features ◽  
Naturally Occurring ◽  
Tumour Vasculature ◽  
Biological Target

Naturally occurring flavonoids are found as secondary metabolites in a wide number of plants exploited for both medicine and food and have long been known to be endowed with multiple biological activities, making them useful tools for the treatment of different pathologies. Due to the versatility of the scaffolds and the vast possibilities of appropriate decoration, they have also been regarded as fruitful sources of lead compounds and excellent chemical platforms for the development of bioactive synthetic compounds. Flavone-8-acetic acid (FAA) and 5,6-dimethylxanthone acetic acid (DMXAA) emerged for their antitumour potential due to the induction of cytokines and consequent rapid haemorrhagic necrosis of murine tumour vasculature, and different series of derivatives have been designed thereafter. Although the promising DMXAA failed in phase III clinical trials because of strict species-specificity, a boost in research came from the recent identification of the stimulator of interferon genes (STING), responsible for supporting tumoural innate immune responses, as a possible biological target. Consequently, in the last decade a renewal of interest for these flavonoid-based structures was noticed, and novel derivatives have been synthesised and evaluated for a deeper understanding of the molecular features needed for affecting human cells. Undoubtedly, these natural-derived molecules deserve further investigation and still appear attractive in an anticancer perspective.

scholarly journals A perspective review of phytochemistry and pharmacology of the Syzygium genus

2021 ◽  
Vol 12 (2) ◽  
pp. 1490-1495
Author(s):  
Yuniarni U ◽  
Sukandar E Y ◽  
Fidrianny I
Keyword(s):  
Traditional Medicine ◽  
Pharmacological Activity ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Ornamental Plants ◽  
Chemical Compounds ◽  
Chemical Components ◽  
Pharmacological Activities ◽  
Widespread Species ◽  
Traditional Uses

Syzygium is a genus of the Myrtaceae family consisting of large and widespread species from Africa, Asia, Australia, and throughout Oceania and the Pacific region. Some have been cultivated for bearing fruit, ornamental plants and used as traditional medicine. This article excavated Syzygium genus which was focused on traditional uses, chemical compounds and biological activities related to treatment of syndrome metabolic. All information was obtained from the scientific literature such as Science Direct, Google Scholar, Scopus and PubMed. Several species were known to have therapeutic potential and used in traditional Chinese medicine, Ayurveda, and herbal medicine in Indonesia. Traditionally, Syzygium is known for its therapeutic purposes such as coughing, diarrhea, colds, dysentery, inflammation, pain, skin, and mouth infections. Only a few species have been scientifically studied to verify their usage as traditional medicine. There were many reports on the traditional uses and medicinal effects of Syzygium plants, but only a few review articles mainly about phytochemical constituents and their role in pharmacological activities. The present reviews highlight the phytochemical and pharmacological activity of various species of the Syzygium genus. The pharmacological activities were discussed in this article focused to metabolic syndrome treatment, such as antidiabetic, antihyperlipidemic, antioxidant and antihypertensive activities. Chemical components isolated mainly flavonoid, terpenoids/sesquiterpenoid, sterols, and lignan. Several bioactive compounds have been identified correlated with pharmacological activity, but the chemical compounds were different for each species.

An Overview on Chemistry and Biological Importance of Pyrrolidinone

2018 ◽  
Vol 15 (2) ◽  
pp. 166-178 ◽  
Author(s):  
Zahra Hosseinzadeh ◽  
Ali Ramazani ◽  
Kamaleddin Hosseinzadeh ◽  
Nima Razzaghi-Asl ◽  
Farideh Gouranlou
Keyword(s):  
Biological Activities ◽  
Wide Spectrum ◽  
Heterocyclic Ring ◽  
Review Article ◽  
Pharmacological Activities ◽  
Future Studies ◽  
Comprehensive Information ◽  
Novel Drugs ◽  
Bioactive Agents ◽  
Great Scope

Background: Pyrrolidinone is a five membered heterocyclic ring that is a versatile lead compound for designing powerful bioactive agents. Pyrrolidinone nucleus is one of the most important heterocyclic compound indicating notable pharmaceutical effects. Many procedures for the preparation of pyrrolidinone and also their various reactions offer great scope in the field of medicinal chemistry. This fascinating group of compounds has diverse pharmacological activities such as antibacterial, antifungal, anticancer and anticonvulsant. Objective: The review article proposes to classify comprehensive information on chemistry and pharmaceutical effects of pyrrolidinone in order to open new viewpoint for future studies. Conclusion: It is clear from the review of the topic that a wide spectrum of pyrrolidinone analogues have been synthesized and the majority of these derivatives have indicated different significant biological activities. Thus, these analogues can be used for future progression of novel drugs against many more poor agents.

scholarly journals Therapeutic potential of oxadiazole or furadiazole containing compounds

BMC Chemistry ◽  
2020 ◽  
Vol 14 (1) ◽  
Author(s):  
Ankit Siwach ◽  
Prabhakar Kumar Verma
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Antiviral Drug ◽  
Biological Properties ◽  
New Drugs ◽  
Pharmacological Activities ◽  
Methylene Groups ◽  
Synthetic Routes ◽  
Azole Ring ◽  
Derivatives Of

AbstractAs we know that, Oxadiazole or furadi azole ring containing derivatives are an important class of heterocyclic compounds. A heterocyclic five-membered ring that possesses two carbons, one oxygen atom, two nitrogen atoms, and two double bonds is known as oxadiazole. They are derived from furan by the replacement of two methylene groups (= CH) with two nitrogen (-N =) atoms. The aromaticity was reduced with the replacement of these groups in the furan ring to such an extent that it shows conjugated diene character. Four different known isomers of oxadiazole were existed such as 1,2,4-oxadiazole, 1,2,3-oxadiazole, 1,2,5-oxadiazole & 1,3,4-oxadiazole. Among them, 1,3,4-oxadiazoles & 1,2,4-oxadiazoles are better known and more widely studied by the researchers due to their broad range of chemical and biological properties. 1,3,4-oxadiazoles have become important synthons in the development of new drugs. The derivatives of the oxadiazole nucleus (1,3,4-oxadiazoles) show various biological activities such as antibacterial, anti-mycobacterial, antitumor, anti-viral and antioxidant activity, etc. as reported in the literature. There are different examples of commercially available drugs which consist of 1,3,4-oxadiazole ring such as nitrofuran derivative (Furamizole) which has strong antibacterial activity, Raltegravir as an antiviral drug and Nesapidil drug is used in anti-arrhythmic therapy. This present review summarized some pharmacological activities and various kinds of synthetic routes for 2, 5-disubstituted 1,3,4-oxadiazole, and their derived products.

scholarly journals Saponin-Rich Extracts and Their Acid Hydrolysates Differentially Target Colorectal Cancer Metabolism in the Frame of Precision Nutrition

Cancers ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 3399
Author(s):  
Marta Gómez de Cedrón ◽  
Joaquín Navarro del Hierro ◽  
Marina Reguero ◽  
Sonia Wagner ◽  
Adrián Bouzas ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Lipid Metabolism ◽  
Molecular Mechanisms ◽  
Cancer Metabolism ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Aerobic Glycolysis ◽  
Metabolic Reprogramming ◽  
Specific Subgroup ◽  
Bioactive Agents

Saponins or their aglycone form, sapogenin, have recently gained interest as bioactive agents due to their biological activities, their antitumoral effects being among them. Metabolic reprogramming has been recognized as a hallmark of cancer and, together with the increased aerobic glycolysis and glutaminolysis, the altered lipid metabolism is considered crucial to support cancer initiation and progression. The purpose of this study was to assess and compare the inhibitory effects on colorectal cancer cell lines of saponin-rich extracts from fenugreek and quinoa (FE and QE, respectively) and their hydrolyzed extracts as sapogenin-rich extracts (HFE and HQE, respectively). By mean of the latest technology in the analysis of cell bioenergetics, we demonstrate that FE and HFE diminished mitochondrial oxidative phosphorylation and aerobic glycolysis; meanwhile, quinoa extracts did not show relevant activities. Distinct molecular mechanisms were identified for fenugreek: FE inhibited the expression of TYMS1 and TK1, synergizing with the chemotherapeutic drug 5-fluorouracil (5-FU); meanwhile, HFE inhibited lipid metabolism targets, leading to diminished intracellular lipid content. The relevance of considering the coexisting compounds of the extracts or their hydrolysis transformation as innovative strategies to augment the therapeutic potential of the extracts, and the specific subgroup of patients where each extract would be more beneficial, are discussed in the frame of precision nutrition.

scholarly journals On the design principles of peptide–drug conjugates for targeted drug delivery to the malignant tumor site

2018 ◽  
Vol 14 ◽  
pp. 930-954 ◽  
Author(s):  
Eirinaios I Vrettos ◽  
Gábor Mező ◽  
Andreas G Tzakos
Keyword(s):  
Rational Design ◽  
Malignant Tumors ◽  
Building Blocks ◽  
Phase Iii ◽  
Peptide Drug ◽  
Phase Iii Clinical Trials ◽  
Drug Conjugates ◽  
Viable Approach ◽  
Peptide Drug Conjugates ◽  
Integral Knowledge

Cancer is the second leading cause of death affecting nearly one in two people, and the appearance of new cases is projected to rise by >70% by 2030. To effectively combat the menace of cancer, a variety of strategies have been exploited. Among them, the development of peptide–drug conjugates (PDCs) is considered as an inextricable part of this armamentarium and is continuously explored as a viable approach to target malignant tumors. The general architecture of PDCs consists of three building blocks: the tumor-homing peptide, the cytotoxic agent and the biodegradable connecting linker. The aim of the current review is to provide a spherical perspective on the basic principles governing PDCs, as also the methodology to construct them. We aim to offer basic and integral knowledge on the rational design towards the construction of PDCs through analyzing each building block, as also to highlight the overall progress of this rapidly growing field. Therefore, we focus on several intriguing examples from the recent literature, including important PDCs that have progressed to phase III clinical trials. Last, we address possible difficulties that may emerge during the synthesis of PDCs, as also report ways to overcome them.

Therapeutic potential of genus Pongamia and Derris: Phytochemical and bioactivity

2020 ◽  
Vol 20 ◽  
Author(s):  
Bharat Goel ◽  
Nancy Tripathi ◽  
Nivedita Bhardwaj ◽  
Bharat Sahu ◽  
Shreyans K. Jain
Keyword(s):  
Seed Oil ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Present Review ◽  
Skin Infections ◽  
Pharmacological Activities ◽  
Plant Parts ◽  
Phenolic Constituents ◽  
Anti Inflammatory

Abstract:: Genus Pongamia and Derris belong to the Leguminosae family and are reported synonymously in literature. Although many compounds have been isolated from different plant parts but seed oil is known to produce non-edible medicinally important furanoflavonoids. The seed oil, commonly known as Karanj oil in Ayurvedic and Siddha traditional systems of medicine, is reported for the treatment of various skin infections and psoriasis. Several phytopharmacological investigations have proved the medicinal potential of furanoflavonoids in skin and other disorders. Not only furanoflavonoids but several other important phenolic constituents such as chalcones, dibenzoylmethanes, aurones, isoflavones, flavanone dihydroflavonol, flavans, pterocarpans, rotenoids, coumarins, coumestans, stilbenoids and peltygynoids and their glycosides have been reported for different biological activities including antihyperglycemic, anti-inflammatory, anticancer, insecticidal, anti-alzheimer’s, gastroprotective, antifungal, antibacterial, etc. In the present review, the phytochemistry and pharmacological activities of the genera Pongamia and Derris have been summarized.

scholarly journals Multi-Therapeutic Potential of Naringenin (4′,5,7-Trihydroxyflavonone): Experimental Evidence and Mechanisms

Plants ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 1784
Author(s):  
Azher Arafah ◽  
Muneeb U. Rehman ◽  
Tahir Maqbool Mir ◽  
Adil Farooq Wali ◽  
Rayeesa Ali ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Biological Effects ◽  
Biological Properties ◽  
Primary Role ◽  
Citrus Fruits ◽  
Pharmacological Activities ◽  
Medicinal Properties

Extensive research has been carried out during the last few decades, providing a detailed account of thousands of discovered phytochemicals and their biological activities that have the potential to be exploited for a wide variety of medicinal purposes. These phytochemicals, which are pharmacologically important for clinical use, primarily consist of polyphenols, followed by terpenoids and alkaloids. There are numerous published reports indicating the primary role of phytochemicals proven to possess therapeutic potential against several diseases. However, not all phytochemicals possess significant medicinal properties, and only some of them exhibit viable biological effects. Naringenin, a flavanone found in citrus fruits, is known to improve immunity, repair DNA damage, and scavenge free radicals. Despite the very low bioavailability of naringenin, it is known to exhibit various promising biological properties of medicinal importance, including anti-inflammatory and antioxidant activities. This review focuses on the various aspects related to naringenin, particularly its physicochemical, pharmacokinetic, and pharmacodynamic properties. Furthermore, various pharmacological activities of naringenin, such as anticancer, antidiabetic, hepatoprotective, neuroprotective, cardioprotective, nephroprotective, and gastroprotective effects, have been discussed along with their mechanisms of action.

scholarly journals Phytochemical and Therapeutic Potential of Citrus grandis (L.) Osbeck: A Review

2021 ◽  
Vol 26 ◽  
pp. 2515690X2110437
Author(s):  
Rusat Jahin Anmol ◽  
Shabnam Marium ◽  
Fei Tsong Hiew ◽  
Wan Chien Han ◽  
Lee Kuan Kwan ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
The Body ◽  
Electrolyte Balance ◽  
Therapeutic Effects ◽  
Pharmacological Activities ◽  
Acridone Alkaloids ◽  
Citrus Maxima ◽  
Human Use ◽  
Sodium And Potassium

Citrus grandis or Citrus maxima, widely recognized as Pomelo is widely cultivated in many countries because of their large amounts of functional, nutraceutical and biological activities. In traditional medicine, various parts of this plant including leaf, pulp and peel are used for generations as they are scientifically proven to have therapeutic potentials and safe for human use. The main objective of this study was to review the different therapeutic applications of Citrus grandis and the phytochemicals associated with its medicinal values. In this article different pharmacological properties like antimicrobial, antitumor, antioxidant, anti-inflammatory, anticancer, antiepileptic, stomach tonic, cardiac stimulant, cytotoxic, hepatoprotective, nephroprotective, and anti-diabetic activities of the plant are highlighted. The enrichment of the fruit with flavonoids, polyphenols, coumarins, limonoids, acridone alkaloids, essential oils and vitamins mainly helps in exhibiting the pharmacological activities within the body. The vitamins enriched fruit is rich in nutritional value and also has minerals like calcium, phosphorous, sodium and potassium, which helps in maintaining the proper health and growth of the bones as well as the electrolyte balance of the body. To conclude, various potential therapeutic effects of Citrus grandis have been demonstrated in recent literature. Further studies on various parts of fruit, including pulp, peel, leaf, seed and it essential oil could unveil additional pharmacological activities which can be beneficial to the mankind.

Research and Development of Proteins and Peptides with Therapeutic Potential from Yam Tubers

2019 ◽  
Vol 20 (3) ◽  
pp. 277-284 ◽  
Author(s):  
Liang Zhang ◽  
Tzi Bun Ng ◽  
Jenny Ka Wing Lam ◽  
Shi Wei Wang ◽  
Lixing Lao ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Inflammatory Diseases ◽  
Biological Activities ◽  
Clinical Applications ◽  
Angiotensin I ◽  
Pharmacological Activities ◽  
Angiotensin I Converting Enzyme ◽  
Dioscorea Opposita ◽  
Dust Mite ◽  
Proteins And Peptides

We discuss the diverse biological activities, therapeutic potential, and clinical applications of peptides and proteins isolated from various yams species including Dioscorea opposita Thunb (Chinese yam), D alata, D japonica (Japanese yam), D pseudojaponica, D batatas (Korea yam), and D cayenensis. Yam peptides and proteins have many pharmacological activities including immunomodulatory, antioxidant, estrogen-stimulating, osteogenic, angiotensin I-converting enzyme inhibiting, carbonic anhydrase and trypsin inhibiting, chitinase, anti-insect, anti-dust mite, lectin, and anti-proliferative activities. Yam peptides and proteins have therapeutic potential for treating cardiovascular diseases, inflammatory diseases, cancers, aging disorders, menopause, and osteoporosis.

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