Cucurbitacins as Anticancer Agents: A Patent Review

2019 ◽  
Vol 14 (2) ◽  
pp. 133-143 ◽  
Author(s):  
Hidayat Hussain ◽  
Ivan R. Green ◽  
Muhammad Saleem ◽  
Khanzadi F. Khattak ◽  
Muhammad Irshad ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Wide Spectrum ◽  
Biological Effects ◽  
Therapeutic Effects ◽  
Cytotoxic Effects ◽  
Natural Sources ◽  
Oh Groups ◽  
Drug Candidates ◽  
The Past ◽  
Wide Range

Background: Cucurbitacins belong to a group of tetracyclic triterpenoids that display a wide range of biological effects. In the past, numerous cucurbitacins have been isolated from natural sources and many active compounds have been synthesized using the privileged scaffold in order to enhance its cytotoxic effects. Objective: his review covers patents on the therapeutic effects of natural cucurbitacins and their synthetic analogs published during the past decade. By far, the majority of patents published are related to cancer and Structure-Activity Relationships (SAR) of these compounds are included to lend gravitas to this important class of natural products. Methods: The date about the published patents was downloaded via online open access patent databases. Results: Cucurbitacins display significant cytotoxic properties, in particular cucurbitacins B and D which possess very potent effects towards a number of cancer cells. Numerous cucurbitacins isolated from natural sources have been derivatized through chemical modification at the C(2)-OH and C(25)- OH groups. Most importantly, an acyl ester of the C(25)-OH and, iso-propyl, n-propyl and ethyl ether groups of the C(2)-OH demonstrated the most increased cytotoxic activity. Conclusion: The significant cytotoxic effects of natural and semi-synthetic cucurbitacins make them attractive as new drug candidates. Moreover, cucurbitacins have the capability to form conjugates with other anticancer drugs which will synergistically enhance their anticancer effects. The authors believe that in order to get lead compounds, there should be a greater focus on the synthesis of homodimers, heterodimers, and halo derivatives of cucurbitacins. In the opinion of the authors the analysis of the published patents on the cucurbitacins indicates that these compounds can be developed into a regimen to treat a wide spectrum of cancers.

Autophagy-regulating N-heterocycles derivatives as potential anticancer agents

2020 ◽  
Vol 12 (3) ◽  
pp. 223-242 ◽  
Author(s):  
Xiaoxia Liang ◽  
Li Zhang ◽  
Fanglong Li ◽  
Shangxian Luan ◽  
Changliang He ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Structural Features ◽  
New Drugs ◽  
Therapeutic Effects ◽  
Antitumor Activities ◽  
Antitumor Therapy ◽  
Drug Candidates ◽  
The Past ◽  
First Time

As a double-edged sword, autophagy in cancer cells could either suppress or promote tumorigenesis. Nowadays, more and more natural compounds with autophagy-regulating activities exhibit therapeutic effects against various cancers. N-Heterocycle derivatives plays an important role for discovery new drugs. In this review, we summarize and classify 116 N-heterocycle derivatives with autophagy-regulating activities in the past decade into 12 classes according to structure characteristics. The structural features, bioactivities, mechanism and problems faced in this field are discussed and reported for the first time. Some of these even exhibited outstanding in vivo antitumor activities, including bisaminoquinoline (3), pancratistatin (8), 10-hydroxyevodiamine (18), lycorine (28), piperine (31) and iridium (III) complex (57), which are potential drug candidates for antitumor therapy.

Therapeutic Perspectives of Food Bioactive Peptides: A Mini Review

2019 ◽  
Vol 26 (9) ◽  
pp. 664-675
Author(s):  
Sulochana Priya
Keyword(s):  
Bioactive Peptides ◽  
Marine Organism ◽  
Biological Effects ◽  
Amide Bond ◽  
Therapeutic Effects ◽  
Specific Sequence ◽  
The Past ◽  
Cancer Immunity ◽  
Microbial Infections ◽  
Diverse Origin

Bioactive peptides are short chain of amino acids (usually 2-20) that are linked by amide bond in a specific sequence which have some biological effects in animals or humans. These can be of diverse origin like plant, animal, fish, microbe, marine organism or even synthetic. They are successfully used in the management of many diseases. In recent years increased attention has been raised for its effects and mechanism of action in various disease conditions like cancer, immunity, cardiovascular disease, hypertension, inflammation, diabetes, microbial infections etc. Bioactive peptides are more bioavailable and less allergenic when compared to total proteins. Food derived bioactive peptides have health benefits and its demand has increased tremendously over the past decade. This review gives a view on last two years research on potential bioactive peptides derived from food which have significant therapeutic effects.

Synthesis and Antibacterial / Anticancer Activities of Compounds Containing Pyrazole Ring Linked to Piperazines

2020 ◽  
Vol 16 (4) ◽  
pp. 419-431
Author(s):  
Kishore K. Valluri ◽  
Tejeswara R. Allaka ◽  
IV Kasi Viswanath ◽  
Nagaraju PVVS
Keyword(s):  
Cell Line ◽  
Cancer Cell ◽  
Anticancer Agents ◽  
Cancer Cell Line ◽  
Pyrazole Ring ◽  
Therapeutic Effects ◽  
Anticancer Activities ◽  
Human Colon Cancer ◽  
Parent Molecule ◽  
Wide Range

Background: Many pyrazole piperazine derivatives are known to exhibit a wide range, thus being attractive for the drug design and synthesis of interesting class of widely studied heterocyclic compounds. It is therefore necessary to devote continuing effort for the identification and development of New Chemical Entities (NCEs) as potential antibacterial and anticancer agents to address serious health problems. Methods: A series of new compounds containing pyrazole ring linked to a piperazine hydrochloride moiety were synthesized and screened for their antibacterial activity, cytotoxicity of novel scaffolds are described by variation in therapeutic effects of parent molecule. The structure variants were characterized by using a blend of spectroscopic 1H NMR, 13C NMR, IR, Mass and chromatographic techniques. Results: When tested for in vitro antibacterial and anticancer activities, several of these compounds showed good activities. The target compounds 9b, 9a and 9e exhibited a high degree of anticancer activity against human colon cancer cell line Caco-2 and human breast cancer cell line MDAMB231. Further, 9a, 9b, 9d, and 9h showed better activity towards four medically relevant organisms; Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Klebsiella Species compared to CPF. In the present investigation, cheminfomatics tools Molinspiration, 2003 and MolSoft, 2007 for the prediction of insilico molecular properties and drug likeness for the target compounds 9a-h was evaluated and positive results were observed. Conclusion: Our study revealed that the molecular framework presented here could be a useful template for the identification of novel small molecules as promising antibacterial/ anticancer agents.

scholarly journals Modern Synthetic Methods for the Stereoselective Construction of 1,3-Dienes

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 249
Author(s):  
Raquel G. Soengas ◽  
Humberto Rodríguez-Solla
Keyword(s):  
Organic Chemistry ◽  
Natural Products ◽  
Functional Group ◽  
Biological Activities ◽  
Synthetic Methods ◽  
Bond Forming ◽  
Drug Candidates ◽  
The Past ◽  
Wide Range

The 1,3-butadiene motif is widely found in many natural products and drug candidates with relevant biological activities. Moreover, dienes are important targets for synthetic chemists, due to their ability to give access to a wide range of functional group transformations, including a broad range of C-C bond-forming processes. Therefore, the stereoselective preparation of dienes have attracted much attention over the past decades, and the search for new synthetic protocols continues unabated. The aim of this review is to give an overview of the diverse methodologies that have emerged in the last decade, with a focus on the synthetic processes that meet the requirements of efficiency and sustainability of modern organic chemistry.

scholarly journals Cannabidiol: from an inactive cannabinoid to a drug with wide spectrum of action

2008 ◽  
Vol 30 (3) ◽  
pp. 271-280 ◽  
Author(s):  
Antonio Waldo Zuardi
Keyword(s):  
Chemical Structure ◽  
Web Of Science ◽  
Inflammatory Diseases ◽  
Wide Spectrum ◽  
Therapeutic Effects ◽  
Neuroprotective Effects ◽  
Wide Range ◽  
Sedative Effects ◽  
Therapeutic Properties ◽  
Number Of Publications

OBJECTIVE: The aim of this review is to describe the historical development of research on cannabidiol. METHOD: This review was carried out on reports drawn from Medline, Web of Science and SciELO. DISCUSSION: After the elucidation of the chemical structure of cannabidiol in 1963, the initial studies showed that cannabidiol was unable to mimic the effects of Cannabis. In the 1970's the number of publications on cannabidiol reached a first peak, having the research focused mainly on the interaction with delta9-THC and its antiepileptic and sedative effects. The following two decades showed lower degree of interest, and the potential therapeutic properties of cannabidiol investigated were mainly the anxiolytic, antipsychotic and on motor diseases effects. The last five years have shown a remarkable increase in publications on cannabidiol mainly stimulated by the discovery of its anti-inflammatory, anti-oxidative and neuroprotective effects. These studies have suggested a wide range of possible therapeutic effects of cannabidiol on several conditions, including Parkinson's disease, Alzheimer's disease, cerebral ischemia, diabetes, rheumatoid arthritis, other inflammatory diseases, nausea and cancer. CONCLUSION: In the last 45 years it has been possible to demonstrate that CBD has a wide range of pharmacological effects, many of which being of great therapeutic interest, but still waiting to be confirmed by clinical trials.

scholarly journals Andrographolide, an Anti-Inflammatory Multitarget Drug: All Roads Lead to Cellular Metabolism

Molecules ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 5
Author(s):  
Rafael Agustín Burgos ◽  
Pablo Alarcón ◽  
John Quiroga ◽  
Carolina Manosalva ◽  
Juan Hancke
Keyword(s):  
Clinical Studies ◽  
Biological Effects ◽  
Metabolic Effects ◽  
Therapeutic Effects ◽  
Related Factor ◽  
Wide Range ◽  
Labdane Diterpene ◽  
Upper Respiratory ◽  
Anti Inflammatory ◽  
Preclinical And Clinical Studies

Andrographolide is a labdane diterpene and the main active ingredient isolated from the herb Andrographis paniculata. Andrographolide possesses diverse biological effects including anti-inflammatory, antioxidant, and antineoplastic properties. Clinical studies have demonstrated that andrographolide could be useful in therapy for a wide range of diseases such as osteoarthritis, upper respiratory diseases, and multiple sclerosis. Several targets are described for andrographolide, including the interference of transcription factors NF-κB, AP-1, and HIF-1 and signaling pathways such as PI3K/Akt, MAPK, and JAK/STAT. In addition, an increase in the Nrf2 (nuclear factor erythroid 2–related factor 2) signaling pathway also supports its antioxidant and anti-inflammatory properties. However, this scenario could be more complex since recent evidence suggests that andrographolide targets can modulate glucose metabolism. The metabolic effect of andrographolide might be the key to explaining the diverse therapeutic effects described in preclinical and clinical studies. This review discusses some of the most recent evidence about the anti-inflammatory and metabolic effects of andrographolide.

scholarly journals Unicellular Eukaryote as a Bio-cellular Model for Studying Effect Benzimidazole: Ultrastructural Analysis

2021 ◽  
Vol 4 (1) ◽  
Author(s):  
Karlen O Hovnanyan
Keyword(s):  
Mechanism Of Action ◽  
Wide Spectrum ◽  
Biological Effects ◽  
Unicellular Eukaryote ◽  
Electron Microscopic ◽  
Cystic Form ◽  
Ultrastructural Characterization ◽  
Wide Range ◽  
First Time ◽  
Derivatives Of

The search for new derivatives of benzoimidazole with an active center that have a wide range of biological effects (antifungal, antiflammatory, antibacterial, antiviral, antitumor, antidiabetic, etc.) is the subject of modern pharmaceutical science. To determine the mechanism of action of benzoimidazole, a search is underway for more. We have previously carried out the Ultrastructural characterization of various prokaryotes and protists, as well as the mechanism of action of antibiotics and chemical preparations on them. From a series of heterocyclic drugs, a drug with a wide spectrum of action was chosen as derivatives of benzimidazole and a model of a free-living unicellular eukaryote Endameba moshkovskii with a vegetative and cystic form. The purpose of this work is the nature of the action of drugs of the benzimidazole series and in the ultrastructural visualization of the mechanism of action of benzimidazole using electron microscopic and electron-cytochemical methods on the model of polyxenic cultures of unicellular eukaryotes Entamoeba moshkovskii. We have established for the first time the excising effect of benzimidazole and the functional-ultrastructural mechanism of the action of benzimidazole on entameoba cells. As a result, the ultrastructural and functional morphology of benzimidazole action in the process of excysting entamoeba was established.

scholarly journals Hydrogen, a Novel Therapeutic Molecule, Regulates Oxidative Stress, Inflammation, and Apoptosis

2021 ◽  
Vol 12 ◽  
Author(s):  
Yan Tian ◽  
Yafang Zhang ◽  
Yu Wang ◽  
Yunxi Chen ◽  
Weiping Fan ◽  
...  
Keyword(s):  
Treatment Guidelines ◽  
Ischemia Reperfusion Injury ◽  
Inflammatory Diseases ◽  
Biological Effects ◽  
Ischemia Reperfusion ◽  
Underlying Mechanism ◽  
Therapeutic Effects ◽  
Mitochondrial Energy Metabolism ◽  
Wide Range ◽  
Anti Inflammatory

Molecular hydrogen (H2) is a colorless and odorless gas. Studies have shown that H2 inhalation has the therapeutic effects in many animal studies and clinical trials, and its application is recommended in the novel coronavirus pneumonia treatment guidelines in China recently. H2 has a relatively small molecular mass, which helps it quickly spread and penetrate cell membranes to exert a wide range of biological effects. It may play a role in the treatment and prevention of a variety of acute and chronic inflammatory diseases, such as acute pancreatitis, sepsis, respiratory disease, ischemia reperfusion injury diseases, autoimmunity diseases, etc.. H2 is primarily administered via inhalation, drinking H2-rich water, or injection of H2 saline. It may participate in the anti-inflammatory and antioxidant activity (mitochondrial energy metabolism), immune system regulation, and cell death (apoptosis, autophagy, and pyroptosis) through annihilating excess reactive oxygen species production and modulating nuclear transcription factor. However, the underlying mechanism of H2 has not yet been fully revealed. Owing to its safety and potential efficacy, H2 has a promising potential for clinical use against many diseases. This review will demonstrate the role of H2 in antioxidative, anti-inflammatory, and antiapoptotic effects and its underlying mechanism, particularly in coronavirus disease-2019 (COVID-19), providing strategies for the medical application of H2 for various diseases.

Idronoxil as an Anticancer Agent: Activity and Mechanisms

2020 ◽  
Vol 20 (5) ◽  
pp. 341-354 ◽  
Author(s):  
Kate Porter ◽  
Walter Douglas Fairlie ◽  
Olivier Laczka ◽  
Frederic Delebecque ◽  
John Wilkinson
Keyword(s):  
Biological Effects ◽  
Cancer Therapies ◽  
Cellular Targets ◽  
The Past ◽  
Cycle Arrest ◽  
Anticancer Effects ◽  
Wide Range ◽  
Inhibition Of Angiogenesis ◽  
The Subject ◽  
Second Chance

Idronoxil has been the subject of more than 50 peer-reviewed publications over the last two decades. This isoflavone is an intriguing regulator of multiple signal transduction pathways, capable of causing a range of biological effects, including cell cycle arrest, apoptosis, an ability to stimulate the immune system, and inhibition of angiogenesis. These multifaceted actions suggest that idronoxil has the potential to synergize with, or complement, a wide range of cancer therapies. Whilst clinically tested in the past, idronoxil’s journey was discontinued as a result of its low bioavailability in humans when administered either intravenously or orally, though strategies to overcome this issue are currently being explored. Here, we summarize the current literature regarding the key cellular targets of idronoxil and the mechanisms by which idronoxil exerts its anticancer effects, laying a new foundation toward giving this unique molecule a second chance of contributing to the future of cancer treatment.

scholarly journals Review on Ethnomedicinal uses of Memory Boosting Herb, Butterfly Pea, Clitoria ternatea

2015 ◽  
Vol 15 (2) ◽  
pp. 71 ◽  
Author(s):  
Piya Kosai ◽  
Kanjana Sirisidthi ◽  
Kanitta Jiraungkoorskul ◽  
Wannee Jiraungkoorskul
Keyword(s):  
Wide Spectrum ◽  
Biological Effects ◽  
Pharmacological Activities ◽  
Medicinal Uses ◽  
Clitoria Ternatea ◽  
Wide Range ◽  
Butterfly Pea ◽  
Anti Fungal ◽  
Anticonvulsant Activities ◽  
Ethnomedicinal Uses

<em>Clitoria ternatea</em> (Family: Fabaceae) is one of the traditional medicinal plants used as “Shanka Pushpi” an Ayurvedic medicine used to boost or enhance neurological health. The plant contains alkaloid, flavonoid, taraxerol, taraxerone, triterpenoid and anthocyanin as active chemicals that bring about its biological effects. Its extracts possess a wide range of pharmacological activities including antibacterial, anti-diabetic, anti-diarrheal, anti-fungal, anti-helmintic, anti-inflammatory, antimicrobial, antioxidant, and antipyretic activities, hypolipidemia, immunomodulatory, and wound healing. This review is an attempt to compile information on various ethno medicinal uses of memory boosting herb, butterfly pea, <em>Clitoria ternatea</em>. <strong>Conclusion</strong>: It has a wide spectrum of neuro pharmacological benefits such as nootropic, anti-depressant, anti-stress, anxiolytic, and anticonvulsant activities.

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