scholarly journals The potential for new and resilient anti-cancer drugs based upon minor groove binders for DNA

2021 ◽  
Vol 9 (11) ◽  
Author(s):  
Fraser Scott ◽  
Colin Suckling
Keyword(s):  
Anticancer Agents ◽  
Minor Groove ◽  
Minor Groove Binders ◽  
Development Of Resistance ◽  
Clostridioides Difficile ◽  
Anti Cancer ◽  
The University ◽  
Groove Binders

Anti-infective and anticancer drugs share the serious problem that over time resistance develops to their effects leading to clinical obsolescence. Research at the University of Strathclyde has discovered a platform of anti-infective drugs based upon minor groove binders for DNA that have exceptional resilience to the development of resistance in their target organisms (bacteria, fungi, and parasites). This property is associated with the fact that the Strathclyde minor groove binders (S-MGBs) act at more than one discrete molecular target. One of the compounds has successfully completed a phase IIa clinical trial for the treatment of Clostridioides difficile infections. Several other compounds have shown activity against a number of cancer cell lines in vitro with indications of in vivo activity in a mouse model of lung cancer. This paper places these discoveries in the context of previous studies of minor groove binders as anticancer agents and considers whether the benefits of multitargeting successfully demonstrated in anti-infective applications can be translated to anticancer applications.

scholarly journals Selective in vitro anti-cancer activity of non-alkylating minor groove binders

MedChemComm ◽  
2019 ◽  
Vol 10 (9) ◽  
pp. 1620-1634 ◽  
Author(s):  
Ryan J. O. Nichol ◽  
Abedawn I. Khalaf ◽  
Kartheek Sooda ◽  
Omar Hussain ◽  
Hollie B. S. Griffiths ◽  
...  
Keyword(s):  
Minor Groove ◽  
Minor Groove Binders ◽  
Anti Cancer ◽  
Groove Binders ◽  
Cancer Activity

We describe the synthesis and evaluation of Strathclyde Minor Groove Binders (S-MGBs) as selective anti-cancer agents which act through a non-alkylating mechanism.

scholarly journals Dihydrotanshinone Inhibits Hepatocellular Carcinoma by Suppressing the JAK2/STAT3 Pathway

2021 ◽  
Vol 12 ◽  
Author(s):  
Xue Hu ◽  
Fangzhou Jiao ◽  
Lan Zhang ◽  
Yingan Jiang
Keyword(s):  
Hepatocellular Carcinoma ◽  
Anticancer Agents ◽  
Nuclear Translocation ◽  
Clinical Investigation ◽  
Stat3 Pathway ◽  
Development Of Resistance ◽  
Liver Cancers ◽  
Induced Apoptosis

Liver cancer is the sixth most commonly diagnosed cancer and the fourth leading cause of cancer death. Most (75–85%) primary liver cancers occurring worldwide are hepatocellular carcinoma (HCC). The development of resistance and other drug related side effects are the prime reasons for the failure of treatment. Therefore, developing high-efficacy and low-toxicity natural anticancer agents is greatly needed in the treatment of HCC. Dihydrotanshinone (DHTS) is widely used for promoting blood circulation and antitumor. The aim of the present study was to investigate the effect and mechanism of DHTS-induced apoptosis of HCC, both in vitro and in vivo. We found that DHTS inhibited the growth of several HCC cells (HCCLM3, SMMC7721, Hep3B and HepG2). DHTS induced the apoptosis of SMMC7721 cells. Immunofluorescence results have showed that DHTS decreased STAT3 nuclear translocation. Moreover, Western blot results have demonstrated that DHTS suppressed the activation of JAK2/STAT3 signaling pathway. In addition, xenograft results have showed that DHTS suppressed tumor growth of SMMC7721 cells in vivo by inhibiting the p-STAT3. Thus, we demonstrated that DHTS could inhibit HCC by suppressing the JAK2/STAT3 pathway. DHTS has potential to be a chemotherapeutic agent in HCC and merits further clinical investigation.

scholarly journals Correction to “Novel Minor Groove Binders Cure Animal African Trypanosomiasis in an in Vivo Mouse Model”

2021 ◽  
Author(s):  
Federica Giordani ◽  
Abedawn I. Khalaf ◽  
Kirsten Gillingwater ◽  
Jane C. Munday ◽  
Harry P. de Koning ◽  
...  
Keyword(s):  
Mouse Model ◽  
Minor Groove ◽  
African Trypanosomiasis ◽  
Animal African Trypanosomiasis ◽  
Minor Groove Binders ◽  
Groove Binders

Ursolic and Oleanolic Acids as Potential Anticancer Agents Acting in the Gastrointestinal Tract

2018 ◽  
Vol 16 (1) ◽  
pp. 78-91 ◽  
Author(s):  
Mateusz Pięt ◽  
Roman Paduch
Keyword(s):  
Gastrointestinal Tract ◽  
Side Effects ◽  
Anticancer Agents ◽  
In Vivo Studies ◽  
Pentacyclic Triterpenoids ◽  
Liver Cancers ◽  
Anti Cancer ◽  
Tumorigenic Activity

Background:Cancer is one of the main causes of death worldwide. Contemporary therapies, including chemo- and radiotherapy, are burdened with severe side effects. Thus, there exists an urgent need to develop therapies that would be less devastating to the patient’s body. Such novel approaches can be based on the anti-tumorigenic activity of particular compounds or may involve sensitizing cells to chemotherapy and radiotherapy or reducing the side-effects of regular treatment.Objective:Natural-derived compounds are becoming more and more popular in cancer research. Examples of such substances are Ursolic Acid (UA) and Oleanolic Acid (OA), plant-derived pentacyclic triterpenoids which possess numerous beneficial properties, including anti-tumorigenic activity.Results:In recent years, ursolic and oleanolic acids have been demonstrated to exert a range of anticancer effects on various types of tumors. These compounds inhibit the viability and proliferation of cancer cells, prevent their migration and metastasis and induce their apoptosis. Both in vitro and in vivo studies indicate that UA and OA are promising anti-cancer agents that can prevent carcinogenesis at each step. Furthermore, cancers at all stages are susceptible to the activity of these compounds. </P><P> Neoplasms that are formed in the gastrointestinal tract, i.e. gastric, colorectal, pancreatic, and liver cancers, are among the most common and most lethal malignancies. Their localization in the digestive system, however, facilitates the action of orally-administered (potential) anti-cancer agents, making chemopreventive drugs more accessible.In this paper, the anti-tumorigenic effect of ursolic and oleanolic acids on gastric, colon, pancreatic, and liver cancers, as well as the mechanisms underlying this process, are presented.

Current developments in the Pyran-Based Analogues as Anticancer Agents

2021 ◽  
Vol 21 ◽  
Author(s):  
Parul Grover ◽  
Monika Bhardwaj ◽  
Lovekesh Mehta ◽  
Garima Kapoor ◽  
Pooja A. Chawla
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Anticancer Compounds ◽  
Appropriate Treatment ◽  
Anti Cancer ◽  
Privileged Structure ◽  
Different Types

: Heterocyclic compounds offer an enormous area for new lead molecules for drug discovery. Till today, efforts are being continuously made to find appropriate treatment for the management of the deadly disease of cancer. Amongst the large number of heterocycles that are found in nature, heterocycles having oxygen obtained noteworthy attention due to their distinctive and pharmacological activities.‘Pyran’ is one of the most significant non-aromatic, six-membered ring composed of one oxygen atom and five carbon atoms. It is considered a privileged structure since pyran and its related derivatives exhibit a wide spectrum of biological activities. Pyran derivatives are found to have excellent anti-cancer properties against various types of cancer. The present review focussed on the current advances in different types of pyran-based derivatives as anti-cancer agents. Various in-vitro (cell based testing), in-vivo (animal based testing) models as well as molecular docking along with results are also covered. A subsection describing briefly natural pyran containing anticancer compounds is also incorporated in the review.

Drug Delivery Systems For Anti-Cancer Active Complexes of Some Coinage Metals

2018 ◽  
Vol 25 (4) ◽  
pp. 493-505 ◽  
Author(s):  
Ming Zhang ◽  
Camille Saint-Germain ◽  
Guiling He ◽  
Raymond Wai-Yin Sun
Keyword(s):  
Drug Delivery ◽  
Metal Complexes ◽  
Drug Delivery Systems ◽  
Platinum Complexes ◽  
Delivery Systems ◽  
Development Of Resistance ◽  
Anti Cancer ◽  
Coinage Metals

Background: Although cisplatin and a number of platinum complexes have widely been used for the treatment of neoplasia, patients receiving these treatments have frequently suffered from their severe toxic side effects, the development of resistance with consequent relapse. In the recent decades, numerous complexes of coinage metals including that of gold, copper and silver have been reported to display promising in vitro and/or in vivo anti-cancer activities as well as potent activities towards cisplatin-resistant tumors. Nevertheless, the medical development of these metal complexes has been hampered by their instability in aqueous solutions and the nonspecific binding in biological systems. Methods: One of the approaches to overcome these problems is to design and develop adequate drug delivery systems (DDSs) for the transport of these complexes. By functionalization, encapsulation or formulation of the metal complexes, several types of DDSs have been reported to improve the desired pharmacological profile of the metal complexes, improving their overall stability, bioavailability, anti-cancer activity and reducing their toxicity towards normal cells. Conclusion: In this review, we summarized the recent findings for different DDSs for various anti- cancer active complexes of some coinage metals.

scholarly journals New Bis(2-aminoimidazoline) and Bisguanidine DNA Minor Groove Binders with Potent in Vivo Antitrypanosomal and Antiplasmodial Activity

2008 ◽  
Vol 51 (4) ◽  
pp. 909-923 ◽  
Author(s):  
Fernando Rodríguez ◽  
Isabel Rozas ◽  
Marcel Kaiser ◽  
Reto Brun ◽  
Binh Nguyen ◽  
...  
Keyword(s):  
Minor Groove ◽  
Antiplasmodial Activity ◽  
Dna Minor Groove ◽  
Minor Groove Binders ◽  
Groove Binders

scholarly journals Novel Minor Groove Binders Cure Animal African Trypanosomiasis in an in Vivo Mouse Model

2019 ◽  
Vol 62 (6) ◽  
pp. 3021-3035
Author(s):  
Federica Giordani ◽  
Abedawn I. Khalaf ◽  
Kirsten Gillingwater ◽  
Jane C. Munday ◽  
Harry P. de Koning ◽  
...  
Keyword(s):  
Mouse Model ◽  
Minor Groove ◽  
African Trypanosomiasis ◽  
Animal African Trypanosomiasis ◽  
Minor Groove Binders ◽  
Groove Binders

Ethnomedicinal uses, Phytochemistry and Pharmacological Aspects of the Genus Berberis Linn: A Comprehensive Review

2020 ◽  
Vol 23 ◽  
Author(s):  
Roohi Mohi-ud-din ◽  
Reyaz Hassan Mir ◽  
Prince Ahad Mir ◽  
Saeema Farooq ◽  
Syed Naiem Raza ◽  
...  
Keyword(s):  
Chemical Constituents ◽  
Pharmacological Activities ◽  
Traditional Use ◽  
Comprehensive Review ◽  
Wide Range ◽  
Anti Cancer ◽  
Comprehensive Survey ◽  
Ethnomedicinal Uses

Background: Genus Berberis (family Berberidaceae), which contains about 650 species and 17 genera worldwide, has been used in folklore and various traditional medicine systems. Berberis Linn. is the most established group among genera with around 450-500 species across the world. This comprehensive review will not only help researchers for further evaluation but also provide substantial information for future exploitation of species to develop novel herbal formulations. Objective: The present review is focussed to summarize and collect the updated review of information of Genus Berberis species reported to date regarding their ethnomedicinal information, chemical constituents, traditional/folklore use, and reported pharmacological activities on more than 40 species of Berberis. Conclusion: A comprehensive survey of the literature reveals that various species of the genus possess various phytoconstituents mainly alkaloids, flavonoid based compounds isolated from different parts of a plant with a wide range of pharmacological activities. So far, many pharmacological activities like anti-cancer, anti-hyperlipidemic, hepatoprotective, immunomodulatory, anti-inflammatory both in vitro & in vivo and clinical study of different extracts/isolated compounds of different species of Berberis have been reported, proving their importance as a medicinal plant and claiming their traditional use.

Ferula hermonis: A Review of Current Use and Pharmacological Studies of its Sesquiterpene Ester Ferutinin

2020 ◽  
Vol 21 (5) ◽  
pp. 499-508 ◽  
Author(s):  
Rémi Safi ◽  
Marwan El-Sabban ◽  
Fadia Najjar
Keyword(s):  
Wide Spectrum ◽  
Endemic Plant ◽  
Anti Cancer ◽  
Pharmacological Studies ◽  
Sexual Impotence ◽  
Novel Applications ◽  
Anti Fungal ◽  
Sesquiterpene Ester

Ferula hermonis Boiss, is an endemic plant of Lebanon, locally known as “shilsh Elzallouh”. It has been extensively used in the traditional medicine as an aphrodisiac and for the treatment of sexual impotence. Crude extracts and isolated compounds of ferula hermonis contain phytoestrogenic substances having a wide spectrum of in vitro and in vivo pharmacological properties including anti-osteoporosis, anti-inflammatory, anti-microbial and anti-fungal, anti-cancer and as sexual activity enhancer. The aim of this mini-review is to highlight the traditional and novel applications of this plant’s extracts and its major sesquiterpene ester, ferutinin. The phytochemical constituents and the pharmacological uses of ferula hermonis crude extract and ferutinin specifically will be discussed.

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