Abstract C218: Novel therapeutic potential in targeting micro tubules by naturally occurring anti cancer agent withaferin A in human cancers.

Author(s):  
Kamalini Ghosh ◽  
Sumita Sengupta
Biomedicines ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 33
Author(s):  
Hee Ra Jung ◽  
Seongman Jo ◽  
Min Jae Jeon ◽  
Hyelim Lee ◽  
Yeonjeong Chu ◽  
...  

In cancer immunotherapy, the cyclic GMP–AMP synthase–stimulator of interferon genes (STING) pathway is an attractive target for switching the tumor immunophenotype from ‘cold’ to ‘hot’ through the activation of the type I interferon response. To develop a new chemical entity for STING activator to improve cyclic GMP-AMP (cGAMP)-induced innate immune response, we identified KAS-08 via the structural modification of DW2282, which was previously reported as an anti-cancer agent with an unknown mechanism. Further investigation revealed that direct STING binding or the enhanced phosphorylation of STING and downstream effectors were responsible for DW2282-or KAS-08-mediated STING activity. Furthermore, KAS-08 was validated as an effective STING pathway activator in vitro and in vivo. The synergistic effect of cGAMP-mediated immunity and efficient anti-cancer effects successfully demonstrated the therapeutic potential of KAS-08 for combination therapy in cancer treatment.


2020 ◽  
Vol 16 ◽  
Author(s):  
Mohammed Asadullah Jahangir ◽  
Mohamad Taleuzzaman ◽  
Sarwar Beg ◽  
Surajpal Verma ◽  
Sadaf Jamal Gilani ◽  
...  

: Eugenol is a bioactive compound frequently available in many herbal plants. The different sources reported for eugenol are clove, cinnamon, holy basil, and pepper. There are several therapeutic activities reported for eugenol as antioxidant, antimicrobial, anesthetic, antiinflammatory, anti-carcinogenic, neuroprotective agent, anti-diabetic and anti-cancer agent. However, due to limited aqueous solubility they have poor bioavailability. Their therapeutic potential has been enhanced with the eugenol nano-formulations developed as liposome, nanoparticles, microemulsions and micelles. This article extensively reviews the chemical properties, pharmacological properties, andeugenol nano-formulations with their biological activity.


Toxicon ◽  
2012 ◽  
Vol 60 (2) ◽  
pp. 107
Author(s):  
J. Michael Conlon ◽  
Milena Mechkarska ◽  
Kholoud Arafat ◽  
Samir Attoub

2020 ◽  
Vol 26 (1) ◽  
pp. 46-59 ◽  
Author(s):  
Ali Irfan ◽  
Laila Rubab ◽  
Mishbah Ur Rehman ◽  
Rukhsana Anjum ◽  
Sami Ullah ◽  
...  

AbstractCoumarin sulfonamide is a heterocyclic pharmacophore and an important structural motif which is a core and integral part of different therapeutic scaffolds and analogues. Coumarin sulfonamides are privileged and pivotal templates which have a broad spectrum of applications in the fields of medicine, pharmacology and pharmaceutics. Coumarin sulfonamide exhibited versatile and myriad biomedical activities such as anti-bacterial, antiviral, antifungal, anti-inflammatory and anti-cancer. This review article focuses on the structural features of coumarin sulfonamide derivatives in the treatment of different lethal diseases on the basis of structure-activity relationships (SAR). The plethora of research cited in this review article summarizes and discusses the various substitutions around the coumarin sulfonamide nucleus which have provided a wide spectrum of biological activities and therapeutic potential that has proved attractive to many researchers looking to exploit the coumarin sulfonamide skeleton for drug discovery and the development of novel therapeutic agents.


Biomolecules ◽  
2020 ◽  
Vol 10 (6) ◽  
pp. 831 ◽  
Author(s):  
Ching-Shu Lai ◽  
Chi-Tang Ho ◽  
Min-Hsiung Pan

In recent decades, cancer has been one of the leading causes of death worldwide. Despite advances in understanding the molecular basis of tumorigenesis, diagnosis, and clinical therapies, the discovery and development of effective drugs is an active and vital field in cancer research. Tetrahydrocurcumin is a major curcuminoid metabolite of curcumin, naturally occurring in turmeric. The interest in tetrahydrocurcumin research is increasing because it is superior to curcumin in its solubility in water, chemical stability, bioavailability, and anti-oxidative activity. Many in vitro and in vivo studies have revealed that tetrahydrocurcumin exerts anti-cancer effects through various mechanisms, including modulation of oxidative stress, xenobiotic detoxification, inflammation, proliferation, metastasis, programmed cell death, and immunity. Despite the pharmacological similarities between tetrahydrocurcumin and curcumin, the structure of tetrahydrocurcumin determines its distinct and specific molecular mechanism, thus making it a potential candidate for the prevention and treatment of cancers. However, the utility of tetrahydrocurcumin is yet to be evaluated as only limited pharmacokinetic and oral bioavailability studies have been performed. This review summarizes research on the anti-cancer properties of tetrahydrocurcumin and describes its mechanisms of action.


2013 ◽  
Vol 6 ◽  
pp. IJTR.S12094 ◽  
Author(s):  
Hollie E. Flick ◽  
Judith M. LaLonde ◽  
William P. Malachowski ◽  
Alexander J. Muller

β-lapachone is a naturally occurring 1,2-naphthoquinone-based compound that has been advanced into clinical trials based on its tumor-selective cytotoxic properties. Previously, we focused on the related 1,4-naphthoquinone pharmacophore as a basic core structure for developing a series of potent indoleamine 2,3-dioxygenase 1 (IDO1) enzyme inhibitors. In this study, we identified IDO1 inhibitory activity as a previously unrecognized attribute of the clinical candidate β-lapachone. Enzyme kinetics-based analysis of β-lapachone indicated an uncompetitive mode of inhibition, while computational modeling predicted binding within the IDO1 active site consistent with other naphthoquinone derivatives. Inhibition of IDO1 has previously been shown to breach the pathogenic tolerization that constrains the immune system from being able to mount an effective anti-tumor response. Thus, the finding that β-lapachone has IDO1 inhibitory activity adds a new dimension to its potential utility as an anti-cancer agent distinct from its cytotoxic properties, and suggests that a synergistic benefit can be achieved from its combined cytotoxic and immunologic effects.


2019 ◽  
Vol 18 (12) ◽  
pp. 1650-1655 ◽  
Author(s):  
Mohammad Saleem ◽  
Jawaria Asif ◽  
Muhammad Asif ◽  
Uzma Saleem

Background: Amygdalin is a cyanogenic glycoside which is described as a naturally occurring anticancer agent. Current review highlights apoptosis-inducing attributes of amygdalin towards different cancers and its potential application as an anti-cancer agent in cancer therapy. Method: Data about amygdalin was retrieved from all major scientific databases i.e., PubMed, ScienceDirect, Google Scholar, Scopus and Medline by using combination of keywords like amygdalin, apoptosis, laetrile, vitamin B- 17, pro-apoptotic proteins, anti-apoptotic proteins, hydrogen cyanide, mechanism of action of amygdalin and amygdalin therapy on humans. However, no specific time frame was followed for collection of data. Results: Data collected from already published articles revealed that apoptosis is a central process activated by amygdalin in cancer cells. It is suggested to stimulate apoptotic process by upregulating expression of Bax (proapoptotic protein) and caspase-3 and downregulating expression of Bcl-2 (anti-apoptotic protein). It also promotes arrest of cell cycle in G0/G1 phase and decrease number of cells entering S and G2/M phases. Thus, it is proposed to enhance deceleration of cell cycle by blocking cell proliferation and growth. Conclusion: The current review epitomizes published information and provides complete interpretations about all known anti-cancer mechanisms of amygdalin, possible role of naturally occurring amygdalin in fight against cancer and mistaken belief about cyanide toxicity causing potential of amygdalin. However, well-planned clinical trials are still needed to be conducted to prove effectiveness of this substance in vivo and to get approval for human use.


Amino Acids ◽  
2012 ◽  
Vol 44 (2) ◽  
pp. 715-723 ◽  
Author(s):  
J. Michael Conlon ◽  
Milena Mechkarska ◽  
Manju Prajeep ◽  
Kholoud Arafat ◽  
Milan Zaric ◽  
...  

2021 ◽  
Vol 14 (12) ◽  
pp. 1315
Author(s):  
Fatemeh Rezaei-Tazangi ◽  
Hossein Roghani-Shahraki ◽  
Mahdi Khorsand Ghaffari ◽  
Firoozeh Abolhasani Zadeh ◽  
Aynaz Boostan ◽  
...  

Ovarian cancer (OCa) is characterized as one of the common reasons for cancer-associated death in women globally. This gynecological disorder is chiefly named the “silent killer” due to lacking an association between disease manifestations in the early stages and OCa. Because of the disease recurrence and resistance to common therapies, discovering an effective therapeutic way against the disease is a challenge. According to documents, some popular herbal formulations, such as curcumin, quercetin, and resveratrol, can serve as an anti-cancer agent through different mechanisms. However, these herbal products may be accompanied by some pharmacological limitations, such as poor bioavailability, instability, and weak water solubility. On the contrary, using nano-based material, e.g., nanoparticles (NPs), micelles, liposomes, can significantly solve these limitations. Therefore, in the present study, we will summarize the anti-cancer aspects of these herbal and-nano-based herbal formulations with a focus on their mechanisms against OCa.


2021 ◽  
pp. 30-39
Author(s):  
Prateek Paul ◽  
Manvi .

For prostaglandin production, the enzyme cyclooxygenase (COX) is required. The two COX isoforms are constitutive COX-1 (which is responsible for physiological functions) and inducible COX-2 (involved in inflammation). COX inhibition explains both the medicinal (inhibition of COX-2) and negative effects (inhibition of COX-1) effects of non-steroidal anti-inflammatory medicines (NSAIDs). Nonsteroidal anti-inflammatory medicines (NSAIDs) act by blocking the enzyme cyclooxygenase (COX), which produces prostaglandins (PGs). To a greater or lesser extent, they share similar side effects, such as stomach and renal toxicity. According to a recent study, there are at least two COX isoenzymes. COX-1 is a naturally occurring enzyme that creates prostaglandins (PGs), which protect the stomach and kidneys. Aspirin's well-known anti-cancer impact could also be related to its influence on COX-2, which is expressed in this condition. As a result, selective COX-2 inhibitors may have new therapeutic potential as anticancer drugs, as well as in preventing premature labor and maybe reducing the progression of Alzheimer's disease.


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