Insights into Novel Drugs Targeting Bcl-2 protein as Potential Anti-cancer Agents

Cyperus rotundus (nut grass in English) is a perennial erect sedge plant and is distributed in over 90 countries of the world, where it has been mostly classified as a highly invasive weed. Despite this classification, the plant has been considered from traditional times to be medicinally important. The traditional uses of the plant in various countries include uses against various gastrointestinal tract disorders, skin diseases, leprosy, fever, and neurological disorders. Evaluation of the plant and especially its rhizomes in a scientific manner has revealed the presence of numerous phytochemicals and wide-ranging pharmacological activities, which include anti-microbial, gastrointestinal, wound healing, anti-diabetic, anti-cancer, anti-malarial, anti-obesity, hepatoprotective, and anti-pyretic activity. The scientific validation of a number of traditional uses strongly indicates that the plant may prove useful in the discovery of a number of lead compounds and novel drugs.

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Ethnic Use, Phytochemistry, and Pharmacology of Cyperus rotundus

Advances in Medical Diagnosis, Treatment, and Care - Ethnomedicinal Plant Use and Practice in Traditional Medicine ◽

10.4018/978-1-7998-1320-0.ch005 ◽

2020 ◽

pp. 82-104

Author(s):

Mohammed Rahmatullah ◽

Khoshnur Jannat ◽

Gerald R. Reeck ◽

Rownak Jahan ◽

Taufiq Rahman ◽

...

Keyword(s):

Wound Healing ◽

Skin Diseases ◽

Cyperus Rotundus ◽

Invasive Weed ◽

Lead Compounds ◽

Traditional Uses ◽

Novel Drugs ◽

Anti Cancer ◽

The World ◽

Scientific Validation

Cyperus rotundus (nut grass in English) is a perennial erect sedge plant and is distributed in over 90 countries of the world, where it has been mostly classified as a highly invasive weed. Despite this classification, the plant has been considered from traditional times to be medicinally important. The traditional uses of the plant in various countries include uses against various gastrointestinal tract disorders, skin diseases, leprosy, fever, and neurological disorders. Evaluation of the plant and especially its rhizomes in a scientific manner has revealed the presence of numerous phytochemicals and wide-ranging pharmacological activities, which include anti-microbial, gastrointestinal, wound healing, anti-diabetic, anti-cancer, anti-malarial, anti-obesity, hepatoprotective, and anti-pyretic activity. The scientific validation of a number of traditional uses strongly indicates that the plant may prove useful in the discovery of a number of lead compounds and novel drugs.

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Drug Repurposing Approaches to Combating Viral Infections

Journal of Clinical Medicine ◽

10.3390/jcm9113777 ◽

2020 ◽

Vol 9 (11) ◽

pp. 3777

Author(s):

Jay Trivedi ◽

Mahesh Mohan ◽

Siddappa N. Byrareddy

Keyword(s):

Viral Infections ◽

Drug Repurposing ◽

Therapeutic Drug ◽

Novel Drugs ◽

Anti Cancer ◽

Immunodeficiency Virus ◽

The Us ◽

Us Fda ◽

Cancer Agent ◽

The 1960S

Development of novel antiviral molecules from the beginning costs an average of $350 million to $2 billion per drug, and the journey from the laboratory to the clinic takes about 10–15 years. Utilization of drug repurposing approaches has generated substantial interest in order to overcome these drawbacks. A drastic reduction in the failure rate, which otherwise is ~92%, is achieved with the drug repurposing approach. The recent exploration of the drug repurposing approach to combat the COVID-19 pandemic has further validated the fact that it is more beneficial to reinvestigate the in-practice drugs for a new application instead of designing novel drugs. The first successful example of drug repurposing is zidovudine (AZT), which was developed as an anti-cancer agent in the 1960s and was later approved by the US FDA as an anti-HIV therapeutic drug in the late 1980s after fast track clinical trials. Since that time, the drug repurposing approach has been successfully utilized to develop effective therapeutic strategies against a plethora of diseases. Hence, an extensive application of the drug repurposing approach will not only help to fight the current pandemics more efficiently but also predict and prepare for newly emerging viral infections. In this review, we discuss in detail the drug repurposing approach and its advancements related to viral infections such as Human Immunodeficiency Virus (HIV) and Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2).

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Topics in Anti-Cancer Research: Volume 8

10.2174/97898114043821190801 ◽

2019 ◽

Keyword(s):

Cancer Research ◽

Endocrine Disruptors ◽

Anticancer Agents ◽

Cell Cancer ◽

New Developments ◽

Novel Drugs ◽

Anti Cancer ◽

Synthetic Estrogens ◽

Therapy Strategies

Topics in Anti-Cancer Research covers new developments in the field of cancer. Novel drugs as anticancer agents include natural and synthetic phenazines and other anti-cancer compounds. It also encompasses the role of estrogen as endocrine disruptors and strategies targeting cancer stem cells for the treatment of different types of cancers, including myeloma and renal cell cancer. The diversity of researches and topics published in this eBook Series will be valuable to cancer researchers, clinicians, and cancer professionals aiming to develop novel anti-cancer targets for the treatment of various cancers. The topics covered in the eighth volume of this series are as follows: Novel Drugs for Multiple Myeloma Synthetic Estrogens are Endocrine Disruptors via Inhibition of AF1 Domain of ERs Recent Progress of Phenazines as Anticancer Agents Cancer Stem Cell Targeting for Anticancer Therapy: Strategies and Challenges

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Small-Molecule Anti-Cancer Drugs From 2016 to 2020: Synthesis and Clinical Application

Natural Product Communications ◽

10.1177/1934578x211040326 ◽

2021 ◽

Vol 16 (9) ◽

pp. 1934578X2110403

Author(s):

Lijiao Wang ◽

Rong Li ◽

Chen Song ◽

Yanli Chen ◽

Haiyue Long ◽

...

Keyword(s):

Malignant Tumors ◽

Tumor Therapy ◽

Public Health Problem ◽

Targeting Therapy ◽

Novel Drugs ◽

Anti Cancer ◽

Significant Public Health Problem ◽

Significant Public Health ◽

Industrial Use ◽

Tumor Drugs

Malignant tumors have become a significant public health problem that severely threatens human health. Drug-targeting therapy is essential for tumor therapy, along with surgery and radiotherapy. Of the 378 novel drugs approved over the past five years, those for oncological therapy remains at the top (25%). These drugs are used to treat patients with various cancers by acting on corresponding targets, such as EGFR, JAK, BTK, IDH, and FLT3. This review examines anti-tumor agents approved between 2016 and 2020, classifying them according to indication (such as lung cancer, leukemia, breast cancer, and myeloma). These drugs are reviewed according to their route of administration, first-in-class designation, approval dates, and expedited review categories. Furthermore, this paper summarizes the targets and modes of action of the approved anti-tumor drugs while systematically discussing their synthetic routes for medicinal chemistry or industrial use, which will benefit next-generation drug discovery.

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Sinularin, an Anti-Cancer Agent Causing Mitochondria-Modulated Apoptosis and Cytoskeleton Disruption in Human Hepatocellular Carcinoma

International Journal of Molecular Sciences ◽

10.3390/ijms22083946 ◽

2021 ◽

Vol 22 (8) ◽

pp. 3946

Author(s):

Chou-Yuan Ko ◽

Po-Chang Shih ◽

Po-Wei Huang ◽

Yi-Hsin Lee ◽

Yen-Fu Chen ◽

...

Keyword(s):

Hepatocellular Carcinoma ◽

Annexin V ◽

Cancer Therapies ◽

Expression Levels ◽

Extracellular Signal ◽

Novel Drugs ◽

Anti Cancer ◽

Ic50 Values ◽

Cancer Agent ◽

Cytoskeleton Disruption

Liver cancer remains a leading cause of death, despite advances in anti-cancer therapies. To develop novel drugs, natural products are being considered as a good source for exploration. In this study, a natural product isolated from a soft coral was applied to evaluate its anti-cancer activities in hepatocellular carcinoma SK-HEP-1 cells. Sinularin was determined to have half-maximal inhibitory concentration (IC50) values of ~10 μM after 24, 48, and 72 h. The TUNEL assay and annexin V/PI staining results showed that sinularin induced DNA fragmentation and apoptosis, respectively. An investigation at the molecular level demonstrated that the expression levels of cleaved caspases 3/9 were significantly elevated at 10 μM sinularin. Mitochondrial and intracellular reactive oxygen species (ROS) levels were significantly increased following sinularin treatment, which also affected the mitochondrial membrane potential. In addition, it significantly lowered the mitochondrial respiration parameters and extracellular acidification rates at 10 μM. Further investigation showed that sinularin significantly attenuated wound healing, cell migration, and potential colony formation at 10 μM. Fluorescence microscopic observations showed that the distribution of F-actin filaments was significantly altered at 10 μM sinularin. Supported by Western blot analyses, the expression levels of AKT, p-ERK (extracellular-signal-related kinase), vimentin and VEGF were significantly down-regulated, whereas p-p38, pJNK and E-cadherin were significantly increased. Overall, at the IC50 concentration, sinularin was able to significantly affect SK-HEP-1 cells.

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