Phytochemical profile and therapeutic potential of white horehound (Marrubium vulgare) – a review of the current state of knowledge

Background: Mouse Double Minute 2 protein (MDM2) is a cellular regulator of p53 tumor suppressor (p53). Inhibition of the interaction between MDM2 and p53 proteins is a promising anticancer therapy. Objective: This updated patent review is an attempt to compile the research and achievements of the various researchers working on small molecule MDM2 inhibitors from 2010 to date. We provide an outlook into the future for therapy based on MDM2 inhibition by presenting an overview of the most relevant patents which have recently appeared in the literature. Methods: Literature and recent patents focusing on the anticancer potential of MDM2-p53 interaction inhibitors and its applications have been analyzed. We put the main emphasis on the most perspective compounds which are or were examined in clinical trials. Results: Literature data indicated that MDM2 inhibitors are therapeutically effective in specific types of cancer or non-cancer diseases. A great number of patents and research work around new MDM2- p53 interaction inhibitors, possible combinations, new indications, clinical regimens in previous years prove that this targeted therapy is in the scope of interest for many business and academic research groups. Conclusion: Novel MDM2 inhibitors thanks to higher potency and better ADME properties have shown effectiveness in preclinical and clinical development however the final improvement of therapeutic potential for MDM2 inhibitors might depend on the useful combination therapy and exploring new cancer and non-cancer indications.

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Biological Properties and Prospects for the Application of Eugenol—A Review

International Journal of Molecular Sciences ◽

10.3390/ijms22073671 ◽

2021 ◽

Vol 22 (7) ◽

pp. 3671

Author(s):

Magdalena Ulanowska ◽

Beata Olas

Keyword(s):

Body Weight ◽

Aromatic Compound ◽

Therapeutic Potential ◽

Antioxidant Properties ◽

Biological Properties ◽

Clove Oil ◽

Current State ◽

Potential Component ◽

Anti Inflammatory ◽

High Concentrations

Eugenol is a phenolic aromatic compound obtained mainly from clove oil. Due to its known antibacterial, antiviral, antifungal, anticancer, anti-inflammatory and antioxidant properties, it has long been used in various areas, such as cosmetology, medicine, and pharmacology. However, high concentrations can be toxic. A dose of 2.5 mg/kg body weight is regarded as safe. This paper reviews the current state of knowledge regarding the activities and application of eugenol and its derivatives and recent research of these compounds. This review is based on information concerning eugenol characteristics and recent research from articles in PubMed. Eugenol remains of great interest to researchers, since its multidirectional action allows it to be a potential component of drugs and other products with therapeutic potential against a range of diseases.

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PHYTO-MEDICINAL EFFECTS OF SYZYGIUM CUMINI ON DIABETES: A REVIEW

International Journal of Research in AYUSH and Pharmaceutical Sciences ◽

10.47070/ijraps.v4i3.80 ◽

2020 ◽

pp. 392-402

Author(s):

Md. Mahmudul Amin

Keyword(s):

Plant Extracts ◽

Therapeutic Potential ◽

Biological Effects ◽

Scientific Evidence ◽

Research Result ◽

Treatment Strategies ◽

Pharmaceutical Preparations ◽

Public Health Problem ◽

Major Public Health Problem ◽

Current State

Diabetes is a major public health problem which has been increasing day by day throughout the world with an alarming rate. In recent years, several plant extracts have been examined for their anti-diabetic properties to identify alternative treatment strategies that pose less risk for diabetes. It has been shown that different parts of these plants are collected from diverse regions and administered in different pharmaceutical preparations. The aim of the present review is to provide an overview of the phytochemicals present in S. cumini plants and their potent anti-diabetic activity, toxicological and biological effects of these plant extracts, their current state, limitation and future prospects in developing countries that are not included in the European Pharmacopoeia. In addition, a prospective research result of synergistic use of this plant with other plant (Ficus racemosa) done presently in our laboratory has been included. Based on the available evidence, we highlight the ways in which their therapeutic potential can be properly harnessed and provide scientific evidence for the discovery of novel leads for herbal drug development.

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Epilogue

10.1093/oso/9780198813910.003.0007 ◽

2021 ◽

pp. 203-208

Author(s):

Walter Glannon

Keyword(s):

Cognitive Functions ◽

Therapeutic Potential ◽

Functional Independence ◽

Shared Control ◽

Loss Of Control ◽

Neural Prosthetics ◽

Current State ◽

The People ◽

Sensory Motor ◽

The Brain

This section summarizes the main neuroscientific and philosophical issues regarding neural prosthetics. It comments on the therapeutic potential of more and less invasive systems to restore sensory, motor, and cognitive functions. It also speculates on future neural prosthetics and how they might change our view of the brain–mind relation and our concept of ourselves as humans. The current state of neural prosthetics does not indicate that machines and implants control the thought and behaviour of people to whom they are connected or in whom they are implanted. There is no loss of control but shared control between these artificial systems and the people who use them. The rehabilitative and restorative capacity of neural prosthetics enable those with neurological or physical disabilities to acquire or regain functional independence.

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Phytochemical profile, toxicological evaluation of Rhipsalis baccifera (Sol.) Stearn (Cactaceae) extract and their antitumor activity in Ehrlich carcinoma-bearing mice

10.53365/nrfhh/142159 ◽

2021 ◽

Author(s):

Jéssica Alves Cavalcantea ◽

Luiz da Silva Maia Neto ◽

Anna Lígia de Castro Figueiredo ◽

Weslley Oliveira ◽

José Roberto Pimentel Cabral de Seixas ◽

...

Keyword(s):

Antitumor Activity ◽

Therapeutic Potential ◽

Lethal Dose ◽

Artemia Salina ◽

Subsequent Treatment ◽

Ehrlich Carcinoma ◽

Toxicological Evaluation ◽

Phytochemical Profile

Rhipsalis baccifera (Sol.) Stearn is a typical cactus from tropical regions with wide geographic distribution, and its therapeutic potential is not yet fully understood, such as antitumoral property. Thus, this study evaluated the cytotoxic ethanolic extract of R. baccifera (EERB) and its antitumor activity against Erlich's tumor in mice. The EERB was obtained, and its phytochemical profile was filed by thin-layer chromatography. The toxicity was evaluated in vitro and in vivo using the microcrustacean Artemia salina Leach and mice. The lethal dose was determined after implantation of a tumor cell suspension, with subsequent treatment with EERB (200 mg/kg and 100 mg/kg) 48h after implantation. These values represent the tenth part of the DL50 and CL50, respectively. The presence of phenols, tannins and triterpenes were demonstrated in the phytochemical results. Toxicity was dose-dependent, and the tumor inhibition was 84.1% and 75.8% at doses of 200 mg/kg and 100 mg/kg, respectively. We can highlight that the growth of Erlich's carcinoma suffered inhibitory effects against the EERB. EERB was found to have low acute toxicity and a high potential for use in antitumor therapy. Thus, new studies involving pre-clinical and clinical analyses of the extract are essential to determine the safe dose.

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Health as a Complex Adaptive System: a new dimension of patient care in internal medicine and general practice

F1000Research ◽

10.12688/f1000research.9042.1 ◽

2016 ◽

Vol 5 ◽

pp. 1672

Author(s):

Johannes Bircher ◽

Eckhart G. Hahn

Keyword(s):

Adaptive System ◽

Complex Adaptive System ◽

Therapeutic Potential ◽

The Past ◽

Complex Interactions ◽

System A ◽

Current State ◽

Concept Of Health ◽

Environmental Determinants Of Health ◽

Complex Adaptive

This paper explores the diagnostic and therapeutic potential of a new concept of health. Investigations into the nature of health have led to a new definition that explains health as a complex adaptive system (CAS) and is based on five components (a-e). Humans like all biological creatures must satisfactorily respond to (a) the demands of life. For this purpose they need (b) a biologically given potential (BGP) and (c) a personally acquired potential (PAP). These properties of individuals are embedded within (d) social and (e) environmental determinants of health. Between these five components of health there are 10 complex interactions that justify health to be viewed as a CAS. In each patient, the current state of his health as a CAS evolved from the past, will move forward to a new future, and has to be analyzed and treated as an autonomous whole. A diagnostic procedure is suggested as follows: together with the patient, the five components and 10 complex interactions are assessed. This may help the patient to better understand his situation and to recognize possible next steps that may be useful for him to evolve toward more health by himself. In this process mutual trust in the patient-physician interaction is critical. The described approach offers new possibilities to help patients to improve their health.

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Carnosine—a natural bioactive dipeptide: bioaccessibility, bioavailability and health benefits

Journal of Food Bioactives ◽

10.31665/jfb.2019.5174 ◽

2019 ◽

Vol 5 ◽

pp. 8-17 ◽

Cited By ~ 7

Author(s):

Lujuan Xing ◽

MacKenzie E. Chee ◽

Hua Zhang ◽

Wangang Zhang ◽

Yoshinori Mine

Keyword(s):

Therapeutic Potential ◽

Antioxidant Activities ◽

Health Benefits ◽

Biochemical Properties ◽

Current State ◽

Preclinical And Clinical Studies ◽

Potential Use ◽

Significant Health

Carnosine is a natural dipeptide synthesized by both vertebrate and invertebrate organisms and has functional properties that are specific to muscle and excitable tissues. Recent in vivo and in vitro studies have shown that carnosine presents metal chelating and antioxidant activities and has the ability to inhibit protein carbonylation and glycoxidation. This review describes the health benefits of carnosine in relation to its bioaccessibility, bioavailability and biochemical properties as well as providing the current state-of-the-art knowledge on the potential use of carnosine as a nutraceutical. The therapeutic potential of carnosine has also been investigated by a number of preclinical and clinical studies for diseases such as diabetes and its associated complications, as well as fatigue, ageing, and some neurological disorders. Altogether the current literature provides supportive evidence on the use of carnosine as a natural dietary supplement with significant health boosting efficiency and without any side effects.

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Ketamine as an antidepressant: overview of its mechanisms of action and potential predictive biomarkers

Therapeutic Advances in Psychopharmacology ◽

10.1177/2045125320916657 ◽

2020 ◽

Vol 10 ◽

pp. 204512532091665 ◽

Cited By ~ 2

Author(s):

Dmitriy Matveychuk ◽

Rejish K. Thomas ◽

Jennifer Swainson ◽

Atul Khullar ◽

Mary-Anne MacKay ◽

...

Keyword(s):

Ampa Receptors ◽

Therapeutic Potential ◽

Predictive Biomarkers ◽

Major Depressive ◽

Delayed Effects ◽

Current State ◽

Resistant Depression ◽

The 1960S ◽

The Brain ◽

Unique Mechanism

Ketamine, a drug introduced in the 1960s as an anesthetic agent and still used for that purpose, has garnered marked interest over the past two decades as an emerging treatment for major depressive disorder. With increasing evidence of its efficacy in treatment-resistant depression and its potential anti-suicidal action, a great deal of investigation has been conducted on elucidating ketamine’s effects on the brain. Of particular interest and therapeutic potential is the ability of ketamine to exert rapid antidepressant properties as early as several hours after administration. This is in stark contrast to the delayed effects observed with traditional antidepressants, often requiring several weeks of therapy for a clinical response. Furthermore, ketamine appears to have a unique mechanism of action involving glutamate modulation via actions at the N-methyl-D-aspartate (NMDA) and [Formula: see text]-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors, as well as downstream activation of brain-derived neurotrophic factor (BDNF) and mechanistic target of rapamycin (mTOR) signaling pathways to potentiate synaptic plasticity. This paper provides a brief overview of ketamine with regard to pharmacology/pharmacokinetics, toxicology, the current state of clinical trials on depression, postulated antidepressant mechanisms and potential biomarkers (biochemical, inflammatory, metabolic, neuroimaging sleep-related and cognitive) for predicting response to and/or monitoring of therapeutic outcome with ketamine.

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The therapeutic potential of targeting tryptophan catabolism in cancer

British Journal of Cancer ◽

10.1038/s41416-019-0664-6 ◽

2019 ◽

Vol 122 (1) ◽

pp. 30-44 ◽

Cited By ~ 15

Author(s):

Christiane A. Opitz ◽

Luis F. Somarribas Patterson ◽

Soumya R. Mohapatra ◽

Dyah L. Dewi ◽

Ahmed Sadik ◽

...

Keyword(s):

Clinical Trials ◽

Immune Responses ◽

Cancer Progression ◽

Therapeutic Potential ◽

Positive Impact ◽

Background Information ◽

Catabolic Enzymes ◽

Current State ◽

Tryptophan Catabolism ◽

Alternative Approaches

AbstractBased on its effects on both tumour cell intrinsic malignant properties as well as anti-tumour immune responses, tryptophan catabolism has emerged as an important metabolic regulator of cancer progression. Three enzymes, indoleamine-2,3-dioxygenase 1 and 2 (IDO1/2) and tryptophan-2,3-dioxygenase (TDO2), catalyse the first step of the degradation of the essential amino acid tryptophan (Trp) to kynurenine (Kyn). The notion of inhibiting IDO1 using small-molecule inhibitors elicited high hopes of a positive impact in the field of immuno-oncology, by restoring anti-tumour immune responses and synergising with other immunotherapies such as immune checkpoint inhibition. However, clinical trials with IDO1 inhibitors have yielded disappointing results, hence raising many questions. This review will discuss strategies to target Trp-degrading enzymes and possible down-stream consequences of their inhibition. We aim to provide comprehensive background information on Trp catabolic enzymes as targets in immuno-oncology and their current state of development. Details of the clinical trials with IDO1 inhibitors, including patient stratification, possible effects of the inhibitors themselves, effects of pre-treatments and the therapies the inhibitors were combined with, are discussed and mechanisms proposed that might have compensated for IDO1 inhibition. Finally, alternative approaches are suggested to circumvent these problems.

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Homeobox Genes in Cancers: From Carcinogenesis to Recent Therapeutic Intervention

Frontiers in Oncology ◽

10.3389/fonc.2021.770428 ◽

2021 ◽

Vol 11 ◽

Author(s):

Yangyang Feng ◽

Tongyue Zhang ◽

Yijun Wang ◽

Meng Xie ◽

Xiaoyu Ji ◽

...

Keyword(s):

Hox Genes ◽

Therapeutic Potential ◽

Human Cancer ◽

Transcriptional Factors ◽

Molecular Networks ◽

Cancer Development ◽

Dual Function ◽

Current State ◽

Genes Encoding ◽

Interfering Rna

The homeobox (HOX) genes encoding an evolutionarily highly conserved family of homeodomain-containing transcriptional factors are essential for embryogenesis and tumorigenesis. HOX genes are involved in cell identity determination during early embryonic development and postnatal processes. The deregulation of HOX genes is closely associated with numerous human malignancies, highlighting the indispensable involvement in mortal cancer development. Since most HOX genes behave as oncogenes or tumor suppressors in human cancer, a better comprehension of their upstream regulators and downstream targets contributes to elucidating the function of HOX genes in cancer development. In addition, targeting HOX genes may imply therapeutic potential. Recently, novel therapies such as monoclonal antibodies targeting tyrosine receptor kinases, small molecular chemical inhibitors, and small interfering RNA strategies, are difficult to implement for targeting transcriptional factors on account of the dual function and pleiotropic nature of HOX genes-related molecular networks. This paper summarizes the current state of knowledge on the roles of HOX genes in human cancer and emphasizes the emerging importance of HOX genes as potential therapeutic targets to overcome the limitations of present cancer therapy.

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