scholarly journals Cyclic Dipeptides: The Biological and Structural Landscape with Special Focus on the Anti-Cancer Proline-Based Scaffold

Biomolecules ◽  
2021 ◽  
Vol 11 (10) ◽  
pp. 1515
Author(s):  
Joanna Bojarska ◽  
Adam Mieczkowski ◽  
Zyta Ziora ◽  
Mariusz Skwarczynski ◽  
Istvan Toth ◽  
...  

Cyclic dipeptides, also know as diketopiperazines (DKP), the simplest cyclic forms of peptides widespread in nature, are unsurpassed in their structural and bio-functional diversity. DKPs, especially those containing proline, due to their unique features such as, inter alia, extra-rigid conformation, high resistance to enzyme degradation, increased cell permeability, and expandable ability to bind a diverse of targets with better affinity, have emerged in the last years as biologically pre-validated platforms for the drug discovery. Recent advances have revealed their enormous potential in the development of next-generation theranostics, smart delivery systems, and biomaterials. Here, we present an updated review on the biological and structural profile of these appealing biomolecules, with a particular emphasis on those with anticancer properties, since cancers are the main cause of death all over the world. Additionally, we provide a consideration on supramolecular structuring and synthons, based on the proline-based DKP privileged scaffold, for inspiration in the design of compound libraries in search of ideal ligands, innovative self-assembled nanomaterials, and bio-functional architectures.

2012 ◽  
pp. 84-89
Author(s):  
Quoc Hung Vo ◽  
Nguyen Phuong Nhi Doan ◽  
Dinh Quynh Phu Nguyen ◽  
Thi Dieu Tram Ho ◽  
Thi Hoai Nguyen

Objectives: Nowadays, bioactive substances isolated from marine organisms which are abundant and varied in Vietnamese sea attracted more and more the attention of scientists in the world and Vietnam as well. We have studied on soft coral Sinularia cruciata – Alcyoniidae, which has never been studied in Vietnam before, to find substances which are useful in medical field, especially in anti-cancer therapy. Materials and method: Specimens of soft coral Sinularia cruciata were collected from Con Co, Quang Tri province in May 2011. Pure compounds were isolated by using Thin Layer Chromatography; Column Chromatography normal phase and inverse phase; Shephadex LH 20. Structures of them were determined by spectral data of Nuclear Magnetic Resonance (NMR), Electrospray Ionization Mass Spectrometry (ESI-MS). Results & Conclusion: Structures of 4 compounds were identified: (1) 5.8-epidioxycholest-6-en-3-ol (2) Cholesterol (3) 1-O-hexadecyl-glycerol (Chimyl alcohol) (4) Glycerol 1-O-octadecyl ether (Batyl alcohol). The substance (1) was demonstrated to have strong anti-cancer effects in previous study. Key words Sinularia cruciata, Alcyoniidae, 5,8-epidioxycholest-6-en-3-ol, soft coral, cancer.


2018 ◽  
Vol 18 (10) ◽  
pp. 957-966 ◽  
Author(s):  
Milene Aparecida Andrade ◽  
Mariana Aparecida Braga ◽  
Pedro Henrique Souza Cesar ◽  
Marcus Vinicius Cardoso Trento ◽  
Mariana Araújo Espósito ◽  
...  

Background: Essential oils are complex mixtures of low molecular weight compounds extracted from plants. Their main constituents are terpenes and phenylpropanoids, which are responsible for their biological and pharmaceutical properties, such as insecticidal, parasiticidal, antimicrobial, antioxidant, anti-inflammatory, analgesic, antinociceptive, anticarcinogenic, and antitumor properties. Cancer is a complex genetic disease considered as a serious public health problem worldwide, accounting for more than 8 million deaths annually. Objective: The activities of prevention and treatment of different types of cancer and the medicinal potential of essential oils are addressed in this review. Conclusion: Several studies have demonstrated anti-carcinogenic and antitumor activity for many essential oils obtained from various plant species. They may be used as a substitution to or in addition to conventional anti-cancer therapy. Although many studies report possible mechanisms of action for essential oils compounds, more studies are necessary in order to apply them safely and appropriately in cancer therapy.


2021 ◽  
Vol 18 ◽  
Author(s):  
Damilare Rotimi ◽  
Jennifer Chidubem Amanze ◽  
Adebola Busola Ojo ◽  
Matthew Iyobhebhe ◽  
Tobiloba Christiana Elebiyo ◽  
...  

Abstract: The use of herbal remedies for medicinal purposes is becoming more popular around the world. As a result, plants have become viable treatment options for a variety of diseases. Garcinia kola (bitter kola) is a perennially grown plant in the Guttiferae family that has been evaluated and reported to have numerous health-promoting properties. Kolaviron is a biflavanoid and major phytochemical found in Garcinia kola that includes Garcinia Biflavanoid-1 (GB-1), kolaflavanone, and Garcinia Biflavanoid-2 (GB-2). It is obtained as a fraction extracted from Garcinia kola. Kolaviron's pharmacological properties include anti-inflammatory, anti-spasmodic, ameliorative, anti-asthmatic, anti-cancer, anti-malarial, hepatoprotective, antioxidant, anti-atherogenic, neuroprotective, anti-diabetic, and anti-amnesic properties. Kolaviron is recommended for use in clinical settings because it has been shown to have a high therapeutic efficacy in clinical trials. The purpose of this review is to assess the therapeutic efficacy of kolaviron.


1995 ◽  
Vol 9 (4) ◽  
pp. 205-216 ◽  
Author(s):  
Norman Longworth

The papers which follow in this special focus on lifelong learning are based on presentations at the First Global Conference on Lifelong Learning, held in Rome on 30 November–2 December 1994. In this introductory paper, Norman Longworth discusses the concept, definition and practice of lifelong learning and assesses why its importance and significance for the future are increasingly appreciated and stressed. He also sets out and discusses the main themes of the Rome conference, and analyses their implications and challenges specifically for business and higher education. Finally he describes the roles of the European Lifelong Learning Initiative (ELU), which organized the Rome conference, and the World Initiative on Lifelong Learning (WILL), which was established at the conference.


2018 ◽  
Vol 4 (5) ◽  
pp. 397-407 ◽  
Author(s):  
Awais Anwar ◽  
Emma Gould ◽  
Ryan Tinson ◽  
Javaid Iqbal ◽  
Chris Hamilton

Abstract Purpose of review This article provides a brief overview of natural phytoprotective products of allium with a special focus on the therapeutic potential of diallyl polysulfanes from garlic, their molecular targets and their fate in the living organisms. A comprehensive overview of antimicrobial and anticancer properties of published literature is presented for the reader to understand the effective concentrations of polysulfanes and their sensitivity towards different human pathogenic microbes, fungi, and cancer cell lines. Recent findings The article finds polysulfanes potentials as new generation novel antibiotics and chemo preventive agent. The effective dose rates of polysulfanes for antimicrobial properties are in the range of 0.5–40 mg/L and for anticancer 20–100 μM. The molecular targets for these redox modulators are mainly cellular thiols as well as inhibition and/or activation of certain cellular proteins in cancer cell lines. Summary Antimicrobial and anticancer activities of polysulfanes published in the literature indicate that with further development, they could be promising candidates for cancer prevention due to their selectivity towards abnormal cells.


F1000Research ◽  
2013 ◽  
Vol 2 ◽  
pp. 135 ◽  
Author(s):  
Asfar S Azmi ◽  
Fazlul H Sarkar ◽  
SM Hadi

“Let food be thy medicine and medicine be thy food” was quoted by Hippocrates more than two thousand years ago and since ancient times the health benefits of different natural agents have been exploited. In modern research, the disease preventive benefits of many such natural agents, particularly dietary compounds and their derivatives, has been attributed to their well recognized activity as the regulators of redox state of the cell. Nevertheless, most of these studies have focused on their antioxidant activity. A large body of evidence indicates that a major fraction of these agents can elicit pro-oxidant (radical generating) behavior which has been linked to their anti-cancer effects. This editorial provides an overview of the under-appreciated pro-oxidant activity of natural products, with a special focus on their ability to generate reactive oxygen species in the presence of transition metal ions, and discusses their possible use as cancer chemotherapeutic agents.


Author(s):  
V. V. Matyushina

The article regards the interrelation between language and consciousness, but with a special focus on the fact that consciousness is not only the tool and method of reflecting human existence or regulating human actions and relations, but it is as well a special device of evaluating the items and phenomena of real life. Consciousness is understood as a person's world outlook. Society members create and get knowledge in the course of cognitive coactivity. Speech is considered to be one of the types of activity. Outwardly the images of consciousness that are figured in the course of activity are expressed with the help of language tools. The procedure of studying consciousness in psychology is described, in psychology consciousness is understood as a person's image of the world, the connection between consciousness (or the image of the world) and the category of linguistic consciousness is traced, linguistic consciousness is thought to be an integral part of consciousness. As in psychology consciousness is compared with and likened to the so called image of the world, the latter can be represented in a form of the system of meanings. The system of meanings that is moulded in the course of perceiving the real world services and works as a specific system to direct a person in life. The knowledge gained in the course of activity is transformed into personal experience and expertise in a person's consciousness. The essence of the fundamental paradigm of modern psycholinguistics is revealed where the image of linguistic consciousness is the basic research pattern. The image of linguistic consciousness is determined as the image of the world mediated by language, or it can be presented as a collection of images of consciousness expressed with the help of language tools. The images of consciousness exist as word meanings. An attempt is made to prove that linguistic consciousness not only forms, stores or processes language signs and their meanings but also determines the attitude of a person to the items and phenomena of real life. Linguistic consciousness where the axiological factor is regarded as its essence directs a person's activity, determines a person's attitude to the items and phenomena of real life. On the basis of all above - mentioned it is proved that the element of value does exist in linguistic consciousness. Consequently values can be defined as the words with socially built meaning.


2022 ◽  
pp. 431-453
Author(s):  
Mohammed Rahmatullah ◽  
Khoshnur Jannat ◽  
Gerald R. Reeck ◽  
Rownak Jahan ◽  
Taufiq Rahman ◽  
...  

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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