scholarly journals The Biological and Biophysical Properties of the Spider Peptide Gomesin

Molecules ◽  
2018 ◽  
Vol 23 (7) ◽  
pp. 1733 ◽  
Author(s):  
John Tanner ◽  
Evelyne Deplazes ◽  
Ricardo Mancera
Keyword(s):  
Cytotoxic Activity ◽  
Current Knowledge ◽  
Cytotoxic Activities ◽  
Binding Properties ◽  
Anti Cancer ◽  
Specific Selectivity ◽  
Cell Type Specific ◽  
Molecular Mechanism Of Action

This review summarises the current knowledge of Gomesin (Gm), an 18-residue long, cationic anti-microbial peptide originally isolated from the haemocytes of the Brazilian tarantula Acanthoscurria gomesiana. The peptide shows potent cytotoxic activity against clinically relevant microbes including Gram-positive and Gram-negative bacteria, fungi, and parasites. In addition, Gm shows in-vitro and in-vivo anti-cancer activities against several human and murine cancers. The peptide exerts its cytotoxic activity by permeabilising cell membranes, but the underlying molecular mechanism of action is still unclear. Due to its potential as a therapeutic agent, the structure and membrane-binding properties, as well as the leakage and cytotoxic activities of Gm have been studied using a range of techniques. This review provides a summary of these studies, with a particular focus on biophysical characterisation studies of peptide variants that have attempted to establish a structure-activity relationship. Future studies are still needed to rationalise the binding affinity and cell-type-specific selectivity of Gm and its variants, while more pre-clinical studies are required to develop Gm into a therapeutically useful peptide.

scholarly journals The Occurrence and Biological Activity of Tormentic Acid—A Review

Molecules ◽  
2021 ◽  
Vol 26 (13) ◽  
pp. 3797
Author(s):  
Marta Olech ◽  
Wojciech Ziemichód ◽  
Natalia Nowacka-Jechalke
Keyword(s):  
Biological Activity ◽  
Plant Species ◽  
Current Knowledge ◽  
In Vivo Studies ◽  
Natural Sources ◽  
Anti Cancer ◽  
Biochemical Mechanisms ◽  
Tormentic Acid

This review focuses on the natural sources and pharmacological activity of tormentic acid (TA; 2α,3β,19α-trihydroxyurs-2-en-28-oic acid). The current knowledge of its occurrence in various plant species and families is summarized. Biological activity (e.g., anti-inflammatory, antidiabetic, antihyperlipidemic, hepatoprotective, cardioprotective, neuroprotective, anti-cancer, anti-osteoarthritic, antinociceptive, antioxidative, anti-melanogenic, cytotoxic, antimicrobial, and antiparasitic) confirmed in in vitro and in vivo studies is compiled and described. Biochemical mechanisms affected by TA are indicated. Moreover, issues related to the biotechnological methods of production, effective eluents, and TA derivatives are presented.

scholarly journals Anti-Cancer Effects of Green Tea Polyphenols Against Prostate Cancer

Molecules ◽  
2019 ◽  
Vol 24 (1) ◽  
pp. 193 ◽  
Author(s):  
Yasuyoshi Miyata ◽  
Yohei Shida ◽  
Tomoaki Hakariya ◽  
Hideki Sakai
Keyword(s):  
Prostate Cancer ◽  
Green Tea ◽  
Molecular Mechanisms ◽  
Current Knowledge ◽  
Tea Polyphenols ◽  
Green Tea Polyphenols ◽  
Anti Cancer ◽  
Prevention And Treatment

Prostate cancer is the most common cancer among men. Green tea consumption is reported to play an important role in the prevention of carcinogenesis in many types of malignancies, including prostate cancer; however, epidemiological studies show conflicting results regarding these anti-cancer effects. In recent years, in addition to prevention, many investigators have shown the efficacy and safety of green tea polyphenols and combination therapies with green tea extracts and anti-cancer agents in in vivo and in vitro studies. Furthermore, numerous studies have revealed the molecular mechanisms of the anti-cancer effects of green tea extracts. We believe that improved understanding of the detailed pathological roles at the molecular level is important to evaluate the prevention and treatment of prostate cancer. Therefore, in this review, we present current knowledge regarding the anti-cancer effects of green tea extracts in the prevention and treatment of prostate cancer, with a particular focus on the molecular mechanisms of action, such as influencing tumor growth, apoptosis, androgen receptor signaling, cell cycle, and various malignant behaviors. Finally, the future direction for the use of green tea extracts as treatment strategies in patients with prostate cancer is introduced.

scholarly journals Phytochemical and Pharmacological Potential of Enhydra fluctuans Available in Bangladesh

2019 ◽  
pp. 1-11
Author(s):  
S. Kamal ◽  
S. R. Rony ◽  
S. Sharmin ◽  
F. R. Laboni ◽  
M. H. Sohrab
Keyword(s):  
Cytotoxic Activity ◽  
Radical Scavenging ◽  
Diffusion Method ◽  
Clot Lysis ◽  
Cytotoxic Activities ◽  
Hypotonic Solution ◽  
Chemical Screening ◽  
Soluble Fractions

Objectives: The possible phytochemical constituents, thrombolytic and membrane stabilizing activities of the crude ethanolic extract of Enhydra fluctuans (CE) were investigated along with the antimicrobial, antioxidant and cytotoxic potentials of its petroleum ether (PESF), carbon tetrachloride (CTCSF), chloroform (CSF) and aqueous (AQSF) soluble fractions. Materials & Methods: The coarse leaf powder was extracted at room temperature with ethanol. Solvent-solvent partitioning was done to obtain the four soluble fractions. Anticoagulant potential was determined by the in vitro thrombolytic model, membrane stabilization method was used to assess in vitro anti-inflammatory activity, the disc diffusion method was used for anti-microbial screening, antioxidant potential was determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging method and brine shrimp lethality bioassay method was used for cytotoxic activity determination. Results: Chemical screening of the crude extract evidenced the presence of alkaloids, saponins, tannins, flavonoids, reducing sugars and gums. It showed significant clot lysis property of 46.91%. It also significantly inhibited heat and hypotonic solution induced lysis of the human red blood cell membrane with values of 71.80% and 47.60%, respectively. CTCSF and PESF showed mild antimicrobial activity. AQSF showed most prominent antioxidant activity with IC50 value of 12.27 µg/mL. CTCSF showed LC50 value of 0.84 µg/mL, with most potent cytotoxic activity. Conclusion: Significant thrombolytic, membrane stabilizing, antioxidant and in vitro cytotoxic activities of the ethanolic plant extract were observed in this study. In vivo activities and isolation of active compound(s) from this extract are yet to be investigated.

Reversine: A Synthetic Purine with a Dual Activity as a Cell Dedifferentiating Agent and a Selective Anticancer Drug

2020 ◽  
Vol 27 (21) ◽  
pp. 3448-3462
Author(s):  
Marco Piccoli ◽  
Andrea Ghiroldi ◽  
Michelle M. Monasky ◽  
Federica Cirillo ◽  
Giuseppe Ciconte ◽  
...  
Keyword(s):  
Stem Cells ◽  
Current Knowledge ◽  
Embryonic Stem ◽  
Cell Types ◽  
Cancer Drug ◽  
Anti Cancer ◽  
Adult Cell ◽  
Induced Pluripotent

The development of new therapeutic applications for adult and embryonic stem cells has dominated regenerative medicine and tissue engineering for several decades. However, since 2006, induced Pluripotent Stem Cells (iPSCs) have taken center stage in the field, as they promised to overcome several limitations of the other stem cell types. Nonetheless, other promising approaches for adult cell reprogramming have been attempted over the years, even before the generation of iPSCs. In particular, two years before the discovery of iPSCs, the possibility of synthesizing libraries of large organic compounds, as well as the development of high-throughput screenings to quickly test their biological activity, enabled the identification of a 2,6-disubstituted purine, named reversine, which was shown to be able to reprogram adult cells to a progenitor-like state. Since its discovery, the effect of reversine has been confirmed on different cell types, and several studies on its mechanism of action have revealed its central role in inhibitory activity on several kinases implicated in cell cycle regulation and cytokinesis. These key features, together with its chemical nature, suggested a possible use of the molecule as an anti-cancer drug. Remarkably, reversine exhibited potent cytotoxic activity against several tumor cell lines in vitro and a significant effect in decreasing tumor progression and metastatization in vivo. Thus, 15 years since its discovery, this review aims at critically summarizing the current knowledge to clarify the dual role of reversine as a dedifferentiating agent and anti-cancer drug.

scholarly journals Scyphocephalione a Isolated from the Stem Bark of Scyphocephalium Ochocoa (Myristicaceae) Attenuate Acute and Chronic Pains Through the Antiinflammatory Activity

2022 ◽  
Author(s):  
Marius Mbiantcha ◽  
Raymond Tchouya Guy Feuya ◽  
William Nana Yousseu ◽  
Donatien Albert Atsamo ◽  
Hibrahim Foundikou ◽  
...  
Keyword(s):  
Neuropathic Pain ◽  
Protein Denaturation ◽  
Cancer Drug ◽  
Cytotoxic Activities ◽  
Second Phase ◽  
Peripheral Neuropathic Pain ◽  
Anti Cancer ◽  
Anti Inflammatory

Abstract Abstract In the treatment of cancer, patients that receive anti-cancer drugs such as Vincristine develop peripheral neuropathic pain. Scyphocephalione A is a new bioactive compound isolated from Scyphocephalium ochocoa (Myristicaceae), a medicinal plant traditionally used in African countries. Recently, an in vitro study has shown its anti-inflammatory and cytotoxic activities on MCF-7 cell line of mammary carcinoma. The purpose of the present study was to assess the in vitro anti-inflammatory and in vivo anti-nociceptive activities of Scyphocephalione A. In vitro tests were carried out on cyclooxygenase and 5-lipoxygenase activities, and on protein denaturation; while in vivo tests were performed on acute and chronic pain models. It was noticed that, Scyphocephalione A (1000 µg/ml), inhibits proteins denaturation, cyclooxygenase and 5-lipoxygenase activities respectively by 74.21%, 75.80% and 64.43%. The dose 50 mg/kg of Scyphocephalione A, inhibits acetic acid (63.43%, p<0.001) and formalin (42.12% (p<0.001) within first phase and 67.53% (p<0.001) within second phase)-induced pains. At the same dose, Scyphocephalione A significantly inhibited mechanical and heat hyperalgesia, as well as cold allodynia induced by vincristine. In addition, the compound restored haematological, biochemical and oxidative stress parameters which were altered following Vincristine administration. These results suggest that Scyphocephalione A is endowed with anti-inflammatory potential and antinociceptive properties. Therefore, Scyphocephalione A can be classified as a promising molecule for the management of peripheral neuropathic pain triggered by anti-cancer drug.

scholarly journals A Review on Daphnane-Type Diterpenoids and Their Bioactive Studies

Molecules ◽  
2019 ◽  
Vol 24 (9) ◽  
pp. 1842 ◽  
Author(s):  
Yue-Xian Jin ◽  
Lei-Ling Shi ◽  
Da-Peng Zhang ◽  
Hong-Yan Wei ◽  
Yuan Si ◽  
...  
Keyword(s):  
Biological Activities ◽  
Structural Diversity ◽  
Cytotoxic Activities ◽  
Hydroxyl Groups ◽  
Substitution Pattern ◽  
In Vivo Experiments ◽  
Wide Range ◽  
Anti Cancer

Natural daphnane diterpenoids, mainly distributed in plants of the Thymelaeaceae and Euphorbiaceae families, usually include a 5/7/6-tricyclic ring system with poly-hydroxyl groups located at C-3, C-4, C-5, C-9, C-13, C-14, or C-20, while some special types have a characteristic orthoester motif triaxially connectedat C-9, C-13, and C-14. The daphnane-type diterpenoids can be classified into five types: 6-epoxy daphnane diterpenoids, resiniferonoids, genkwanines, 1-alkyldaphnanes and rediocides, based on the oxygen-containing functions at rings B and C, as well as the substitution pattern of ring A. Up to now, nearly 200 daphnane-type diterpenoids have been isolated and elucidated from the Thymelaeaceae and Euphorbiaceae families. In-vitro and in-vivo experiments of these compounds have shown that they possess a wide range of biological activities, including anti-HIV, anti-cancer, anti-leukemic, neurotrophic, pesticidal and cytotoxic effects. A comprehensive account of the structural diversity is given in this review, along with the cytotoxic activities of daphnane-type diterpenoids, up to April 2019.

scholarly journals An Updated Review of Smac Mimetics, LCL161, Birinapant, and GDC-0152 in Cancer Treatment

2020 ◽  
Vol 11 (1) ◽  
pp. 335
Author(s):  
Yung-Chieh Chang ◽  
Chun Hei Antonio Cheung
Keyword(s):  
Cancer Treatment ◽  
Phase 1 ◽  
The Novel ◽  
Iap Antagonist ◽  
Anti Cancer ◽  
Smac Mimetics ◽  
Molecular Mechanism Of Action ◽  
Apoptosis Proteins

Inhibitor of apoptosis proteins (IAPs) are suggested as therapeutic targets for cancer treatment. Smac/DIABLO is a natural IAP antagonist in cells; therefore, Smac mimetics have been developed for cancer treatment in the past decade. In this article, we review the anti-cancer potency and novel molecular targets of LCL161, birinapant, and GDC-0152. Preclinical studies demonstrated that Smac mimetics not only induce apoptosis but also arrest cell cycle, induce necroptosis, and induce immune storm in vitro and in vivo. The safety and tolerance of Smac mimetics are evaluated in phase 1 and phase 2 clinical trials. In addition, the combination of Smac mimetics and chemotherapeutic compounds was reported to improve anti-cancer effects. Interestingly, the novel anti-cancer molecular mechanism of action of Smac mimetics was reported in recent studies, suggesting that many unknown functions of Smac mimetics still need to be revealed. Exploring these currently unknown signaling pathways is important to provide hints for the modification and combination therapy of further compounds.

scholarly journals Perspectives in Manipulating EVs for Therapeutic Applications: Focus on Cancer Treatment

2020 ◽  
Vol 21 (13) ◽  
pp. 4623 ◽  
Author(s):  
Katarzyna Nazimek ◽  
Krzysztof Bryniarski
Keyword(s):  
Membrane Lipids ◽  
Current Knowledge ◽  
Parental Cell ◽  
Target Cells ◽  
Adjuvant Activity ◽  
Micro Rnas ◽  
Anti Cancer ◽  
Research Findings

Extracellular vesicles (EVs) receive special attention from oncologists due to their assumed usefulness as prognostic markers, vaccines to induce anti-cancer immune response, and physiological delivery tools. The latter application, which supports the reduction of side effects of treatment, is still fraught with many challenges, including established methods for loading EVs with selected cargo and directing them towards target cells. EVs could be loaded with selected cargo either in vitro using several physicochemical techniques, or in vivo by modification of parental cell, which may have an advantage over in vitro procedures, since some of them significantly influence EVs’ properties. Otherwise, our research findings suggest that EVs could be passively supplemented with micro RNAs (miRNAs) or miRNA antagonists to induce expected biological effect. Furthermore, our observations imply that antigen-specific antibody light chains could coat the surface of EVs to increase the specificity of cell targeting. Finally, the route of EVs’ administration also determines their bioavailability and eventually induced therapeutic effect. Besides, EV membrane lipids may possibly possess immune adjuvant activity. The review summarizes the current knowledge on the possibilities to manipulate EVs to use them as a delivery tool, with the special emphasis on anti-cancer therapy.

scholarly journals In Vitro and In Vivo Studies of Anti-Lung Cancer Activity of Artemesia judaica L. Crude Extract Combined with LC-MS/MS Metabolic Profiling, Docking Simulation and HPLC-DAD Quantification

Antioxidants ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 17
Author(s):  
Marwa S. Goda ◽  
Mohamed S. Nafie ◽  
Basma M. Awad ◽  
Maged S. Abdel-Kader ◽  
Amany K. Ibrahim ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Liquid Chromatography ◽  
Cytotoxic Activity ◽  
Active Sites ◽  
Array Detector ◽  
Cytotoxic Activities ◽  
Promising Source ◽  
Cancer Activity

Artemisia judaica L. (Family: Asteraceae) exhibited antioxidant, anti-inflammatory, and antiapoptotic effects. The in vitro cytotoxic activity of A. judaica ethanolic extract was screened against a panel of cancer cell lines. The results revealed its cytotoxic activity against a lung cancer (A549) cell line with a promising IC50 of 14.2 μg/mL compared to doxorubicin as a standard. This was confirmed through the downregulation of antiapoptotic genes, the upregulation of proapoptotic genes, and the cell cycle arrest at the G2/M phase. Further in vivo study showed that a solid tumor mass was significantly reduced, with a tumor inhibition ratio of 54% relative to doxorubicin therapy in a Xenograft model. From a chemical point of view, various classes of natural products have been identified by liquid chromatography combined with tandem mass spectrometry (LC-MS/MS). The docking study of the detected metabolites approved their cytotoxic activity through their virtual binding affinity towards the cyclin-dependent kinase 2 (CDK-2) and epidermal growth factor receptor (EGFR) active sites. Finally, A. judaica is a fruitful source of polyphenols that are well-known for their antioxidant and cytotoxic activities. As such, the previously reported polyphenols with anti-lung cancer activity were quantified by high-performance liquid chromatography coupled with a diode array detector (HPLC-DAD). Rutin, quercetin, kaempferol, and apigenin were detected at concentrations of 6 mg/gm, 0.4 mg/gm, 0.36 mg/gm, and 3.9 mg/gm of plant dry extract, respectively. It is worth noting that kaempferol and rutin are reported for the first time. Herein, A. judaica L. may serve as an adjuvant therapy or a promising source of leading structures in drug discovery for lung cancer treatment.

scholarly journals An Insight into the Anti-Angiogenic and Anti-Metastatic Effects of Oridonin: Current Knowledge and Future Potential

Molecules ◽  
2021 ◽  
Vol 26 (4) ◽  
pp. 775
Author(s):  
Nurul Akmaryanti Abdullah ◽  
Nur Fariesha Md Hashim ◽  
Aula Ammar ◽  
Noraina Muhamad Zakuan
Keyword(s):  
Cancer Therapy ◽  
Cancer Biology ◽  
Cancer Metastasis ◽  
Epithelial To Mesenchymal Transition ◽  
Current Knowledge ◽  
Angiogenic Growth Factors ◽  
Mesenchymal Transition ◽  
Anti Cancer

Cancer is one of the leading causes of death worldwide, with a mortality rate of more than 9 million deaths reported in 2018. Conventional anti-cancer therapy can greatly improve survival however treatment resistance is still a major problem especially in metastatic disease. Targeted anti-cancer therapy is increasingly used with conventional therapy to improve patients’ outcomes in advanced and metastatic tumors. However, due to the complexity of cancer biology and metastasis, it is urgent to develop new agents and evaluate the anti-cancer efficacy of available treatments. Many phytochemicals from medicinal plants have been reported to possess anti-cancer properties. One such compound is known as oridonin, a bioactive component of Rabdosia rubescens. Several studies have demonstrated that oridonin inhibits angiogenesis in various types of cancer, including breast, pancreatic, lung, colon and skin cancer. Oridonin’s anti-cancer effects are mediated through the modulation of several signaling pathways which include upregulation of oncogenes and pro-angiogenic growth factors. Furthermore, oridonin also inhibits cell migration, invasion and metastasis via suppressing epithelial-to-mesenchymal transition and blocking downstream signaling targets in the cancer metastasis process. This review summarizes the recent applications of oridonin as an anti-angiogenic and anti-metastatic drug both in vitro and in vivo, and its potential mechanisms of action.

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