scholarly journals Tetramethylpyrazine: A Review of Its Antitumor Potential and Mechanisms

2021 ◽  
Vol 12 ◽  
Author(s):  
Shaojie Yang ◽  
Shuodong Wu ◽  
Wanlin Dai ◽  
Liwei Pang ◽  
Yaofeng Xie ◽  
...  
Keyword(s):  
Gene Mutations ◽  
Chemotherapeutic Agents ◽  
Antitumor Drugs ◽  
Major Research ◽  
Research Focus ◽  
Antitumor Effects ◽  
Biological Perspective ◽  
Antitumor Potential ◽  
Low Toxicity ◽  
Significant Attention

Cancer remains a major public health threat. The mitigation of the associated morbidity and mortality remains a major research focus. From a molecular biological perspective, cancer is defined as uncontrolled cell division and abnormal cell growth caused by various gene mutations. Therefore, there remains an urgent need to develop safe and effective antitumor drugs. The antitumor effect of plant extracts, which are characterized by relatively low toxicity and adverse effect, has attracted significant attention. For example, increasing attention has been paid to the antitumor effects of tetramethylpyrazine (TMP), the active component of the Chinese medicine Chuanqiong, which can affect tumor cell proliferation, apoptosis, invasion, metastasis, and angiogenesis, as well as reverse chemotherapeutic resistance in neoplasms, thereby triggering antitumor effects. Moreover, TMP can be used in combination with chemotherapeutic agents to enhance their effects and reduce the side effect associated with chemotherapy. Herein, we review the antitumor effects of TMP to provide a theoretical basis and foundation for the further exploration of its underlying antitumor mechanisms and promoting its clinical application.

scholarly journals Antitumor Potential of Lippia citriodora Essential Oil in Breast Tumor-Bearing Mice

Antioxidants ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 875
Author(s):  
Katerina Spyridopoulou ◽  
Tamara Aravidou ◽  
Evangeli Lampri ◽  
Eleni Effraimidou ◽  
Aglaia Pappa ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Antiproliferative Activity ◽  
Folk Medicine ◽  
Tumor Model ◽  
Flowering Plant ◽  
Antitumor Effects ◽  
Lippia Citriodora ◽  
Antitumor Potential ◽  
Apoptotic Marker

Lippia citriodora is a flowering plant cultivated for its lemon-scented leaves and used in folk medicine for the preparation of tea for the alleviation of symptoms of gastrointestinal disorders, cold, and asthma. The oil extracted from the plant leaves was shown to possess antioxidant potential and to exert antiproliferative activity against breast cancer. The aim of this study was to further investigate potential antitumor effects of L. citriodora oil (LCO) on breast cancer. The in vitro antiproliferative activity of LCO was examined against murine DA3 breast cancer cells by the sulforhodamine B assay. We further explored the LCO’s pro-apoptotic potential with the Annexin-PI method. The LCO’s anti-migratory effect was assessed by the wound-healing assay. LCO was found to inhibit the growth of DA3 cells in vitro, attenuate their migration, and induce apoptosis. Finally, oral administration of LCO for 14 days in mice inhibited by 55% the size of developing tumors in the DA3 murine tumor model. Noteworthy, in the tumor tissue of LCO-treated mice the apoptotic marker cleaved caspase-3 was elevated, while a reduced protein expression of survivin was observed. These results indicate that LCO, as a source of bioactive compounds, has a very interesting nutraceutical potential.

Evaluation of Paclitaxel Nanocrystals In Vitro and In Vivo

Drug Research ◽  
2017 ◽  
Vol 68 (04) ◽  
pp. 205-212 ◽  
Author(s):  
Wanqing Li ◽  
Zhiguo Li ◽  
Lisha Wei ◽  
Aiping Zheng
Keyword(s):  
Drug Concentration ◽  
Antitumor Effects ◽  
High Drug ◽  
High Drug Concentration ◽  
Low Toxicity ◽  
Nanoparticle Drug Delivery ◽  
Antitumor Evaluation ◽  
Mcf 7

AbstractWe created a novel paclitaxel (PTX) nanoparticle drug delivery system and compared this to acommercial injection preparation to evaluate the antitumor effects for both formulations in vivo and in vitro.PTXnanocrystals were 194.9 nm with potential of −29.6 mV. Cytotoxicity tests indicated that both formulations had similar effects and cytotoxicity was dose- and time-dependent.Pharmacodynamics indicated that the drug concentration at the tumor was greater with PTX nanocrystals compared to commercial injection (P<0.01) and that drug accumulated more and for a longer duration. In vivo antitumor evaluation indicated significant antitumor effects and low toxicity of PTX nanocrystals. Moreover, bioimaging indicated that the PTX retention time in MCF-7-bearing mice was longer, especially at the tumor site, and this high drug concentration was maintained for a long time.Overall, PTX nanocrystalsare feasible and superior to traditional injection formulation chemotherapy.

Probiotics for the Chemoprotective Role Against the Toxic Effect of Cancer Chemotherapy

2021 ◽  
Vol 21 ◽  
Author(s):  
Aafrin Waziri ◽  
Charu Bharti ◽  
Mohammed Aslam ◽  
Parween Jamil ◽  
Aamir Mirza ◽  
...  
Keyword(s):  
Side Effects ◽  
Clinical Management ◽  
Clinical Evidence ◽  
Unmet Need ◽  
Chemotherapeutic Agents ◽  
Antitumor Effects ◽  
Anti Cancer ◽  
Different Types ◽  
Growth Promoting ◽  
High Degree

Background: The processes of chemo- and radiation therapy-based clinical management of different types of cancers are associated with toxicity and side effects of chemotherapeutic agents. So, there is always an unmet need to explore agents to reduce such risk factors. Among these, natural products have generated much attention because of their potent antioxidant and antitumor effects. In the past, some breakthrough outcomes established that various bacteria in the human intestinal gut are bearing growth-promoting attributes and suppressing the conversion of pro-carcinogens into carcinogens. Hence, probiotics integrated approaches are nowadays being explored as rationalized therapeutics in the clinical management of cancer. Methods: Here, published literature was explored to review chemoprotective roles of probiotics against toxic and side effects of chemotherapeutics. Results: Apart from excellent anti-cancer abilities, probiotics are bearing and alleviate toxicity and side effects of chemotherapeutics, with a high degree of safety and efficiency. Conclusion: Preclinical and clinical evidence suggested that due to the chemoprotective roles of probiotics against side effects and toxicity of chemotherapeutics, their integration in chemotherapy would be a judicious approach.

scholarly journals Beyond Alkaloids: Novel Bioactive Natural Products From Lobelia Species

2021 ◽  
Vol 12 ◽  
Author(s):  
Qinfang Zheng ◽  
Ye Wang ◽  
Shuihan Zhang
Keyword(s):  
Molecular Mechanisms ◽  
The Novel ◽  
Bioactive Components ◽  
Research Focus ◽  
Bioactive Natural Products ◽  
Hyperactivity Disorder ◽  
Multicenter Phase ◽  
Major Shift ◽  
Significant Attention

In this work, we reviewed the progress in the phytochemical and biological investigations of bioactive components derived from medicinally valuable Lobelia species. In the last 60 years, Lobelia has garnered significant attention from the phytochemist from around the world, majorly due to the discovery of bioactive piperidine alkaloids (e.g., lobinaline and lobeline) in the early 1950s. Later, lobeline underwent clinical trials for several indications including the treatment of attention deficit hyperactivity disorder and a multicenter phase three trial for smoking cessation. Subsequently, several other alkaloids derived from different species of Lobelia were also investigated for their pharmacological characteristics. However, in the last few years, the research focus has started shifting to the characterization of the other novel chemical classes. The major shift has been noticed due to the structurally similar alkaloid components, which essentially share similar pharmacological, physicochemical, and toxicological profiles. In this review, we present an up-to-date overview of their progress with special attention to understanding the molecular mechanisms of the novel bioactive components.

Modulation of Long Non-Coding RNAs by Different Classes of Secondary Metabolites from Plants: A Mini-Review on Antitumor Effects

2021 ◽  
Vol 21 ◽  
Author(s):  
Tamires Cunha Almeida ◽  
Janaína Brandão Seibert ◽  
Tatiane Roquete Amparo ◽  
Gustavo Henrique Bianco de Souza ◽  
Glenda Nicioli da Silva ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Large Scale ◽  
Biological Effects ◽  
Migration And Invasion ◽  
Antitumor Action ◽  
Pharmacokinetic Parameters ◽  
Antitumor Effects ◽  
Antitumor Potential ◽  
Inhibition Of Tumor Growth ◽  
Non Coding Rnas

: The broad pharmacological spectrum of plants is related to their secondary metabolism, which is responsible for the synthesis of different compounds that have multiple effects on cellular physiology. Among the biological effects presented by phytochemicals, their use for the prevention and treatment of cancer can be highlighted. This occurs due to several mechanisms of antitumor action demonstrated by these compounds, including regulation of the cell signaling pathways and inhibition of tumor growth. In this way, long non-coding RNAs (lncRNAs) appear to be promising targets for the treatment of cancer. Their deregulation has already been related to a variety of clinical-pathological parameters. However, the effects of secondary metabolites on lncRNAs are still restricted. For this reason, the present review aimed to gather data on phytochemicals with action on lncRNAs in order to confirm their possible antitumor potential. According to the literature, terpenoid and flavonoid are the main examples of secondary metabolites involved with lncRNAs activity. In addition, the lncRNAs H19, CASC2, HOTAIR, NKILA, CCAT1, MALAT1, AFAP1-AS1, MEG3, and CDKN2B-AS1 can be highlighted as important targets in the search for new anti-tumor agents since they act as modulating pathways related to cell proliferation, cell cycle, apoptosis, cell migration and invasion. Finally, challenges for the use of natural products as a commercial drug were also discussed. The low yield, selectivity index and undesirable pharmacokinetic parameters were emphasized as a difficulty for obtaining these compounds on a large scale and for improving the potency of its biological effect. However, the synthesis and/or development of formulations were suggested as a possible approach to solve these problems. All of these data together confirm the potential of secondary metabolites as a source of new anti-tumor agents acting on lncRNAs.

scholarly journals Mechanisms of Multidrug Resistance in Cancer Chemotherapy

2020 ◽  
Vol 21 (9) ◽  
pp. 3233 ◽  
Author(s):  
Karol Bukowski ◽  
Mateusz Kciuk ◽  
Renata Kontek
Keyword(s):  
Multidrug Resistance ◽  
Cancer Treatment ◽  
Anticancer Agents ◽  
Alkylating Agents ◽  
Gene Mutations ◽  
Resistance Mechanisms ◽  
Chemotherapeutic Agents ◽  
Future Research ◽  
Repair Capacity ◽  
Dna Repair Capacity

Cancer is one of the main causes of death worldwide. Despite the significant development of methods of cancer healing during the past decades, chemotherapy still remains the main method for cancer treatment. Depending on the mechanism of action, commonly used chemotherapeutic agents can be divided into several classes (antimetabolites, alkylating agents, mitotic spindle inhibitors, topoisomerase inhibitors, and others). Multidrug resistance (MDR) is responsible for over 90% of deaths in cancer patients receiving traditional chemotherapeutics or novel targeted drugs. The mechanisms of MDR include elevated metabolism of xenobiotics, enhanced efflux of drugs, growth factors, increased DNA repair capacity, and genetic factors (gene mutations, amplifications, and epigenetic alterations). Rapidly increasing numbers of biomedical studies are focused on designing chemotherapeutics that are able to evade or reverse MDR. The aim of this review is not only to demonstrate the latest data on the mechanisms of cellular resistance to anticancer agents currently used in clinical treatment but also to present the mechanisms of action of novel potential antitumor drugs which have been designed to overcome these resistance mechanisms. Better understanding of the mechanisms of MDR and targets of novel chemotherapy agents should provide guidance for future research concerning new effective strategies in cancer treatment.

scholarly journals Muscle Fatigue-Alleviating Effects of a Prescription Composed of Polygonati Rhizoma and Notoginseng Radix et Rhizoma

2020 ◽  
Vol 2020 ◽  
pp. 1-6
Author(s):  
Ya-Qin Yang ◽  
Yan-Qin Li ◽  
Li-Ping Yu ◽  
Xue Li ◽  
Jian-Kang Mu ◽  
...  
Keyword(s):  
Energy Metabolism ◽  
Muscle Fatigue ◽  
Weight Bearing ◽  
Herbal Medicines ◽  
Liver Glycogen ◽  
Serum Creatine Kinase ◽  
Oxidative Status ◽  
Major Research ◽  
Research Focus

Long-term muscle fatigue is a major cause of injury. Drugs/nutrients from herbal medicines that prevent fatigue remain a major research focus. In China, a prescription composed of Polygonati Rhizoma and Notoginseng Radix et Rhizoma has been commonly used as a herb and food nutrient, providing protection against fatigue in the clinic. To date, the mechanisms through which this prescription prevented fatigue are unknown. Here, we identified the effects of this prescription on muscle fatigue based on energy and oxidation regulation. Fatigue mouse models were produced through weight-bearing exhaustive swimming. Mice were intragastrically administered prescription extracts (1 and 2 g/kg) for four weeks. Changes in exhaustive swimming times, antifatigue biochemical indicators, oxidative status, and energy metabolism were investigated. The prescription prolonged the exhaustive swimming time of the mice. The content of lactic acid and blood urea nitrogen in the serum was also markedly reduced by the prescription. The content of liver glycogen and lactate dehydrogenase in the serum increased. The prescription also significantly reduced malondialdehyde levels and increased the levels of superoxide dismutase and glutathione peroxidase. The levels of ATPase, complexes I and II in the mitochondria of hind-leg skeletal muscle, and serum creatine kinase also increased in response to the prescription. Our results indicated that the prescription could effectively alleviate muscle fatigue status by promoting energy metabolism and antioxidation ability. The prescription therefore represents a useful drug/nutrient strategy to alleviate muscle fatigue.

scholarly journals The substrates and binding partners of protein kinase Cε

2010 ◽  
Vol 427 (2) ◽  
pp. 189-196 ◽  
Author(s):  
Philip M. Newton ◽  
Robert O. Messing
Keyword(s):  
Protein Kinase ◽  
Active Drug ◽  
Major Research ◽  
Research Focus ◽  
Cellular Mechanisms ◽  
Future Studies ◽  
Kinase C ◽  
Binding Partners ◽  
Signalling Cascades ◽  
Substrate Phosphorylation

The ε isoform of protein kinase C (PKCε) has important roles in the function of the cardiac, immune and nervous systems. As a result of its diverse actions, PKCε is the target of active drug-discovery programmes. A major research focus is to identify signalling cascades that include PKCε and the substrates that PKCε regulates. In the present review, we identify and discuss those proteins that have been conclusively shown to be direct substrates of PKCε by the best currently available means. We will also describe binding partners that anchor PKCε near its substrates. We review the consequences of substrate phosphorylation and discuss cellular mechanisms by which target specificity is achieved. We begin with a brief overview of the biology of PKCε and methods for substrate identification, and proceed with a discussion of substrate categories to identify common themes that emerge and how these may be used to guide future studies.

scholarly journals Combined Effect of Bortezomib and Menadione Sodium Bisulfite on Proteasomes of Tumor Cells: The Dramatic Decrease of Bortezomib Toxicity in a Preclinical Trial

Cancers ◽  
2018 ◽  
Vol 10 (10) ◽  
pp. 351 ◽  
Author(s):  
Tatiana Astakhova ◽  
Alexey Morozov ◽  
Pavel Erokhov ◽  
Maria Mikhailovskaya ◽  
Sergey Akopov ◽  
...  
Keyword(s):  
High Efficiency ◽  
Sodium Bisulfite ◽  
Proteasome Activity ◽  
26S Proteasome ◽  
Mammary Adenocarcinoma ◽  
Antitumor Drugs ◽  
Antitumor Effects ◽  
Preclinical Trial ◽  
Menadione Sodium Bisulfite

Tumor growth is associated with elevated proteasome expression and activity. This makes proteasomes a promising target for antitumor drugs. Current antitumor drugs such as bortezomib that inhibit proteasome activity have significant side effects. The purpose of the present study was to develop effective low-toxic antitumor compositions with combined effects on proteasomes. For compositions, we used bortezomib in amounts four and ten times lower than its clinical dose, and chose menadione sodium bisulfite (MSB) as the second component. MSB is known to promote oxidation of NADH, generate superoxide radicals, and as a result damage proteasome function in cells that ensure the relevance of MSB use for the composition development. The proteasome pool was investigated by the original native gel electrophoresis method, proteasome chymotrypsin-like activity—by Suc-LLVY-AMC-hydrolysis. For the compositions, we detected 10 and 20 μM MSB doses showing stronger proteasome-suppressing and cytotoxic in cellulo effects on malignant cells than on normal ones. MSB indirectly suppressed 26S-proteasome activity in cellulo, but not in vitro. At the same time, MSB together with bortezomib displayed synergetic action on the activity of all proteasome forms in vitro as well as synergetic antitumor effects in cellulo. These findings determine the properties of the developed compositions in vivo: antitumor efficiency, higher (against hepatocellular carcinoma and mammary adenocarcinoma) or comparable to bortezomib (against Lewis lung carcinoma), and drastically reduced toxicity (LD50) relative to bortezomib. Thus, the developed compositions represent a novel generation of bortezomib-based anticancer drugs combining high efficiency, low general toxicity, and a potentially expanded range of target tumors.

Sign in / Sign up

Export Citation Format

Share Document