Anti-Cancer Effects of Asiatic Acid, a Triterpene from Centilla asiatica L: A Review

2020 ◽  
Vol 20 (5) ◽  
pp. 536-547
Author(s):  
Muhammad T. Islam ◽  
Eunus S. Ali ◽  
Shaikh J. Uddin ◽  
Ishaq N. Khan ◽  
Manik C. Shill ◽  
...  
Keyword(s):  
Apoptotic Cell ◽  
Human Cancer ◽  
Biological Activities ◽  
Folk Medicine ◽  
Asiatic Acid ◽  
Inhibition Of Proliferation ◽  
Anti Cancer ◽  
Cancer Tumor ◽  
Anti Inflammatory ◽  
Anti Tumor Activity

Background: Centilla asiatica L is a medicinal herb that has been widely used in folk medicine to treat various diseases. Asiatic Acid (AA), a triterpene and a known component of this herb, has been shown to display important biological activities, including anti-inflammatory, antibacterial, antidiabetic and antihyperlipidemic, neuroprotective, anxiolytic and antidepressant, hepatoprotective, pancreas protective, and cardio- protective. Objective: This review focuses on AA’s anti-cancer effects on the basis of published literature found in a number of databases such as PubMed and Science Direct. Emphasis has been given to the mechanisms of action of its anti-cancer effect. Methods: A literature survey was conducted using known databases such as PubMed and Science Direct using the keywords ‘Asiatic acid’, pairing with ‘cancer’, ‘tumor’, ‘anti-cancer effect’, ‘cytotoxic effect’, ‘anti-tumor activity’, ‘cell line’, ‘animal cancer’, and ‘human cancer’. Results: Findings suggest that AA exerts anti-cancer effects in several test systems through various pathways, including oxidative/antioxidant, anti-inflammatory, cytotoxicity, apoptotic cell death, necrosis, anti-angiogenesis, inhibition of proliferation and cell migration, and chemoprevention. Conclusions: AA may be an effective plant-based cancer chemotherapeutic agent and a promising lead for the development of potent anticancer drugs.

Helenalin - A Sesquiterpene Lactone with Multidirectional Activity

2019 ◽  
Vol 20 (4) ◽  
pp. 444-452 ◽  
Author(s):  
Joanna Drogosz ◽  
Anna Janecka
Keyword(s):  
Sesquiterpene Lactone ◽  
Molecular Mechanisms ◽  
Biological Activities ◽  
Sesquiterpene Lactones ◽  
Folk Medicine ◽  
Biological Properties ◽  
Pathological Conditions ◽  
Anti Cancer ◽  
Anti Inflammatory ◽  
Minor Injuries

Sesquiterpene lactones, secondary metabolites of plants, present in a large number of species mostly from the Asteracea family, are used in the traditional medicine of many countries for the treatment of various pathological conditions. They exert a broad range of activities, including antiinflammatory, anti-bacterial and anti-cancer properties. The best-known sesquiterpene lactones which are already used as drugs or are used in clinical trials are artemisinin, thapsigargin and parthenolide. Yet another sesquiterpene lactone, helenalin, an active component of Arnica montana, known for its strong anti-inflammatory activity, has been used for centuries in folk medicine to treat minor injuries. Unfortunately, helenalin’s ability to cause allergic reactions and its toxicity to healthy tissues prevented so far the development of this sesquiterpene lactone as an anticancer or anti-inflammatory drug. Recently, the new interest in the biological properties, as well as in the synthesis of helenalin analogs has been observed. This review describes helenalin's major biological activities, molecular mechanisms of action, its toxicity and potential for further research.

Natural Sesquiterpene Lactones in the Prevention and Treatment of Inflammatory Disorders and cancer: A Systematic Study of this Emerging Therapeutic Approach based on Chemical and Pharmacological Aspect

2020 ◽  
Vol 17 (9) ◽  
pp. 1102-1116
Author(s):  
Sudip Kumar Mandal ◽  
Utsab Debnath ◽  
Amresh Kumar ◽  
Sabu Thomas ◽  
Subhash Chandra Mandal ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Biological Activities ◽  
Sesquiterpene Lactones ◽  
Structural Diversity ◽  
Cancer Drug ◽  
Cancer Drug Discovery ◽  
Anti Cancer ◽  
Drug Discovery Program ◽  
Anti Inflammatory ◽  
Family Based

Background and Introduction: Sesquiterpene lactones are a class of secondary metabolite that contains sesquiterpenoids and lactone ring as pharmacophore moiety. A large group of bioactive secondary metabolites such as phytopharmaceuticals belong to this category. From the Asteraceae family-based medicinal plants, more than 5,000 sesquiterpene lactones have been reported so far. Sesquiterpene lactone-based pharmacophore moieties hold promise for broad-spectrum biological activities against cancer, inflammation, parasitic, bacterial, fungal, viral infection and other functional disorders. Moreover, these moiety based phytocompounds have been highlighted with a new dimension in the natural drug discovery program worldwide after the 2015 Medicine Nobel Prize achieved by the Artemisinin researchers. Objective: These bitter substances often contain an α, β-unsaturated-γ-lactone as a major structural backbone, which in recent studies has been explored to be associated with anti-tumor, cytotoxic, and anti-inflammatory action. Recently, the use of sesquiterpene lactones as phytomedicine has been increased. This study will review the prospect of sesquiterpene lactones against inflammation and cancer. Methods: Hence, we emphasized on the different features of this moiety by incorporating its structural diversity on biological activities to explore structure-activity relationships (SAR) against inflammation and cancer. Results: How the dual mode of action such as anti-inflammatory and anti-cancer has been exhibitedby these phytopharmaceuticals will be forecasted in this study. Furthermore, the correlation of anti-inflammatory and anti-cancer activity executed by the sesquiterpene lactones for fruitful phytotherapy will also be revealed in the present review in the milieu of pharmacophore activity relation and pharmacodynamics study as well. Conclusion: So, these metabolites are paramount in phytopharmacological aspects. The present discussion on the future prospect of this moiety based on the reported literature could be a guide for anti-inflammatory and anti-cancer drug discovery programs for the upcoming researchers.

scholarly journals Chemical Constituents of Eupatorium japonicum and Anti-Inflammatory, Cytotoxic, and Apoptotic Activities of Eupatoriopicrin on Cancer Stem Cells

2021 ◽  
Vol 2021 ◽  
pp. 1-12
Author(s):  
Minh Giang Phan ◽  
Thi Thao Do ◽  
Thi Nga Nguyen ◽  
Thi Viet Huong Do ◽  
Ngoc Phuc Dong ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Sesquiterpene Lactones ◽  
No Production ◽  
Bioactive Constituents ◽  
Anti Inflammatory ◽  
First Time ◽  
Eupatorium Japonicum

Eupatorium japonicum Thunb. of the plant family Asteraceae is a popular traditional herb in Vietnam. However, its chemical constituents as well as bioactive principles have not been investigated yet. We investigated the phytochemistry of E. japonicum in Vietnam and isolated seventeen compounds (1–17) including phytosterols, terpenoids, phenolic acids, flavonoids, fatty alcohols, and fatty acids. They were structurally determined by MS and NMR analysis. Except for compounds 6 and 12, all the other compounds were identified for the first time from E. japonicum. Since many sesquiterpene lactones with α-methylene γ-lactone ring are reported as anti-inflammatory and anticancer agents, eupatoriopicrin (10), 1-hydroxy-8-(4,5-dihydroxytigloyloxy)eudesma-4(15),11(13)-dien-6,12-olide (11) were selected among the isolates for biological assays. Compound 10 was identified as the main bioactive sesquiterpene lactone of E. japonicum showing its potent anti-inflammatory and cytotoxic activity through inhibiting NO production and the growth of HepG2 and MCF-7 human cancer cell lines. For the first time, eupatoriopicrin (10) was demonstrated to strongly inhibit NTERA-2 human cancer stem cell (CSC) line in vitro. It is noticeable that the cytotoxicity of eupatoriopicrin against NTERA-2 cells is mediated by its apoptosis-inducing capability of 10 as demonstrated by the results of Hoechst 33342 staining, flow cytometry apoptosis analysis, and caspase-3 activity assays. The biological activities of the main bioactive constituents 1–7, 10, 12, and 15 supported the reported anti-inflammatory and anticancer properties of extracts from E. japonicum.

scholarly journals Effect of Three Centaurea Species Collected from Central Anatolia Region of Turkey on Human Melanoma Cells

2016 ◽  
Vol 11 (3) ◽  
pp. 1934578X1601100
Author(s):  
Alessandra Russo ◽  
Venera Cardile ◽  
Adriana C.E. Graziano ◽  
Daniela Rigano ◽  
Abdurrahman Aktumsek ◽  
...  
Keyword(s):  
Melanoma Cell Line ◽  
Apoptotic Cell ◽  
Biological Activities ◽  
Folk Medicine ◽  
Human Melanoma ◽  
Central Anatolia ◽  
Major Activity ◽  
Melanoma Cancer ◽  
Ongoing Effort ◽  
Asteraceae Family

Centaurea is the largest genus within the Asteraceae family. Many members of this genus are used in traditional folk medicine, such as Centaurea pulchella used to treat skin problems such as to resolve the abscess. Although biological activities of many Centaurea species have been investigated in different countries and Turkey, cytotoxic effect of C. patula, C. pulchella and C. tchihatcheffii has not been studied yet. Melanoma is one of the most invasive and deadly forms of skin cancer. Therefore, in an ongoing effort to identify new natural anticancer products for the treatment and/or prevention of melanoma cancer, the present study was undertaken to investigate the effect of these Centaurea species, collected from Central Anatolia region of Turkey on cell growth and death in human melanoma cell line, A375. The results revealed that all extracts were able to inhibit, after 48 h of treatment, the growth of cancer cells, that could be related to an overall action of the phenolic compounds present. In fact, C. pulchella, with the highest level of phenolics, showed a major activity followed by C. patula and C. tchihatcheffii. Our data also demonstrate that these natural products induce apoptotic cell death. In conclusion, the study of plant extracts for their cytotoxic and apoptotic properties has shown that medicinal herbs from Centaurea species might have also importance in the prevention and treatment of melanoma.

scholarly journals Veronicastrum axillare Alleviates Lipopolysaccharide-Induced Acute Lung Injury via Suppression of Proinflammatory Mediators and Downregulation of the NF-κB Signaling Pathway

2016 ◽  
Vol 2016 ◽  
pp. 1-9 ◽  
Author(s):  
Quanxin Ma ◽  
Kai Wang ◽  
Qinqin Yang ◽  
Shun Ping ◽  
Weichun Zhao ◽  
...  
Keyword(s):  
Acute Lung Injury ◽  
Lung Injury ◽  
Signaling Pathway ◽  
Biological Activities ◽  
Interleukin 1 ◽  
Folk Medicine ◽  
Protective Effects ◽  
Proinflammatory Mediators ◽  
Anti Inflammatory

Veronicastrum axillare is a traditional medical plant in China which is widely used in folk medicine due to its versatile biological activities, especially for its anti-inflammatory effects. However, the detailed mechanism underlying this action is not clear. Here, we studied the protective effects of V. axillare against acute lung injury (ALI), and we further explored the pharmacological mechanisms of this action. We found that pretreatment with V. axillare suppressed the release of proinflammatory cytokines in the serum of ALI mice. Histological analysis of lung tissue demonstrated that V. axillare inhibited LPS-induced lung injury, improved lung morphology, and reduced the activation of nuclear factor-κB (NF-κB) in the lungs. Furthermore, the anti-inflammatory actions of V. axillare were investigated in vitro. We observed that V. axillare suppressed the mRNA expression of interleukin-1β (IL-1β), IL-6, monocyte chemotactic protein-1 (MCP-1), cyclooxygenase-2 (COX-2), and tumor necrosis factor-α (TNF-α) in RAW264.7 cells challenged with LPS. Furthermore, pretreatment of V. axillare in vitro reduced the phosphorylation of p65 and IκB-α which is activated by LPS. In conclusion, our data firstly demonstrated that the anti-inflammatory effects of V. axillare against ALI were achieved through downregulation of the NF-κB signaling pathway, thereby reducing the production of inflammatory mediators.

scholarly journals New Oleoyl Hybrids of Natural Antioxidants: Synthesis and In Vitro Evaluation as Inducers of Apoptosis in Colorectal Cancer Cells

Antioxidants ◽  
2020 ◽  
Vol 9 (11) ◽  
pp. 1077
Author(s):  
Gabriele Carullo ◽  
Sarah Mazzotta ◽  
Adrian Koch ◽  
Kristin M. Hartmann ◽  
Oliver Friedrich ◽  
...  
Keyword(s):  
Healthy Lifestyle ◽  
Apoptotic Cell ◽  
Human Cancer ◽  
Natural Antioxidants ◽  
In Vitro Assays ◽  
Human Cancer Cell Lines ◽  
Cancer Management ◽  
Anti Cancer ◽  
Colorectal Cancer Cells

Nowadays, the beneficial role of a healthy lifestyle, particularly emphasizing the quality of foods and cancer management, is accepted worldwide. Polyphenols and oleic acid play a key role in this context, but are still scarcely used as anti-cancer agents due to their bio-accessibility limits. Therefore, we aimed to synthesize a set of new oleoyl-hybrids of quercetin, morin, pinocembrin, and catechin to overcome the low bioavailability of polyphenols, throughout a bio-catalytic approach using pancreatic porcine lipase as a catalyst. The in vitro assays, using a wide panel of human cancer cell lines showed, mainly for two novel regioisomer oleoyl-hybrids of quercetin, a remarkable increase in apoptotic cell populations. We suggested that the DNA damage shown as ɣH2AX signals might be the major cause of apoptotic cell death. Finally, we demonstrated convincing data about two novel polyphenol-based hybrids displaying a highly selective anti-cancer cytotoxicity and being superior compared to their reference/parental compounds.

scholarly journals Metabolomic Profiling, Antioxidant and Anti-inflammatory Activities of Hypericum Species Growing in South Korea

2017 ◽  
Vol 12 (7) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Heung Joo Yuk ◽  
Kyeong Yeol Oh ◽  
Doo-Young Kim ◽  
Hyuk-Hwan Song ◽  
Jun Young Kim ◽  
...  
Keyword(s):  
Biological Activities ◽  
Chemical Constituents ◽  
Folk Medicine ◽  
Principal Component ◽  
Ultra Performance Liquid Chromatography ◽  
Raw 264.7 Cells ◽  
Bioactive Metabolites ◽  
Flight Mass Spectrometry ◽  
Anti Inflammatory ◽  
Hypericum Species

Although Hypericum species are best known as plants that produce hypericin and are used in folk medicine, their other chemical constituents are poorly understood. Polyphenolic secondary metabolites from whole plants of representative Korean Hypericum species ( H. laxum Koidz., H. erectum Thunb., and H. ascyron L.) were analyzed using a ultra performance liquid chromatography-quadrupole time-of-flight/mass spectrometry (UPLC-Q-TOF/MS)-based approach combined with unsupervised principal component analysis (PCA) multivariate analysis. On the loading scatter plot, significant changes in metabolites were found between species, and three flavonol glycosides (8: quercetin-3- O-galactoside, 12: kaempferol-3- O-glucoside, and 13: quercetin-3- O-rhamnoside) were evaluated as key markers among 17 isolated metabolites. The extracts of H. laxum Koidz. exhibited significant quenching effects on DPPH and ABTS radicals, with IC50 values of 10–20 μg/mL, and were slightly higher in total phenol (TP) and total flavonoid (TF) contents than other species. Additionally, anti-inflammatory activity was observed by reduced nitric oxide (NO) and interleukin-6 (IL-6) production from lipopolysaccharide (LPS)-stimulated macrophages (RAW 264.7 cells). This is the first study to report the presence of bioactive metabolites and their correlating biological activities in H. laxum Koidz.

scholarly journals Nanoformulation of a Novel Pyrano[2,3-c] Pyrazole Heterocyclic Compound AMDPC Exhibits Anti-Cancer Activity via Blocking the Cell Cycle through a P53-Independent Pathway

Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 624 ◽  
Author(s):  
Xuanrong Sun ◽  
Longchao Zhang ◽  
Mengshi Gao ◽  
Xiangjie Que ◽  
Chenfeng Zhou ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Cancer Cells ◽  
Biological Activities ◽  
Polymeric Micelle ◽  
In Vivo Studies ◽  
One Pot ◽  
Anti Cancer ◽  
G2 Phase ◽  
Anti Tumor Activity

Pyrano[2,3-c]pyrazole derivatives have been reported as exerting various biological activities. One compound with potential anti-tumor activity was screened out by MTT assay from series of dihydropyrazopyrazole derivatives we had synthesized before using a one-pot, four-component reaction, and was named as 6-amino-4-(2-hydroxyphenyl)-3-methyl-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile (hereinafter abbreviated as AMDPC). The IC50 of AMDPC against Bcap-37 breast cancer cells was 46.52 μg/mL. Then the hydrophobic AMDPC was encapsulated in PEG-PLGA block copolymers, and then self-assembled as polymeric micelle (mPEG-PLGA/AMDPC) to improve both physiochemical and release profiles. The effect of mPEG-PLGA/AMDPC on BCAP-37 cancer cells showed similar anti-tumor effects as AMDPC. Furthermore, the anti-tumor mechanism of mPEG-PLGA/AMDPC was investigated, which can probably be attributed to stimulating the expression of P21 gene and therefore protein production on BCAP-37 cells, and then blocked the cell cycle through the P53-independent pathway both in S phase and G2 phase. Thus, mPEG-PLGA/AMDPC is a promising therapeutic agent for cancer treatment, and further in vivo studies will be developed.

scholarly journals Biochemical Basis of Anti-Cancer-Effects of Phloretin—A Natural Dihydrochalcone

Molecules ◽  
2019 ◽  
Vol 24 (2) ◽  
pp. 278 ◽  
Author(s):  
Bu Choi
Keyword(s):  
Cancer Cells ◽  
Tumor Cells ◽  
Human Cancer ◽  
Cancer Drug ◽  
Biochemical Basis ◽  
Human Cancer Cells ◽  
Anti Cancer ◽  
Anti Inflammatory ◽  
Natural Agent ◽  
Growth Of Tumor

Apple is a rich source of bioactive phytochemicals that help improve health by preventing and/or curing many disease processes, including cancer. One of the apple polyphenols is phloretin [2′,4′,6′-Trihydroxy-3-(4-hydroxyphenyl)-propiophenone], which has been widely investigated for its antioxidant, anti-inflammatory and anti-cancer activities in a wide array of preclinical studies. The efficacy of phloretin in suppressing xenograft tumor growth in athymic nude mice implanted with a variety of human cancer cells, and the ability of the compound to interfere with cancer cells signaling, have made it a promising candidate for anti-cancer drug development. Mechanistically, phloretin has been reported to arrest the growth of tumor cells by blocking cyclins and cyclin-dependent kinases and induce apoptosis by activating mitochondria-mediated cell death. The blockade of the glycolytic pathway via downregulation of GLUT2 mRNA and proteins, and the inhibition of tumor cells migration, also corroborates the anti-cancer effects of phloretin. This review sheds light on the molecular targets of phloretin as a potential anti-cancer and anti-inflammatory natural agent.

Cytotoxicity and Anti-cancer Activity of the Genus Achillea L.

2020 ◽  
Vol 27 (41) ◽  
pp. 6910-6925 ◽  
Author(s):  
Konstantina Papakosta ◽  
Maria-Eleni Grafakou ◽  
Christina Barda ◽  
Ioannis V. Kostopoulos ◽  
Ourania Tsitsilonis ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Traditional Medicine ◽  
Human Cancer ◽  
Biological Activities ◽  
Northern Greece ◽  
Human Cancer Cell Lines ◽  
Anti Cancer ◽  
Analgesic Agents ◽  
Selection Of

Background: The genus Achillea L. is rich in bioactive sesquiterpenes and flavonoids; most of the studied species exhibit several biological activities and are used as emmenagogue, wound healing and analgesic agents. Some species are also used in local folklore medicine. Objective: Following a literature survey, we discuss the anti-cancer properties of Achillea species, taking into consideration ethnopharmacological data on their use in traditional medicine for the treatment of cancer. In addition, we screened extracts and isolated secondary metabolites from A. coarctata for cytotoxicity, upon information based on local traditional medicine. The plant was collected in Kozani (Northern Greece), where it is locally used for treating gastrointestinal disorders, including stomach cancer. Methods: A selection of the relevant data was performed through a search in PubMed, Scopus, Google Scholar and Science Direct databases. In addition, extracts and isolated compounds from A. coarctata were tested for their in vitro activity against the human cancer cell lines MCF-7 and HeLa. Conclusion: The genus Achillea L. is a valuable source of bioactive secondary metabolites. The most significant outcome of the investigation of medicinal plants is the documentation and the assessment of the traditional information and its use and perspectives in the light of modern pharmacology.

Sign in / Sign up

Export Citation Format

Share Document