scholarly journals Baicalein-Enriched Fraction Extracted from Oroxylum indicum (L.) Benth. ex Kurz Leaves Exerts Antioxidant and Inhibitory Effects Against Glioblastoma Multiforme

Processes ◽  
2019 ◽  
Vol 7 (12) ◽  
pp. 963 ◽  
Author(s):  
In Nee Kang ◽  
Nik Nur Hakimah Nik Salleh ◽  
Wan Jie Chung ◽  
Chong Yew Lee ◽  
Suat Cheng Tan
Keyword(s):  
Glioblastoma Multiforme ◽  
Crude Extract ◽  
Therapeutic Potential ◽  
Antioxidant Properties ◽  
Extraction Procedure ◽  
Inhibitory Effect ◽  
Extraction System ◽  
Oroxylum Indicum ◽  
Fractionation Procedure ◽  
Anti Cancer

Glioblastoma multiforme (GBM) is the most malignant subtype of primary brain cancer. To date, standard clinical treatment for GBM is limited in effectiveness and could impose additional side effects. Recently, numerous bioactive compounds isolated from natural plants appear to have beneficial anti-cancer properties. Here, the GBM inhibitory effect of baicalein, a bioactive flavonoid extracted from Oroxylum indicum (L.) Benth. ex Kurz, was evaluated. Firstly, three solvents were used to extract the baicalein. We found that the binary extraction system, using a combination of petroleum ether and methanol (PM), yielded the highest amount of baicalein (15%) compared to the mono extraction system using methanol (13%) or aqueous (0.04%) only. In order to further enhance the baicalein yield in PM crude extract, it was subjected to an enrichment fractionation procedure, which successfully increased the baicalein by nearly two-fold from the initial crude extract (15%) to the enriched fraction 5 (F5) (29%). The enriched F5 not only showed significantly higher (~2.5-fold) antioxidant properties as compared to the crude extract, it was also found to significantly suppress GBM cell proliferation ~2.5-fold better than the crude extract. In conclusion, this study successfully optimized an extraction procedure for increased yield of baicalein metabolite from O. indicum leaves and enhanced its therapeutic potential for GBM treatment.

scholarly journals Inhibitory Effect onIn VitroLDL Oxidation and HMG Co-A Reductase Activity of the Liquid-Liquid Partitioned Fractions ofHericium erinaceus(Bull.) Persoon (Lion’s Mane Mushroom)

2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Mohammad Azizur Rahman ◽  
Noorlidah Abdullah ◽  
Norhaniza Aminudin
Keyword(s):  
Therapeutic Potential ◽  
Reductase Activity ◽  
Antioxidant Properties ◽  
Density Lipoprotein ◽  
Thiobarbituric Acid ◽  
Inhibitory Effect ◽  
Hexane Fraction ◽  
Ldl Oxidation ◽  
Hericium Erinaceus

Oxidation of low-density lipoprotein (LDL) has been strongly suggested as the key factor in the pathogenesis of atherosclerosis. Mushrooms have been implicated in having preventive effects against chronic diseases due especially to their antioxidant properties. In this study,in vitroinhibitory effect ofHericium erinaceuson LDL oxidation and the activity of the cholesterol biosynthetic key enzyme, 3-hydroxy-3-methyl glutaryl coenzyme A (HMG Co-A) reductase, was evaluated using five liquid-liquid solvent fractions consisting of methanol : dichloromethane (M : DCM), hexane (HEX), dichloromethane (DCM), ethyl acetate (EA), and aqueous residue (AQ). The hexane fraction showed the highest inhibition of oxidation of human LDL as reflected by the increased lag time (100 mins) for the formation of conjugated diene (CD) at 1 µg/mL and decreased production (68.28%, IC500.73 mg/mL) of thiobarbituric acid reactive substances (TBARS) at 1 mg/mL. It also mostly inhibited (59.91%) the activity of the HMG Co-A reductase at 10 mg/mL. The GC-MS profiling of the hexane fraction identified the presence of myconutrients:inter alia, ergosterol and linoleic acid. Thus, hexane fraction ofHericium erinaceuswas found to be the most potentin vitroinhibitor of both LDL oxidation and HMG Co-A reductase activity having therapeutic potential for the prevention of oxidative stress-mediated vascular diseases.

scholarly journals Anti-tumor effect of fruit rind of Myristica malabarica in an Ehrlich ascites carcinoma model

2019 ◽  
Vol 8 (3) ◽  
pp. 383
Author(s):  
Chandrakana Bandyopadhyay ◽  
Alak Manna ◽  
Soumita De ◽  
Nafisha Yasmin ◽  
Ajay K. Bauri ◽  
...  
Keyword(s):  
Crude Extract ◽  
Hematological Parameters ◽  
Ehrlich Ascites Carcinoma ◽  
Inhibitory Effect ◽  
Renal Functions ◽  
Ehrlich Ascites ◽  
Anti Cancer ◽  
Anti Tumor Activity ◽  
Fruit Rind

Background: Among the various modalities of anti-cancer treatment, cancer chemotherapy plays a very vital role. The alarming side effects being its main drawback leads to relentless research for newer agents. A new natural agent with promising anti-cancer properties from in-vitro studies leads to this study. Here we have evaluated the anti-tumor activity of a crude extract of fruit rind of Myristica malabarica in an Ehrlich ascites carcinoma model in mice.Methods: A murine model of cancer was established with i.p. inoculation of Ehrlich Ascites carcinoma (EAC) cells; animals were divided into five groups (including normal control) to observe the inhibitory effect of a crude extract of the fruit rind of Myristica malabarica/rampatri (0-100mg/kg b.w. i.p.) as compared with methotrexate (0.4mg/kg bw., i.p.). Blood and ascitic fluid were collected on the 10th day for analysis.Results: In the EAC model, there was an increase in tumor volume, tumor weight, and tumor packed cell volume, which was decreased by rampatri (50 and 100mg/kg bw) along with an increase in the mean survival time (MST). Rampatri caused minimal alterations in hematological parameters, renal functions remained unchanged but an increase in hepatic SGOT was demonstrated.Conclusions: The crude extract of rampatri (containing Malabaricones) exhibited significant anti-tumor activity with minimal effect on hematological and renal functions.

scholarly journals An Overview on the Anti-inflammatory Potential and Antioxidant Profile of Eugenol

2018 ◽  
Vol 2018 ◽  
pp. 1-9 ◽  
Author(s):  
Joice Nascimento Barboza ◽  
Carlos da Silva Maia Bezerra Filho ◽  
Renan Oliveira Silva ◽  
Jand Venes R. Medeiros ◽  
Damião Pergentino de Sousa
Keyword(s):  
Oxidative Stress ◽  
Therapeutic Potential ◽  
Inflammatory Diseases ◽  
Antioxidant Properties ◽  
Redox Status ◽  
Inhibitory Effect ◽  
New Drugs ◽  
Inflammatory Processes ◽  
Anti Inflammatory

The bioactive compounds found in foods and medicinal plants are attractive molecules for the development of new drugs with action against several diseases, such as those associated with inflammatory processes, which are commonly related to oxidative stress. Many of these compounds have an appreciable inhibitory effect on oxidative stress and inflammatory response, and may contribute in a preventive way to improve the quality of life through the use of a diet rich in these compounds. Eugenol is a natural compound that has several pharmacological activities, action on the redox status, and applications in the food and pharmaceutical industry. Considering the importance of this compound, the present review discusses its anti-inflammatory and antioxidant properties, demonstrating its mechanisms of action and therapeutic potential for the treatment of inflammatory diseases.

scholarly journals Luteolin, an emerging anti-cancer flavonoid, poisons eukaryotic DNA topoisomerase I

2002 ◽  
Vol 366 (2) ◽  
pp. 653-661 ◽  
Author(s):  
Arnab Roy CHOWDHURY ◽  
Shalini SHARMA ◽  
Suparna MANDAL ◽  
Anindya GOSWAMI ◽  
Sibabrata MUKHOPADHYAY ◽  
...  
Keyword(s):  
Catalytic Activity ◽  
Topoisomerase I ◽  
Therapeutic Potential ◽  
Wide Spectrum ◽  
Inhibitory Effect ◽  
Dna Topoisomerase I ◽  
Dna Topoisomerase ◽  
Mouse Splenocytes ◽  
Anti Cancer ◽  
Eukaryotic Dna

Luteolin, a naturally occurring flavonoid, is abundant in our daily dietary intake. It exhibits a wide spectrum of pharmacological properties, but little is known about its biochemical targets other than the fact that it induces topoisomerase II-mediated apoptosis. In the present study, we show that luteolin completely inhibits the catalytic activity of eukaryotic DNA topoisomerase I at a concentration of 40μM, with an IC50 of 5μM. Preincubation of enzyme with luteolin before adding a DNA substrate increases the inhibition of the catalytic activity (IC50 = 0.66μM). Treatment of DNA with luteolin before addition of topoisomerase I reduces this inhibitory effect. Subsequent fluorescence tests show that luteolin not only interacts directly with the enzyme but also with the substrate DNA, and intercalates at a very high concentration (>250μM) without binding to the minor groove. Direct interaction between luteolin and DNA does not affect the assembly of the enzyme–DNA complex, as evident from the electrophoretic mobility-shift assays. Here we show that the inhibition of topoisomerase I by luteolin is due to the stabilization of topoisomerase-I DNA-cleavable complexes. Hence, luteolin is similar to camptothecin, a class I inhibitor, with respect to its ability to form the topoisomerase I-mediated ‘cleavable complex'. But, unlike camptothecin, luteolin interacts with both free enzyme and substrate DNA. The inhibitory effect of luteolin is translated into concanavalin A-stimulated mouse splenocytes, with the compound inducing SDS–K+-precipitable DNA–topoisomerase complexes. This is the first report on luteolin as an inhibitor of the catalytic activity of topoisomerase I, and our results further support its therapeutic potential as a lead anti-cancer compound that poisons topoisomerases.

scholarly journals Gallotannin-Enriched Fraction from Quercus infectoria Galls as an Antioxidant and Inhibitory Agent against Human Glioblastoma Multiforme

Plants ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 2581
Author(s):  
Nur Alisa Kamarudin ◽  
Nik Nur Hakimah Nik Salleh ◽  
Suat Cheng Tan
Keyword(s):  
Glioblastoma Multiforme ◽  
Crude Extract ◽  
High Efficiency ◽  
Antioxidant Activities ◽  
Rapid Development ◽  
Extraction Procedure ◽  
Phase System ◽  
Inhibitory Effects ◽  
Two Phase ◽  
Quercus Infectoria

In recent years, herbal medicine has experienced rapid development in the search for alternative anticancer compounds. Various phytochemicals present in Quercus infectoria (QI) galls have been reported to trigger cytotoxic effects on many types of cancer cells. However, a specific active constituent of QI galls with the potential to inhibit highly invasive stage IV malignant brain tumor, glioblastoma multiforme (GBM), is yet to be discovered. In this study, a two-phase system composed of aqueous soxhlet extraction and methanolic enrichment fractionation was employed to extract an anticancer compound, gallotannin, from the QI galls. This optimized two-phase system successfully generated a fraction (F4) with ~71% gallotannin, verified by the TLC and HPLC assays. Astoundingly, this fraction showed significantly higher (~1.15-fold) antioxidant activities compared to its crude extract, as well as to a commercial synthetic pure gallotannin. The F4 was also found to significantly suppress GBM cell growth, better than the synthetic pure gallotannin and the QI gall crude extract, probably related to its significantly higher antioxidant property. Moreover, the inhibitory effects exerted by the F4 treatment on GBM cells were comparable to the effects of two clinically used chemo-drugs (Temozolomide and Tamoxifen), indicating its high efficiency in combating human cancer. In conclusion, this study pioneered the development of an optimized extraction procedure for enriched yield of the natural gallotannin metabolite from the galls of the QI medicinal plant with high antioxidant potential and inhibitory effects on human GBM cells.

Biological role of AKT, and regulation of AKT signaling pathway by thymoquinone: perspectives in cancer therapeutics

2020 ◽  
Vol 20 ◽  
Author(s):  
Md. Junaid ◽  
Yeasmin Akter ◽  
Syeda Samira Afrose ◽  
Mousumi Tania ◽  
Md. Asaduzzaman Khan
Keyword(s):  
Clinical Trials ◽  
Signaling Pathways ◽  
Signaling Pathway ◽  
Inhibitory Effect ◽  
Akt Signaling ◽  
Review Article ◽  
Therapeutic Drug ◽  
Akt Signaling Pathway ◽  
Anti Cancer

Background: AKT/PKB is an important enzyme with numerous biological functions, and its overexpression is related to the carcinogenesis. AKT stimulates different signaling pathways that are downstream of activated tyrosine kinases and phosphatidylinositol 3-kinase, hence functions as an important target for anti-cancer drugs. Objective: In this review article, we have interpreted the role of AKT signaling pathways in cancer and natural inhibitory effect of Thymoquinone (TQ) in AKT and its possible mechanism. Method: We have collected the updated information and data on AKT, their role in cancer and inhibitory effect of TQ in AKT signaling pathway from google scholar, PubMed, Web of Science, Elsevier, Scopus and many more. Results: There are many drugs already developed, which can target AKT, but very few among them have passed clinical trials. TQ is a natural compound, mainly found in black cumin, which has been found to have potential anti-cancer activities. TQ targets numerous signaling pathways, including AKT, in different cancers. In fact, many studies revealed that AKT is one of the major targets of TQ. The preclinical success of TQ suggests its clinical studies on cancer. Conclusion: This review article summarizes the role of AKT in carcinogenesis, its potent inhibitors in clinical trials, and how TQ acts as an inhibitor of AKT and TQ’s future as a cancer therapeutic drug.

Phytochemical, Pharmacological Activities and Ayurvedic Significances of Magical Plant Mimosa pudica Linn

2020 ◽  
Vol 17 ◽  
Author(s):  
Vijay Kumar
Keyword(s):  
Therapeutic Potential ◽  
Wide Spectrum ◽  
Chemical Constituents ◽  
Future Research ◽  
Mimosa Pudica ◽  
Pharmacological Activities ◽  
Medicinal Uses ◽  
Traditional Medicines ◽  
Crude Extracts ◽  
Anti Cancer

: Mimosa pudica Linn is an integrated part of Traditional Medicines Systems of India, China, Africa, Korea and America. It has been used from centuries in traditional medicines to cure different diseases like fever, diabetes, constipation, jaundice, ulcers, biliousness, and dyspepsia. It is an important ingredient of wide class of herbal formulations. To assess the scientific evidence for therapeutic potential of Mimosa pudica Linn and to identify the gaps for future research. The available information on the ethno-medicinal uses, phytochemistry, pharmacology and toxicology of Mimosa pudica Linn was collected via a library and electronic searches in Sci-Finder, Pub-Med, Science Direct, Google Scholar for the period, 1990 to 2020. In traditional medicinal systems, variety of ethno-medicinal applications of Mimosa pudica Linn has been noticed. Phytochemical investigation has resulted in identification of 40 well known chemical constituents, among which alkaloids, phenols and flavionoids are the predominant groups. The crude extracts and isolates have exhibited a wide spectrum of in vitro and in vivo pharmacological activities including anti-cancer, anti-inflammation, osteoporosis, neurological disorders, hypertension etc.. To quantify the Mimosa pudica Linn and its formulations, analytical techniques like HPLC and HPTLC has shown dominancy with good range of recovery and detection limit. Mimosa pudica Linn is the well-known herb since an ancient time. The pharmacological results supported some of the applications of Mimosa pudica Linn in traditional medicine systems. Perhaps, the predominance of alkaloids, phenols and flavionoids are responsible for the pharmacological activities the crude extracts and isolates of Mimosa pudica Linn. Further, there is need to isolate and evaluate the active chemical constituents of Mimosa pudica Linn having significant medicinal values. In future, it is important to study the exact mechanism associated with the phytochemicals of Mimosa pudica Linn especially on anti-cancer activities. Notably, toxicity studies on Mimosa pudica Linn are limited which are to be explored in future for the safe application of Mimosa pudica Linn and its formulations.

Synergistic Antitumor Effect of 5-Fluorouracil Combined with Constituents from Pleurospermum lindleyanum in Hepatocellular carcinoma SMMC-7721 Cells

2020 ◽  
Vol 20 ◽  
Author(s):  
Xiao-Feng Zhu ◽  
Xiao-Jin Li ◽  
Zhong-Lian Cao ◽  
Xiu-Jie Liu ◽  
Ping Yang ◽  
...  
Keyword(s):  
Hepatocellular Carcinoma ◽  
Treatment Effectiveness ◽  
Synergistic Effects ◽  
Folk Medicine ◽  
Inhibitory Effect ◽  
Caspase 9 ◽  
Whole Plant ◽  
Anti Cancer ◽  
Induced Apoptosis

Background: A Chinese folk medicine plant Pleurospermum lindleyanum possesses pharmacological activities of heat-clearing, detoxifying and preventing from hepatopathy, coronary heart disease, hypertension, and high altitude sickness. We isolated and characterized its constituents to investigate its synergistic effects against human hepatoma SMMC-7721 cells. Objective: The aim of this study was to explore the synergistic anti-cancer activities of isolates from P. lindleyanum with 5-FU on hepatoma SMMC-7721 cells in vitro and their primary mechanisms. Methods: Sequential chromatographic techniques were conducted for the isolation studies. The isolates structures were established by spectroscopic analysis as well as X-ray crystallographic diffraction. Growth inhibition was detected by MTT assay. The isobologram method was used to assess the effect of drug combinations. Flow cytometry and western blot were used to examine apoptosis and protein expression. Results: A new coumarin (16), along with sixteen known compounds, were isolated from the whole plant of P. lindleyanum and their structures were elucidated by spectroscopic methods. Four coumarins (2, 3, 5, and 16), two flavonoids (8 and 9) and three phytosterols and triterpenes (12-14) were found to synergistically enhance the inhibitory effect of 5-FU against SMMC-7721 cells. Among them, compounds 3 and 16 exhibited the best synergistic effects with IC50 of 5-FU reduced by 16-fold and 22-fold possessing the minimum Combination Index (CI) 0.34 and 0.27. The mechanism of action of combinations might be through synergistic arresting for the cell cycle at G1 phases and the induction of apoptosis. Moreover, western blotting and molecular docking revealed that compounds 3 or 5 might promote 5-FU-induced apoptosis by regulating the expression of Caspase 9 and PARP. Conclusion: Constituents from P. lindleyanum may improve the treatment effectiveness of 5-FU against hepatocellular carcinoma cells.

Resveratrol as an Enhancer of Apoptosis in Cancer: A Mechanistic Review

2020 ◽  
Vol 20 ◽  
Author(s):  
Milad Ashrafizadeh ◽  
Shahram Taeb ◽  
Hamed Haghi-Aminjan ◽  
Shima Afrashi ◽  
Kave Moloudi ◽  
...  
Keyword(s):  
Stem Cells ◽  
Cancer Stem Cells ◽  
Cancer Cells ◽  
Fas Ligand ◽  
Inhibitory Effect ◽  
Mitochondrial Pathway ◽  
Multi Drug Resistance ◽  
Chemotherapy Drugs ◽  
Normal Tissues ◽  
Anti Cancer

: Resistance of cancer cells to therapy is a challenge for achieving an appropriate therapeutic outcome. Cancer (stem) cells possess several mechanisms for increasing their survival following exposure to toxic agents such as chemotherapy drugs, radiation as well as immunotherapy. Evidences show that apoptosis plays a key role in response of cancer (stem) cells and their multi drug resistance. Modulation of both intrinsic and extrinsic pathways of apoptosis can increase efficiency of tumor response and amplify the therapeutic effect of radiotherapy, chemotherapy, targeted therapy and also immunotherapy. To date, several agents as adjuvant have been proposed to overcome resistance of cancer cells to apoptosis. Natural products are interesting because of low toxicity on normal tissues. Resveratrol is a natural herbal agent that has shown interesting anti-cancer properties. It has been shown to kill cancer cells selectively, while protecting normal cells. Resveratrol can augment reduction/oxidation (redox) reactions, thus increases the production of ceramide and the expression of apoptosis receptors such as Fas ligand (FasL). Resveratrol also triggers some pathways which induce mitochondrial pathway of apoptosis. On the other hand, resveratrol has an inhibitory effect on anti-apoptotic mediators such as nuclear factor κ B (NFκB), cyclooxygenase-2 (COX-2), phosphatidylinositol 3–kinase (PI3K) and mTOR. In this review, we explain the modulatory effects of resveratrol on apoptosis, which can augment the therapeutic efficiency of anti-cancer drugs or radiotherapy.

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