In Vitro Estrogenic and Breast Cancer Inhibitory Activities of Chemical Constituents Isolated from Rheum undulatum L.

Breast cancer is reported to rank fifth among all types of cancer with a case of death of 6.6%. In the Central Kalimantan region, early examinations of cancers including breast cancer were carried out and 247 tumors in the breast were identified (1.76%). Kelakai (Stenochlaena palustris) as one of the typical plants of Kalimantan which contain natural chemical constituents has been reported to be effective as an anti-inflammatory and antioxidant, so that with this potential can be developed to overcome diseases associated with it, one of them is breast cancer. This study aimed to examine the cytotoxicity of MCF-7 breast cancer cells using ethanol extract. The cytotoxicity assay of kelakai extract against MCF-7 cells conducted in vitro by the MTT reduction method. The variation of concentration used is 1000; 500; 250; 125; 62.5; 31.5; and 15.625 µg/ml, doxorubicin as a positive control was performed in a concentration of 1 μg / ml. The results of the cytotoxicity assay showed that the kelakai extract had a toxic effect on MCF-7 cells with an IC50 value of 493.57 µg / ml.

Download Full-text

Evaluation of Antioxidant and α-glucosidase Inhibitory Activities of Codonopsisjavanica (Blume) Hook. f. Thoms’ Root Extract

VNU Journal of Science Medical and Pharmaceutical Sciences ◽

10.25073/2588-1132/vnumps.4267 ◽

2020 ◽

Vol 36 (3) ◽

Author(s):

Nguyen Thi Thuy ◽

Ngo Ha Linh Trang ◽

Nguyen Thi Thanh Binh ◽

Bui Thanh Tung

Keyword(s):

Ethyl Acetate ◽

Inhibitory Activity ◽

Chemical Constituents ◽

Radical Scavenging ◽

Diabetes Type 2 ◽

Ethyl Acetate Fraction ◽

Diabetes Type ◽

Inhibitory Activities

This study aims to evaluate the antioxidant ability and α-glucosidase inhibitory activities of Codonopsisjavanica extract to elucidate its mechanism in the treatment of diabetes type 2. The roots of Codonopsisjavanica were extracted with ethanol solvents and fractionated with n-hexane, ethyl acetate and butanol solvents. The total extract and the fractions were evaluated for free radical scavenging by 2.2-diphenyl-1-picrylhydrazyl method and α-glucosidase inhibitory activity in vitro. The study results show that ethyl acetate fraction from Codonopsisjavanica roots had the strongest antioxidant activity with a value of IC50 of 80.6 ± 2.8 µg/mL and a strong α-glucosidase enzyme inhibitory activity with a value of IC50 of 80.4 ± 5 µg/mL. These data suggest that ethyl acetate fraction from Codonopsisjavanica roots may have potential for the prevention and treatment of diabetes type 2. Keywords Codonopsisjavanica, diabetes type 2, α-glucosidase, antioxidant ability, fraction. References [1] B.Y. Te. Guidelines for the diagnosis and treatment of type 2 diabetes, 2017.[2] U. Asmat, K. Abad, K. Ismail. Diabetes mellitus and oxidative stress-A concise review. Saudi pharmaceutical journal 24(5) (2016) 547.[3] D.K. Thu, V.M. Hung, N.T. Trang, B.T. Tung. Study on α-glucosidase enzyme inhibitory activity and DPPH free radical scavenging of green coffee bean extract (Coffea canephora). VNU Journal of Science: Medical and Pharmaceutical Sciences 35(2) (2019).[4] C.Y. Li, H.X. Xu, Q.B. Han, T.S. Wu. Quality assessment of Radix Codonopsis by quantitative nuclear magnetic resonance. Journal of Chromatography A 1216(11) (2009) 2124.[5] S.M. Gao, J.S. Liu, M. Wang, T.T. Cao, Y.D. Qi, B.G. Zhang, et al. Traditional uses, phytochemistry, pharmacology and toxicology of Codonopsis: A review. Journal of ethnopharmacology 219((2018) 50.[6] T.T. Ha, H.V. Oanh, D.T. Ha. Chemical constituents of the n-butanol fractions from the roots of Vietnamese Codonopsis javanica (Blume) Hook.f. Journal of Pharmacy 56(4) (2016).[7] T.T. Ha, N.M. Khoi, N.T. Ha, N.V. Nghi, D.T. Ha. Chemical Constituents from Roots of Codonopsis javanica (Blume) Hook.f. Journal of Medicinal Materials 19((2014) 211.[8] B.T. Tung, D.K. Thu, N.T.K. Thu, N.T. Hai. Antioxidant and acetylcholinesterase inhibitory activities of ginger root (Zingiber officinale Roscoe) extract. Journal of Complementary and Integrative Medicine 14(4) (2017).[9] B.T. Tung, D.K. Thu, P.T. Hai, N.T. Hai. Evaluation of α-glucosidase inhibitory effects of Pomegranate fruit extracts (Punica granatum Linn). Journal of Traditional Vietnamese Medicine and Pharmacy 5(18) (2018) 59.[10] F. Moradi-Afrapoli, B. Asghari, S. Saeidnia, Y. Ajani, M. Mirjani, M. Malmir, et al. In vitro α-glucosidase inhibitory activity of phenolic constituents from aerial parts of Polygonum hyrcanicum. DARU Journal of Pharmaceutical Sciences 20(1) (2012) 37.[11] D.T. Bao. Free radicals. Journal of Pharmacy 6((2001) 29.[12] M. Carocho, I.C. Ferreira. A review on antioxidants, prooxidants and related controversy: natural and synthetic compounds, screening and analysis methodologies and future perspectives. Food and chemical toxicology 51((2013) 15.[13] National Institute of Medicinal Materials. Method for studying the pharmacological effects of herbal drugs. Science and Technology Publishing House, 2006.[14] J.W. Baynes. Role of oxidative stress in development of complications in diabetes. Diabetes 40(4) (1991) 405.[15] S.M. Jeon, S.Y. Kim, I.H. Kim, J.S. Go, H.R. Kim, J.Y. Jeong, et al. Antioxidant activities of processed Deoduck (Codonopsis lanceolata) extracts. Journal of the Korean Society of Food Science and Nutrition 42(6) (2013) 924.[16] C.S. Yoo, S.J. Kim. Methanol extract of Codonopsis pilosula inhibits inducible nitric oxide synthase and protein oxidation in lipopolysaccharide-stimulated raw cells. Tropical Journal of Pharmaceutical Research 12(5) (2013) 705.[17] J.Y.W. Chan, F.C. Lam, P.C. Leung, C.T. Che, K.P. Fung. Antihyperglycemic and antioxidative effects of a herbal formulation of Radix Astragali, Radix Codonopsis and Cortex Lycii in a mouse model of type 2 diabetes mellitus. Phytotherapy Research: An International Journal Devoted to Pharmacological and Toxicological Evaluation of Natural Product Derivatives 23(5) (2009) 658.[18] S. Kumar, S. Narwal, V. Kumar, O. Prakash. α-glucosidase inhibitors from plants: A natural approach to treat diabetes. Pharmacognosy reviews 5(9) (2011) 19.[19] K. Tadera, Y. Minami, K. Takamatsu, T. Matsuoka. Inhibition of α-glucosidase and α-amylase by flavonoids. Journal of nutritional science and vitaminology 52(2) (2006) 149.[20] C.W. Choi, Y.H. Choi, M.-R. Cha, D.S. Yoo, Y.S. Kim, G.H. Yon, et al. Yeast α-glucosidase inhibition by isoflavones from plants of Leguminosae as an in vitro alternative to acarbose. Journal of agricultural and food chemistry 58(18) (2010) 9988.[21] K. He, X. Li, X. Chen, X. Ye, J. Huang, Y. Jin, et al. Evaluation of antidiabetic potential of selected traditional Chinese medicines in STZ-induced diabetic mice. Journal of ethnopharmacology 137(3) (2011) 1135.[22] S.W. Jung, A.J. Han, H.J. Hong, M.G. Choung, K.S. Kim, S.H. Park. alpha-glucosidase inhibitors from the roots of Codonopsis lanceolata Trautv. Agricultural Chemistry and Biotechnology 49(4) (2006) 162.[23] R. Gupta, A.K. Sharma, M. Dobhal, M. Sharma, R. Gupta. Antidiabetic and antioxidant potential of β‐sitosterol in streptozotocin‐induced experimental hyperglycemia. Journal of diabetes 3(1) (2011) 29.[24] R. Khanra, N. Bhattacharjee, T.K. Dua, A. Nandy, A. Saha, J. Kalita, et al. Taraxerol, a pentacyclic triterpenoid, from Abroma augusta leaf attenuates diabetic nephropathy in type 2 diabetic rats. Biomedicine & Pharmacotherapy 94((2017) 726.[25] A.I. Alagbonsi, T.M. Salman, H.M. Salahdeen, A.A. Alada. Effects of adenosine and caffeine on blood glucose levels in rats. Nigerian Journal of Experimental and Clinical Biosciences 4(2) (2016) 35.[26] A.M. Mahmoud, O.E. Hussein. Hesperidin as a promising anti-diabetic flavonoid: the underlying molecular mechanism. Int J Food Nutr Sci| Volume 3(3) (2014) 1.

Download Full-text

Acetylcholinesterase and Butyrylcholinesterase Inhibitory Activities ofβ-Carboline and Quinoline Alkaloids Derivatives from the Plants of GenusPeganum

Journal of Chemistry ◽

10.1155/2013/717232 ◽

2013 ◽

Vol 2013 ◽

pp. 1-6 ◽

Cited By ~ 28

Author(s):

Ting Zhao ◽

Ke-min Ding ◽

Lei Zhang ◽

Xue-mei Cheng ◽

Chang-hong Wang ◽

...

Keyword(s):

Chemical Constituents ◽

Critical Role ◽

Quantitative Structure Activity Relationship ◽

Ache Inhibitor ◽

Design And Synthesis ◽

Quinoline Alkaloids ◽

Potent Inhibition ◽

Inhibitory Activities ◽

Relationship Of

It was reported that the main chemical constituents in plants of genus Peganum were a serial ofβ-carboline and quinoline alkaloids. These alkaloids were quantitatively assessed for selective inhibitory activities on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) byin vitroEllman method. The results indicated that harmane was the most potent selective AChE inhibitor with an IC50of 7.11 ± 2.00 μM and AChE selectivity index (SI, IC50of BChE/IC50of AChE) of 10.82. Vasicine was the most potent BChE inhibitor with feature of dual AChE/BChE inhibitory activity, with an IC50versus AChE/BChE of 13.68 ± 1.25/2.60 ± 1.47 μM and AChE SI of 0.19. By analyzing and comparing the IC50and SI of those chemicals, it was indicated that theβ-carboline alkaloids displayed more potent AChE inhibition but less BChE inhibition than quinoline alkaloids. The substituent at the C7 position of theβ-carboline alkaloids and C3 and C9 positions of quinoline alkaloids played a critical role in AChE or BChE inhibition. The potent inhibition suggested that those alkaloids may be used as candidates for treatment of Alzheimer’s disease. The analysis of the quantitative structure-activity relationship of those compounds investigated might provide guidance for the design and synthesis of AChE and BChE inhibitors.

Download Full-text

Chemical constituents from Sonneratia ovata Backer and their in vitro cytotoxicity and acetylcholinesterase inhibitory activities

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2015.04.017 ◽

2015 ◽

Vol 25 (11) ◽

pp. 2366-2371 ◽

Cited By ~ 8

Author(s):

Thi-Hoai-Thu Nguyen ◽

Huu-Viet-Thong Pham ◽

Nguyen-Kim-Tuyen Pham ◽

Ngo-Diem-Phuong Quach ◽

Khanitha Pudhom ◽

...

Keyword(s):

Chemical Constituents ◽

In Vitro Cytotoxicity ◽

Inhibitory Activities

Download Full-text

Combination of a novel growth hormone releasing hormone Antagonist JMR 132 and Tamoxifen enhances the inhibitory effects on growth of ZR 75 and T47D estrogen dependent human breast cancer cells in vitro and in vivo

Geburtshilfe und Frauenheilkunde ◽

10.1055/s-0029-1225201 ◽

2009 ◽

Vol 69 (05) ◽

Author(s):

S Buchholz ◽

AV Schally ◽

A Krishan ◽

A Papadia ◽

O Ortmann ◽

...

Keyword(s):

Breast Cancer ◽

Growth Hormone ◽

Human Breast Cancer ◽

Breast Cancer Cells ◽

Growth Hormone Releasing Hormone ◽

Human Breast Cancer Cells ◽

Human Breast ◽

Inhibitory Effects

Download Full-text

Melatonin modifies tumor hypoxia and metabolism by inhibiting HIF-1α and energy metabolic pathway in the in vitro and in vivo models of breast cancer

Melatonin Research ◽

10.32794/mr11250042 ◽

2019 ◽

Vol 2 (4) ◽

pp. 83-98 ◽

Cited By ~ 2

Author(s):

André De Lima Mota ◽

Bruna Vitorasso Jardim-Perassi ◽

Tialfi Bergamin De Castro ◽

Jucimara Colombo ◽

Nathália Martins Sonehara ◽

...

Keyword(s):

Breast Cancer ◽

Glucose Metabolism ◽

Tumor Growth ◽

Tumor Cells ◽

Carbonic Anhydrases ◽

In Vivo Models ◽

Ca Ix ◽

Gene And Protein Expression

Breast cancer is the most common cancer among women and has a high mortality rate. Adverse conditions in the tumor microenvironment, such as hypoxia and acidosis, may exert selective pressure on the tumor, selecting subpopulations of tumor cells with advantages for survival in this environment. In this context, therapeutic agents that can modify these conditions, and consequently the intratumoral heterogeneity need to be explored. Melatonin, in addition to its physiological effects, exhibits important anti-tumor actions which may associate with modification of hypoxia and Warburg effect. In this study, we have evaluated the action of melatonin on tumor growth and tumor metabolism by different markers of hypoxia and glucose metabolism (HIF-1α, glucose transporters GLUT1 and GLUT3 and carbonic anhydrases CA-IX and CA-XII) in triple negative breast cancer model. In an in vitro study, gene and protein expressions of these markers were evaluated by quantitative real-time PCR and immunocytochemistry, respectively. The effects of melatonin were also tested in a MDA-MB-231 xenograft animal model. Results showed that melatonin treatment reduced the viability of MDA-MB-231 cells and tumor growth in Balb/c nude mice (p <0.05). The treatment significantly decreased HIF-1α gene and protein expression concomitantly with the expression of GLUT1, GLUT3, CA-IX and CA-XII (p <0.05). These results strongly suggest that melatonin down-regulates HIF-1α expression and regulates glucose metabolism in breast tumor cells, therefore, controlling hypoxia and tumor progression.

Download Full-text

The truncated somatostatin receptor sst5TMD4 stimulates the production of pro-angiogenic factors in in vitro and in vivo breast cancer models

Endocrine Abstracts ◽

10.1530/endoabs.35.p516 ◽

2014 ◽

Author(s):

Raul M Luque ◽

Mario Duran-Prado ◽

David Rincon-Fernandez ◽

Marta Hergueta-Redondo ◽

Michael D Culler ◽

...

Keyword(s):

Breast Cancer ◽

Somatostatin Receptor ◽

Angiogenic Factors ◽

Cancer Models

Download Full-text