Cytotoxic effect of avocado (Persea americana) seed extract containing quercetin in T47D cells by inducing apoptotic pathway in vitro and in silico

Molecules ◽  
2021 ◽  
Vol 26 (9) ◽  
pp. 2780
Author(s):  
Ozvaldo Linares-Anaya ◽  
Alcives Avila-Sorrosa ◽  
Francisco Díaz-Cedillo ◽  
Luis Ángel Gil-Ruiz ◽  
José Correa-Basurto ◽  
...  

A series of benzo [d] [1,3] azoles 2-substituted with benzyl- and allyl-sulfanyl groups were synthesized, and their cytotoxic activities were in vitro evaluated against a panel of six human cancer cell lines. The results showed that compounds BTA-1 and BMZ-2 have the best inhibitory effects, compound BMZ-2 being comparable in some cases with the reference drug tamoxifen and exhibiting a low cytotoxic effect against healthy cells. In silico molecular coupling studies at the tamoxifen binding site of ERα and GPER receptors revealed affinity and the possible mode of interaction of both compounds BTA-1 and BMZ-2.


Author(s):  
Ganiyu Oboh ◽  
Veronica O. Odubanjo ◽  
Fatai Bello ◽  
Ayokunle O. Ademosun ◽  
Sunday I. Oyeleye ◽  
...  

AbstractAvocado pear (The inhibitory effects of extracts on AChE and BChE activities and antioxidant potentials (inhibition of FeThe extracts inhibited AChE and BChE activities and prooxidant-induced TBARS production in a dose-dependent manner, with the seed extract having the highest inhibitory effect and the leaf extract exhibiting higher phenolic content and radical scavenging abilities, but lower Fe chelation ability compared with that of the seed. The phytochemical screening revealed the presence of saponins, alkaloids, and terpenoids in both extracts, whereas the total alkaloid profile was higher in the seed extract than in the leaf extract, as revealed by GC-FID.The anti-cholinesterase and antioxidant activities of avocado leaf and seed could be linked to their phytoconstituents and might be the possible mechanisms underlying their use as a cheap and natural treatment/management of AD. However, these extracts should be further investigated in vivo.


Author(s):  
Rochmah Kurnijasanti ◽  
Amaq Fadholly

Capsicum annum L. is a potential natural plant that have a lot of various pharmacological effects, including as anticancer agent. This study Aim to analyze Capsicum annum extract (CAE) on T47D cells. CAE (10, 20, 40, 60, 80µg/mL) treated on T47D cells to determined IC50 value by MTT assay. Apoptosis induction is also investigated through caspase-3 expressions (IC50, 2IC50). The present study showed that CAE suppress T47D cells proliferation with IC50 value of 75.81µg/mL. The caspase-3 expression on 2IC50 is higher (67.16%) than IC50 (52.16%). This result indicate that CAE has ability as anticancer agent by inhibiting cell growth and induce apoptosis through caspase-3 expression on T47D cells. Further study of CAE holds potential for novel therapies of cancer prevention and treatment.


2021 ◽  
Author(s):  
Jaykaran Charan ◽  
Priyanka Riyad ◽  
Heera Ram ◽  
Ashok Purohit ◽  
Sneha Ambwani ◽  
...  

Abstract Background: The HMG-CoA inhibitor are used to control adverse cardiovascular event caused by Hypercholesterolemia and dyslipidaemia. The current study was aimed to evaluate the ability of phytoconstituents of an aqueous seed extract of Acacia senegal (L.) Willd to inhibit HMG-CoA reductase and regress the formation of atherosclerotic plaque. Methods: The chemical fingerprinting of the test extract was assessed by LC-MS. Consequently, the assessments of in-vitro, in-vivo, and in-silico were performed by following the standard methods.Results: The in-vitro assessment of the test extract revealed 74.1 % inhibition potential of HMG-CoA reductase. In-vivo evaluations of the test extract indicated that treated hypercholesterolemic rabbits exhibited a significant (𝑃 ≤ 0.001) ameliorations in the biomarker indices of the dyslipidaemia, such as the atherogenic index, Castelli risk index (I&II), atherogenic coefficient along with lipid profile. Concomitantly, significant reductions were observed in the atherosclerotic plaque area and antioxidants. The in-silico study of molecular docking shown interactions capabilities of key phytoconstituents of the test extract with target protein of HMG-CoA reductase which further validated by the molecular dynamics through potentail energy, NPT, NVT, RSMD and others. Subsequently, the ADMET analysis shown ideal druggability. Conclusion: The results indicate that phytoconstituents of an aqueous seed extract of Acacia senegal (L.) Willd. could inhibit HMG-CoA reductase and improve the levels of antioxidants activity that may reduce symptoms associated with hypercholesterolemia.


Author(s):  
Isabella Reis ◽  
Eric Umehara ◽  
Rodrigo Conceição ◽  
Larissa Oliveira ◽  
Manoelito Junior ◽  
...  

Author(s):  
Dang Kim Thu ◽  
Hoang Thu Thuy ◽  
Bui Thi Thanh Duyen ◽  
Luc Thi Thanh Hang ◽  
Nguyen Thi Trang ◽  
...  

Medicinal plants are a potential source of enzyme acetylcholinesrerase (AChE) inhibitors, a key target in the treatment of Alzheimer’s disease. This paper studies the AChE inhibitory activity and the antioxidant effect of Persea Americana Mill extract. The sample leave, seed, exocarp and mesocarp of avocado were extracted with 50% ethanol and subsequently fractionated with n-hexane, ethyl acetate (EtOA) and n-butanol (n-BuOH) solvents. The AChE inhibitory activity was evaluated by Ellman’s colorimetric method and the antioxidant activity by screening DPPH free radicals.  The results show that the seed of Persea Americana extract had the strongest AChE inhibitory activity and antioxidant effect, followed by the leave extract, and the exocarp extract and mesocarp extract were the weakest. The Persea Americana seed extract inhibited AChE activity in a dose-dependent manner with an IC50 value of 47.43 ± 0.5 μg/mL and the antioxidant effect with an IC50 value of 68.7 ± 0.35 µg/mL. The results also show that n–BuOH fraction of Persea Americana seed extract had strong AChE inhibitory and antioxidant activities with an IC50 value of 15.24 ± 0.52 µg/ml and 15.73 ± 0.42 μg/mL, respectively. The study results suggest that the Persea Americana Mill is a promising ingredient in Alzheimer’s disease prevention and treatment. Keywords Persea Americana Mill, Acetylcholinesrerase inhibitors (AChE), Alzheimer, DPPH. References [1] M.M. Essa et al., Neuroprotective effect of natural products against Alzheimer's disease, Neurochem Res. 37(9) (2012) 1829.[2] B. McGleenon, K. Dynan, A. Passmore,. Acetylcholinesterase inhibitors in Alzheimer's disease, British journal of clinical pharmacology. 48 (1999) 471.[3] P. B. Watkins et al, Hepatotoxic effects of tacrine administration in patients with Alzheimer's disease, In: Jama. pp. 992 (1994).[4] O. Adeyemi, S. Okpo, O. Ogunti,. Analgesic and anti-inflammatory effects of the aqueous extract of leaves of Persea americana Mill (Lauraceae). In: Fitoterapia. pp. 375 (2002).[5] P.D.D. Dzeufiet, et al, Antihypertensive potential of the aqueous extract which combine leaf of Persea americana Mill. (Lauraceae), stems and leaf of Cymbopogon citratus (DC) Stapf.(Poaceae), fruits of Citrus medical L.(Rutaceae) as well as honey in ethanol and sucrose experimental model. In: BMC complementary and alternative medicine. p. 507 (2014).[6] B.I. Brai, A. Odetola, P. Agomo,. Hypoglycemic and hypocholesterolemic potential of Persea americana leaf extracts, Journal of medicinal food. 10(2) (2007) 356.[7] Phạm Khuê. Bệnh Alzheimer. Nhà xuất bản Y học (2002).[8] Đàm Trung Bảo. Các gốc tự do, Tạp chí Dược học. 6 (2001) 29 [9] F.R. Mowsumi, A. Rahaman, N.C. Sarker, B.K. Choudhury, S. Hossain, In vitro relative free radical scavenging effects of Calocybe indica (milky oyster) and Pleurotus djamor (pink oyster), World J Pharm Pharm Sci. 4(07) (2015) 186.[10] Y. Bao, Y. Qu, J. Li, Y. Li, X. Ren, K. Maffuci, et al. In vitro and in vivo antioxidant activities of the flowers and leaves from Paeonia rockii and identification of their antioxidant constituents by UHPLC-ESI-HRMSn via pre-column DPPH reaction, Molecules. 23(2) (2018) 392.[11] Phan Kế Sơn. Đánh giá tác dụng ức chế enzym Acetylcholinsterase in vitro của các phân đoạn dịch chiết Hoàng Liên Ô rô (Mahonia Nepalensis DC., họ Berberidaceae). Khóa luận tốt nghiệp Đại học ngành Dược học. Khoa Y Dược - Đại học Quốc Gia Hà Nội (2017).[12] D. Mohammad, P. Chan, J. Bradley, K. Lanctôt, N. Herrmann, Acetylcholinesterase inhibitors for treating dementia symptoms-a safety evaluation, Expert opinion on drug safety. 16(9) (2017) 1009.[13] A. Mohammadi-Farani, S.S. Darbandi, A. Aliabadi, Synthesis and acetylcholinesterase inhibitory evaluation of 4-(1, 3-dioxoisoindolin-2-yl)-N-phenyl benzamide derivatives as potential anti-alzheimer agents, Iranian journal of pharmaceutical research. IJPR 15(3) (2016) 313.[14] T.B. Fernandes, M.R. Cunha, R.P. Sakata, T.M. Candido, A.R. Baby, M.T. Tavares, et al. Synthesis, Molecular Modeling, and Evaluation of Novel Sulfonylhydrazones as Acetylcholinesterase Inhibitors for Alzheimer's Disease, Archiv der Pharmazie. 350(11) (2017) 1700163.[15] M.I. Alkhalf, W.S. Alansari, E.A. Ibrahim, M.E. Elhalwagy, Anti-oxidant, anti-inflammatory and anti-cancer activities of avocado (Persea americana) fruit and seed extract. Journal of King Saud University-Science (2018).[16] F. Gómez, S. Sánchez, M. Iradi, N. Azman, M. Almajano, Avocado seeds: extraction optimization and possible use as antioxidant in food, Antioxidants. 3(2) (2014) 439.[17] O.A. Folasade, R.A. Olaide, T.A. Olufemi, Antioxidant properties of Persea americana M. seed as affected by different extraction solvent, Journal of Advances in Food Science & Technology. 3(2) (2016) 101.[18] C.A. Alagbaoso, I.I. Tokunbo, O.S. Osakwe, Comparative study of antioxidant activity and mineral composition of methanol extract of seeds of ripe and unripe avocado pear (Persea americana, Mill.). NISEB Journal. 15(4) (2017).[19] G. Oboh, V.O. Odubanjo, F. Bello, A.O. Ademosun, S.I. Oyeleye, E.E. Nwanna et al. Aqueous extracts of avocado pear (Persea americana Mill.) leaves and seeds exhibit anti-cholinesterases and antioxidant activities in vitro, Journal of basic and clinical physiology and pharmacology. 27(2) (2016) 131.[20] H. Cavdar, M. Senturk, M. Guney , S. Durdagi, G. Kayik, C.T. Supuran, et al. Inhibition of acetylcholinesterase and butyrylcholinesterase with uracil derivatives: kinetic and computational studies, Journal of enzyme inhibition and medicinal chemistry. 34(1) (2019) 429.    


Author(s):  
B Figer ◽  
R Pissurlenkar ◽  
Premlata Ambre ◽  
Samidha Kalekar ◽  
Renuka Munshi ◽  
...  

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