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在体、体外和计算机模拟抗癌症活性的羊驼叶：一种在墨西哥可食用和药用的植物。

In Vivo, In Vitro and In Silico Anticancer Activity of Ilama Leaves: An Edible and Medicinal Plant in Mexico.

机构信息

Instituto Politécnico Nacional, Escuela Superior de Medicina, Sección de Estudios de Posgrado e Investigación, Plan de San Luis y Salvador Díaz Mirón S/N, Col. Casco de Santo Tomás, Mexico City 11340, Mexico.

Unidad de Investigación Médica en Farmacología, UMAE Hospital de Especialidades 2° Piso CORSE Centro Médico Nacional Siglo XXI, Instituto Mexicano del Seguro Social, Av. Cuauhtémoc 330, Col. Doctores, Mexico City 06720, Mexico.

出版信息

Molecules. 2024 Apr 24;29(9):1956. doi: 10.3390/molecules29091956.

DOI:10.3390/molecules29091956
PMID:38731446
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11085222/
Abstract

Ilama leaves are an important source of secondary metabolites with promising anticancer properties. Cancer is a disease that affects a great number of people worldwide. This work aimed to investigate the in vivo, in vitro and in silico anticancer properties of three acyclic terpenoids (geranylgeraniol, phytol and farnesyl acetate) isolated from petroleum ether extract of ilama leaves. Their cytotoxic activity against U-937 cells was assessed using flow cytometry to determine the type of cell death and production of reactive oxygen species (ROS). Also, a morphological analysis of the lymph nodes and a molecular docking study using three proteins related with cancer as targets, namely, Bcl-2, Mcl-1 and VEGFR-2, were performed. The flow cytometry and histomorphological analysis revealed that geranylgeraniol, phytol and farnesyl acetate induced the death of U-937 cells by late apoptosis and necrosis. Geranylgeraniol and phytol induced a significant increase in ROS production. The molecular docking studies showed that geranylgeraniol had more affinity for Bcl-2 and VEGFR-2. In the case of farnesyl acetate, it showed the best affinity for Mcl-1. This study provides information that supports the anticancer potential of geranylgeraniol, phytol and farnesyl acetate as compounds for the treatment of cancer, particularly with the potential to treat non-Hodgkin's lymphoma.

摘要

羊驼叶是具有有前景抗癌特性的次生代谢产物的重要来源。癌症是一种影响全球大量人群的疾病。本研究旨在研究从羊驼叶石油醚提取物中分离得到的三种无环萜烯（香叶醇、叶绿醇和法呢基醋酸酯）的体内、体外和计算机辅助抗癌特性。使用流式细胞术评估它们对 U-937 细胞的细胞毒性活性，以确定细胞死亡类型和活性氧 (ROS) 的产生。此外，还对淋巴结进行形态分析，并对三种与癌症相关的蛋白质（Bcl-2、Mcl-1 和 VEGFR-2）作为靶标进行分子对接研究。流式细胞术和组织形态学分析表明，香叶醇、叶绿醇和法呢基醋酸酯通过晚期细胞凋亡和坏死诱导 U-937 细胞死亡。香叶醇和叶绿醇诱导 ROS 产生显著增加。分子对接研究表明，香叶醇对 Bcl-2 和 VEGFR-2 具有更高的亲和力。就法呢基醋酸酯而言，它对 Mcl-1 表现出最好的亲和力。本研究提供了支持香叶醇、叶绿醇和法呢基醋酸酯作为抗癌化合物的抗癌潜力的信息，特别是在治疗非霍奇金淋巴瘤方面。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/a61dd9d375df/molecules-29-01956-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/c84197c1a6e8/molecules-29-01956-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/b62314169c07/molecules-29-01956-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/d39a1daecff3/molecules-29-01956-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/7f4fb987e268/molecules-29-01956-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/d4cc2c9d852f/molecules-29-01956-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/6db6c2897114/molecules-29-01956-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/d74b3d617a44/molecules-29-01956-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/8a2151c10016/molecules-29-01956-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/a61dd9d375df/molecules-29-01956-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/c84197c1a6e8/molecules-29-01956-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/b62314169c07/molecules-29-01956-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/d39a1daecff3/molecules-29-01956-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/7f4fb987e268/molecules-29-01956-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/d4cc2c9d852f/molecules-29-01956-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/6db6c2897114/molecules-29-01956-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/d74b3d617a44/molecules-29-01956-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/8a2151c10016/molecules-29-01956-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/964c/11085222/a61dd9d375df/molecules-29-01956-g009.jpg

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引用本文的文献

[1]
Anti-lymphoma Activity of Acyclic Terpenoids and Its Structure-Activity Relationship: In Vivo, In Vitro, and In Silico Studies.

Int J Mol Sci. 2025-6-13

[2]
Caryophyllene Oxide, a Bicyclic Terpenoid Isolated from with Antitumor Activity: In Vivo, In Vitro, and In Silico Studies.

Int J Mol Sci. 2024-12-12

[3]
Antiprotozoal Activity Against and of Cyclopeptides Isolated from Saff.

Molecules. 2024-11-28

本文引用的文献

[1]
Understanding the Antilymphoma Activity of Donn and Its Acyclic Terpenoids: In Vivo, In Vitro, and In Silico Studies.

Molecules. 2022-10-21

[2]
Therapeutic Potential of Certain Terpenoids as Anticancer Agents: A Scoping Review.

Cancers (Basel). 2022-2-22

[3]
Natural Bioactive Compounds Targeting Epigenetic Pathways in Cancer: A Review on Alkaloids, Terpenoids, Quinones, and Isothiocyanates.

Nutrients. 2021-10-22

[4]
BCL2 and MCL1 inhibitors for hematologic malignancies.

Blood. 2021-9-30

[5]
Terpenoids' anti-cancer effects: focus on autophagy.

Apoptosis. 2021-10

[6]
Ligand-Based Pharmacophore Modeling, Molecular Docking, and Molecular Dynamic Studies of Dual Tyrosine Kinase Inhibitor of EGFR and VEGFR2.

Int J Mol Sci. 2020-10-21

[7]
New biomarkers in non-Hodgkin lymphoma and acute leukemias.

Adv Clin Chem. 2020

[8]
Targeting MCL-1 in hematologic malignancies: Rationale and progress.

Blood Rev. 2020-11

[9]
In vitro and in silico anticancer activity of amygdalin on the SK-BR-3 human breast cancer cell line.

Mol Biol Rep. 2019-10-3

[10]
Synergistic interaction of β-caryophyllene with aromadendrene oxide 2 and phytol induces apoptosis on skin epidermoid cancer cells.

Phytomedicine. 2018-5-9

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