Cytotoxicity Evaluation of Turmeric Extract Incorporated Oil-in-Water Nanoemulsion

Yoon, Hee Jeong; Zhang, Xiaowei; Kang, Min Gyeong; Kim, Gyeong Jin; Shin, Sun Young; Baek, Sang Hong; Lee, Bom Nae; Hong, Su Jung; Kim, Jun Tae; Hong, Kwonho; Bae, Hojae

doi:10.3390/ijms19010280

Cited by 31 publications

(16 citation statements)

References 51 publications

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“…Similarly, the toxicity of curcuminoid preparation was also tested for HEK-293 cells, and no significant toxicity was observed below 6.25 µg/mL or higher concentrations. These results are in agreement with the previously reported toxicity values for curcumin in NIH3T3, H9C2, and HepG2 cells [51]. Human trials using up to 8000 mg of curcumin found no evidence of toxicity [52].…”

Section: Resultssupporting

confidence: 92%

Bioactivity of Curcumin on the Cytochrome P450 Enzymes of the Steroidogenic Pathway

Castaño

Parween

Pandey

2019

IJMS

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Turmeric, a popular ingredient in the cuisine of many Asian countries, comes from the roots of the Curcuma longa and is known for its use in Chinese and Ayurvedic medicine. Turmeric is rich in curcuminoids, including curcumin, demethoxycurcumin, and bisdemethoxycurcumin. Curcuminoids have potent wound healing, anti-inflammatory, and anti-carcinogenic activities. While curcuminoids have been studied for many years, not much is known about their effects on steroid metabolism. Since many anti-cancer drugs target enzymes from the steroidogenic pathway, we tested the effect of curcuminoids on cytochrome P450 CYP17A1, CYP21A2, and CYP19A1 enzyme activities. When using 10 µg/mL of curcuminoids, both the 17α-hydroxylase as well as 17,20 lyase activities of CYP17A1 were reduced significantly. On the other hand, only a mild reduction in CYP21A2 activity was observed. Furthermore, CYP19A1 activity was also reduced up to ~20% of control when using 1–100 µg/mL of curcuminoids in a dose-dependent manner. Molecular docking studies confirmed that curcumin could dock onto the active sites of CYP17A1, CYP19A1, as well as CYP21A2. In CYP17A1 and CYP19A1, curcumin docked within 2.5 Å of central heme while in CYP21A2 the distance from heme was 3.4 Å, which is still in the same range or lower than distances of bound steroid substrates. These studies suggest that curcuminoids may cause inhibition of steroid metabolism, especially at higher dosages. Also, the recent popularity of turmeric powder as a dilatory supplement needs further evaluation for the effect of curcuminoids on steroid metabolism. The molecular structure of curcuminoids could be modified to generate better lead compounds with inhibitory effects on CYP17A1 and CYP19A1 for potential drugs against prostate cancer and breast cancer.

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Section: Resultssupporting

confidence: 92%

Bioactivity of Curcumin on the Cytochrome P450 Enzymes of the Steroidogenic Pathway

Castaño

Parween

Pandey

2019

IJMS

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show abstract

“…Similarly, the toxicity of curcuminoid preparation was also tested for HEK-293 cells, and no significant toxicity was observed below 6.25 µg/ml or higher concentrations ( Supplementary Figure 1). These results are in agreement with the previously reported toxicity values for curcumin in NIH3T3, H9C2, and HepG2 cells [30]. Human trials using up to 8000 mg of curcumin found no evidence of toxicity [31].…”

Section: Toxicity Of Curcuminoids On Nci-h295r Cellssupporting

confidence: 92%

Bioactivity of curcumin on the cytochrome P450 enzymes of the steroidogenic pathway

Castaño

Parween

Pandey

2019

Preprint

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Turmeric, a popular ingredient in the cuisine of many Asian countries, comes from the roots of the Curcuma longa and is known for its use in Chinese and Ayurvedic medicine. Turmeric is rich in curcuminoids, including curcumin, demethoxycurcumin, and bisdemethoxycurcumin. Curcuminoids have potent wound healing, anti-inflammatory, and anti-carcinogenic activities. While curcuminoids have been studied for many years, not much is known about their effects on steroid metabolism. Since many anti-cancer drugs target enzymes from the steroidogenic pathway, we tested the effect of curcuminoids on cytochrome P450 CYP17A1, CYP21A2, and CYP19A1 enzyme activities. When using 10 µg/ml of curcuminoids, both the 17α-hydroxylase as well as 17,20 lyase activities of CYP17A1 were reduced significantly. On the other hand, only a mild reduction in CYP21A2 activity was observed. Furthermore, CYP19A1 activity was also reduced up to ~20% of control when using 1-100 µg/ml of curcuminoids in a dose-dependent manner. Molecular docking studies confirmed that curcumin could dock into the active sites of CYP17A1, CYP19A1 as well as CYP21A2. In CYP17A1 and CYP19A1, curcumin docked within 2.5 Å of central heme while in CYP21A2 the distance from heme was 3.4 Å, which is still in the same range or lower than distances of bound steroid substrates. These studies suggest that curcuminoids may cause inhibition of steroid metabolism, especially at higher dosages. Also, the recent popularity of turmeric powder as a dilatory supplement needs further evaluation for the effect of curcuminoids on steroid metabolism. Molecular structure of curcuminoids could be modified to generate better lead compounds with inhibitory effects on CYP17A1 and CYP19A1 for potential drugs against prostate cancer and breast cancer.

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“…Moreover, formulations of curcumin with NEs significantly reduced its cytotoxicity in cells, probably because NEs decreased access of the drug to cells. [209] Vater et al compared the cytotoxicity of lecithin-based NEs with NEs based on conventional surfactants on human skin cells (primary human keratinocytens as well as fibroblasts). In addition, they evaluated the effect of the nanodroplet size in the range from 124 to 245 nm.…”

Section: Cytotoxicitymentioning

confidence: 99%

Dye‐Loaded Nanoemulsions: Biomimetic Fluorescent Nanocarriers for Bioimaging and Nanomedicine

Klymchenko

Liu

Collot

et al. 2020

Adv Healthcare Materials

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Lipid nanoemulsions (NEs), owing to their controllable size (20 to 500 nm), stability and biocompatibility, are now frequently used in various fields, such as food, cosmetics, pharmaceuticals, drug delivery, and even as nanoreactors for chemical synthesis. Moreover, being composed of components generally recognized as safe (GRAS), they can be considered as “green” nanoparticles that mimic closely lipoproteins and intracellular lipid droplets. Therefore, they attracted attention as carriers of drugs and fluorescent dyes for both bioimaging and studying the fate of nanoemulsions in cells and small animals. In this review, the composition of dye‐loaded NEs, methods for their preparation, and emerging biological applications are described. The design of bright fluorescent NEs with high dye loading and minimal aggregation‐caused quenching (ACQ) is focused on. Common issues including dye leakage and NEs stability are discussed, highlighting advanced techniques for their characterization, such as Förster resonance energy transfer (FRET) and fluorescence correlation spectroscopy (FCS). Attempts to functionalize NEs surface are also discussed. Thereafter, biological applications for bioimaging and single‐particle tracking in cells and small animals as well as biomedical applications for photodynamic therapy are described. Finally, challenges and future perspectives of fluorescent NEs are discussed.

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Cytotoxicity Evaluation of Turmeric Extract Incorporated Oil-in-Water Nanoemulsion

Cited by 31 publications

References 51 publications

Bioactivity of Curcumin on the Cytochrome P450 Enzymes of the Steroidogenic Pathway

Bioactivity of Curcumin on the Cytochrome P450 Enzymes of the Steroidogenic Pathway

Bioactivity of curcumin on the cytochrome P450 enzymes of the steroidogenic pathway

Dye‐Loaded Nanoemulsions: Biomimetic Fluorescent Nanocarriers for Bioimaging and Nanomedicine

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