Future of nano bisdemethoxy curcumin analog: Guaranteeing safer intravenous delivery

Francis, Arul Prakash; Ganapathy, Selvam; Palla, Venkata Rajsekhar; Murthy, P. Balakrishna; Thiyagarajan, Devasena

doi:10.1016/j.etap.2014.12.018

Cited by 8 publications

(3 citation statements)

References 16 publications

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“…The results clearly showed that RFA had no obvious cytotoxicity to PBMC, and may promote proliferation within a certain concentration range. Hemolysis was regarded as the red blood cell toxicity index, the red blood cell hemolysis test of RFA showed that the percentage of hemolysis was less than 2.5%, which met the recognized requirement that the hemolysis rate should not exceed 5% (Guo et al, 2013;Francis et al, 2015). Therefore, we preliminarily believe that RFA is non-toxic and safe.…”

Section: Discussionmentioning

confidence: 81%

“…Completely lysed blood is obtained by adding deionized water to a 2% RBC solution. Deionized water was used as a positive control and PBS was used as a negative control (Guo et al, 2013;Francis et al, 2015). The percentage of hemolysis is calculated by the following formula: Hemolysis (%) =(Sample OD-Negative control OD)/(Positive control OD-Negative control OD)×100%.…”

Section: Hemolytic Assaymentioning

confidence: 99%

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A novel biflavone from Reineckia carnea induces apoptosis of human renal cancer 786-O cells

Yang

Xiao

et al. 2022

Front. Pharmacol.

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Renal cell carcinoma (RCC) is a common malignant tumor of the urinary system, which is highly invasive, metastatic, and insensitive to radiotherapy and chemotherapy. Chinese herbal medicine has always been an important source of anti-tumor drug development. Reineckia carnea Kunth is a traditional herb commonly used by the Miao nationality in southwest China. In this study, the extract of Reineckia carnea was isolated and purified by reverse phase preparative chromatography and other chromatographic techniques. According to the physicochemical properties and spectral data, the structure of the compound was identified, and a novel biflavone compound named Reineckia-biflavone A (RFA) was obtained. The result of antiproliferative activity showed that RFA had cytotoxicity on 786-O cells with an IC50 value of 19.34 μmol/L. The results of CCK-8 and hemolysis assays showed that RFA was not significantly cytotoxic to both red blood cells (RBC) and peripheral blood mononuclear cells (PBMC). By Hoechst 33258 apoptosis staining, typical apoptotic morphology was observed under fluorescence microscope. RFA could induce the apoptosis of 786-O cells with the increase of apoptosis rate. The cell cycle tests showed that the cell proportion was obviously arrested in the S phase. At the same time, RFA could decrease the mitochondrial membrane potential and increase the intracellular free Ca2+ concentration. Western blot showed that the expression levels of pro-apoptotic proteins (Bax, Caspase-3, Cleaved Caspase-3, and Cytochrome c) in cells rose, while the expression level of anti-apoptotic proteins (Bcl-2) declined significantly. In conclusion, this study suggests that the RFA is a new biflavone determined by SciFinder retrieval. The apoptosis may be triggered by RFA through the mitochondrial pathway, which is mediated by up-regulating the intracellular calcium ion, down-regulating the mitochondrial membrane potential, and changing the apoptosis-related proteins.

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Section: Discussionmentioning

confidence: 81%

Section: Hemolytic Assaymentioning

confidence: 99%

A novel biflavone from Reineckia carnea induces apoptosis of human renal cancer 786-O cells

Yang

Xiao

et al. 2022

Front. Pharmacol.

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“…A more recent approach to improve bioavailability of curcumin has been to use nano formulations of curcumin [23,24,25]. Several different nanocurcumin preparations have been made and tested for in vitro as well as in vivo effects and toxicities [26,27,28]. The nano particle formulations of curcumin have been shown to improve bioavailability and therapeutic potential of curcumin and its analogues and can be considered a medium of choice for delivery of curcuminoids [29,30,31,32,33].…”

Section: Introductionmentioning

confidence: 99%

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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Toxicity of Graphene: An Update

Devasena

Francis

Ramaprabhu

2021

Reviews of Environmental Contamination and Toxicology

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Future of nano bisdemethoxy curcumin analog: Guaranteeing safer intravenous delivery

Cited by 8 publications

References 16 publications

A novel biflavone from Reineckia carnea induces apoptosis of human renal cancer 786-O cells

A novel biflavone from Reineckia carnea induces apoptosis of human renal cancer 786-O cells

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

Toxicity of Graphene: An Update

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