Anti-atherosclerosis potency of<i>Pandanus tectorius</i>fruit rich by trangeretin and ethyl trans-caffeate, and their cytotoxicity against HepG2 cell line

Andriani, Yosie; Pangestika, Inten; Oksal, Efriyana; Mohamad, Habsah; Amir, Hermansyah; Muhammad, Tengku Sifzizul Tengku; Wahid, M.

doi:10.1088/1757-899x/509/1/012155

Cited by 3 publications

(1 citation statement)

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“…The fruit consists of fifteen secondary metabolite compounds, ten phenolics and five semipolar, such as vanillin, trans -ethyl caffeate, tangeretin, chrysin, naringenin ( Zhang et al, 2013b ), and caffeoylquinic acid ( Zhang et al, 2013a ). The fruit and its compounds have been reported to have potential as anti-hypercholesterolemia agent ( Andriani et al, 2019 , Pangestika et al, 2020 ). However, the semipolar properties of P. tectorius extract cause it to exhibit poor solubility if it is used as a medical remedy.…”

Section: Introductionmentioning

confidence: 99%

In vitro and in vivo studies of nanoparticles of chitosan-Pandanus tectorius fruit extract as new alternative treatment for hypercholesterolemia via Scavenger Receptor Class B type 1 pathway

Oksal

Pangestika

Muhammad

et al. 2020

Saudi Pharmaceutical Journal

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Pandanus tectorius fruit, a natural product rich in tangeretin and ethyl caffeate, has been reported to have potential as anti-hypercholesterolemia agent via Scavenger Receptor Class B type 1 (SR-B1) pathway. However, due to its semi-polar properties, P. tectorius extract exhibits poor solubility when used as a medical remedy. The extract’s solubility can potentially be improved through a synthesis of nanoparticles of chitosan- P. tectorius fruit extract. This can also increase the extract’s SR-B1 gene expression activity. To date, no studies of nanoparticles of chitosan- P. tectorius fruit extract and its pathway via SR-B1 have been published anywhere. In this study, cytotoxicity properties against HepG2 were explored by MTT. Then luciferase assay was used to detect their effectiveness in increasing SR-B1 activity. An in vivo study using Sprague dawley was carried out to observe the extract nanoparticles’ effectiveness in reducing the cholesterol levels and the toxicity property in rat’s liver. As the results showed, the extract nanoparticles had no cytotoxic activity against HepG2 cells and exhibited higher SR-B1 gene expression activity than the non-nanoparticle form. As the in vivo study proved, nanoparticle treatment can reduce the levels of TC (197%), LDL (360%), and TG (109%), as well as increase the level of HDL cholesterol by 150%, in comparison to those for the untreated high-cholesterol diet group. From the toxicity study, it was found that there was non-toxicity in the liver. It can be concluded that nanoparticles of chitosan- P. tectorius fruit extract successfully increased P. tectorius fruit extract’s effectiveness in reducing hypercholesterolemia via SR-B1 pathway. Hence, it can be suggested that nanoparticles of chitosan- P. tectorius fruit extract is safe and suitable as an alternative treatment for controlling hypercholesterolemia via SR-B1 pathway.

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Section: Introductionmentioning

confidence: 99%

In vitro and in vivo studies of nanoparticles of chitosan-Pandanus tectorius fruit extract as new alternative treatment for hypercholesterolemia via Scavenger Receptor Class B type 1 pathway

Oksal

Pangestika

Muhammad

et al. 2020

Saudi Pharmaceutical Journal

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Inhibitory effects of tangeretin and trans-ethyl caffeate on the HMG-CoA reductase activity: Potential agents for reducing cholesterol levels

Pangestika

Oksal

Muhammad

et al. 2020

Saudi Journal of Biological Sciences

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One of the pathways to reduce cholesterol production in the liver is through the inhibition of HMG-Coa reductase (HMGCR) by current drugs, statins. However, these have side effects if consumed in prolonged periods. Tangeretin and trans-ethyl caffeate as alternative drugs in reducing hypercholesterolemia and preventing atherosclerosis have never been reported. Their effects on inhibiting HMGCR activity were investigated through enzymatic method ( in vitro and in vivo ). The toxicity property was analyzed on the Serum Glutamate Oxalate Transaminase (SGOT)/Serum Glutamate Piruvate Transaminase (SGPT) levels and rat liver histology. The results showed that both compounds inhibited HMGCR activity significantly compare to the control simvastatin ( p < 0.05). Tangeretin which showed very good activity in inhibiting HMGCR (83.8 of % inhibition, equal to simvastatin) was selected and used for anti-hypercholesterolemia in vivo assessment. Furthermore, tangeretin was shown to effectively reduced Total Cholesterol (TC) and Low Density Lipoprotein (LDL), and increased High Density Lipoprotein (HDL) levels significantly compared to the simvastatin group ( p < 0.05). Tangeretin group was also proven to inhibit HMGCR rat liver activity significantly compare to the control simvastatin ( p < 0.05). The toxicity study on the SGOT/SGPT levels and liver histology revealed that there were no side effects after administration by tangeretin. Results found that both tangeretin and trans-ethyl caffeate are potent candidates as anti-hypercholesterolemia agent in vitro . In addition, tangeretin was also shown to be safe and suitable as an alternative treatment for controlling hypercholesterolemia in vivo as well as have potency for preventing atherosclerosis.

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Aaptamine Counteracts Statin-Induced PCSK9 Elevation to Improve LDL Receptor Expression and Cholesterol Uptake

Matin,

Chaudhry,

Sung

et al. 2024

Preprint

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Atherosclerosis arises from lipid accumulation and plaque formation, primarily driven by elevated levels of LDL-cholesterol (LDL-C). PCSK9 plays a critical role by degrading LDL receptors (LDL-R), which are responsible for the clearance of LDL-C from the bloodstream. Consequently, inhibiting PCSK9 represents a promising strategy to enhance LDL-R expression and promote LDL-C uptake. Statins are commonly used to treat high cholesterol by decreasing the production of cholesterol. However, they also raise PCSK9 levels, which may explain why some patients don't respond as well as they should to statins. Aaptamines, marine alkaloids with notable structural diversity and bioactivity, are known to regulate gene transcription. This study aimed to evaluate the effects of aaptamine in mitigating the statin-induced increase in PCSK9 expression, LDL-R levels, and LDL-C uptake. Cytotoxicity was assessed using the MTS assay for simvastatin, aaptamine, and their combination. PCSK9 mRNA levels were quantified by real-time PCR, while protein expression was analyzed via western blotting. Immunohistochemistry was employed to assess LDL-R levels and LDL-C uptake in liver cells. The results demonstrated that simvastatin significantly upregulated PCSK9 gene expression. However, co-treatment with aaptamine reduced PCSK9 expression by 94–61%. Additionally, aaptamine enhanced LDL-R protein levels and LDL-C uptake by 3.21-fold in cells co-treated with simvastatin. These results suggest that aaptamine lowers the rise in PCSK9 caused by statins and raises the expression of LDL-R, which helps liver cells get rid of LDL-C.

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Anti-atherosclerosis potency ofPandanus tectoriusfruit rich by trangeretin and ethyl trans-caffeate, and their cytotoxicity against HepG2 cell line

Cited by 3 publications

References 18 publications

In vitro and in vivo studies of nanoparticles of chitosan-Pandanus tectorius fruit extract as new alternative treatment for hypercholesterolemia via Scavenger Receptor Class B type 1 pathway

In vitro and in vivo studies of nanoparticles of chitosan-Pandanus tectorius fruit extract as new alternative treatment for hypercholesterolemia via Scavenger Receptor Class B type 1 pathway

Inhibitory effects of tangeretin and trans-ethyl caffeate on the HMG-CoA reductase activity: Potential agents for reducing cholesterol levels

Aaptamine Counteracts Statin-Induced PCSK9 Elevation to Improve LDL Receptor Expression and Cholesterol Uptake

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