Structural investigation of ginsenoside Rf with PPARγ major transcriptional factor of adipogenesis and its impact on adipocyte

Siraj, Fayeza Md,Natarajan, Sathishkumar,Huq, Md Amdadul,Kim, Yeon Ju,Yang, Deok Chun The Korean Society of Ginseng 2015 Journal of Ginseng Research Vol.39 No.2

Background: Adipocytes, which are the main cellular component of adipose tissue, are the building blocks of obesity. The nuclear hormone receptor $PPAR{\gamma}$ is a major regulator of adipocyte differentiation and development. Obesity, which is one of the most dangerous yet silent diseases of all time, is fast becoming a critical area of research focus. Methods: In this study, we initially aimed to investigate whether the ginsenoside Rf, a compound that is only present in Panax ginseng Meyer, interacts with $PPAR{\gamma}$ by molecular docking simulations. After we performed the docking simulation the result has been analyzed with several different software programs, including Discovery Studio, Pymol, Chimera, Ligplus, and Pose View. All of the programs identified the same mechanism of interaction between $PPAR{\gamma}$ and Rf, at the same active site. To determine the drug-like and biological activities of Rf, we calculate its absorption, distribution, metabolism, excretion, and toxic (ADMET) and prediction of activity spectra for substances (PASS) properties. Considering the results obtained from the computational investigations, the focus was on the in vitro experiments. Results: Because the docking simulations predicted the formation of structural bonds between Rf and $PPAR{\gamma}$, we also investigated whether any evidence for these bonds could be observed at the cellular level. These experiments revealed that Rf treatment of 3T3-L1 adipocytes downregulated the expression levels of $PPAR{\gamma}$ and perilipin, and also decreased the amount of lipid accumulated at different doses. Conclusion: The ginsenoside Rf appears to be promising compound that could prove useful in antiobesity treatments.

Structural investigation of ginsenoside Rf with PPARg major transcriptional factor of adipogenesis and its impact on adipocyte

Fayeza Md Siraj,Sathishkumar Natarajan,Md Amdadul Huq,Yeon Ju Kim,양덕춘 고려인삼학회 2015 Journal of Ginseng Research Vol.39 No.2

Background: Adipocytes, which are the main cellular component of adipose tissue, are the buildingblocks of obesity. The nuclear hormone receptor PPARg is a major regulator of adipocyte differentiationand development. Obesity, which is one of the most dangerous yet silent diseases of all time, is fastbecoming a critical area of research focus. Methods: In this study, we initially aimed to investigate whether the ginsenoside Rf, a compound that isonly present in Panax ginseng Meyer, interacts with PPARg by molecular docking simulations. After weperformed the docking simulation the result has been analyzed with several different software programs,including Discovery Studio, Pymol, Chimera, Ligplus, and Pose View. All of the programs identified thesame mechanism of interaction between PPARg and Rf, at the same active site. To determine the druglikeand biological activities of Rf, we calculate its absorption, distribution, metabolism, excretion, andtoxic (ADMET) and prediction of activity spectra for substances (PASS) properties. Considering the resultsobtained from the computational investigations, the focus was on the in vitro experiments. Results: Because the docking simulations predicted the formation of structural bonds between Rf andPPARg, we also investigated whether any evidence for these bonds could be observed at the cellular level. These experiments revealed that Rf treatment of 3T3-L1 adipocytes downregulated the expression levelsof PPARg and perilipin, and also decreased the amount of lipid accumulated at different doses. Conclusion: The ginsenoside Rf appears to be promising compound that could prove useful in antiobesitytreatments

Ginsenoside F2 possesses anti-obesity activity via binding with PPARγ and inhibiting adipocyte differentiation in the 3T3-L1 cell line

Siraj, Fayeza Md.,SathishKumar, Natarajan,Kim, Yeon Ju,Kim, Se Young,Yang, Deok Chun Informa UK Ltd. 2015 Journal of enzyme inhibition and medicinal chemist Vol.30 No.1

<P><I>Panax ginseng</I> Meyer has been shown to be effective in mitigating various diseases. Protopanaxadiols (PPD) and protopanaxatriols (PPT), which are the main constituents of ginseng, have been shown to impact obesity. Therefore, we selected several important ginsenosides to perform our docking study and determine if they had binding affinity with the peroxisome proliferator activated receptor gamma (PPARγ), which is a major transcription factor in adipocytes. Among them, only a few ginsenosides demonstrated binding affinity with PPARγ. Other than ginsenoside F2 rest of them were previously reported by the researchers in experimental study in case of obesity cell line 3T3-L1 adipocyte. In few recent studies, it was reported that F2 has protective effects on malignant brain tumors as well as anti-cancer activity in breast cancer. Therefore, we felt it was important to focus on F2 when considering obesity. Our study focused on this ginsenoside and analyzed its impact on 3T3-L1 adipocytes. Following the molecular interaction studies, further experimental studies were carried out and demonstrated that ginsenoside F2 when treated with different doses reduces the level of lipid accumulated by the 3T3-L1 cell line during adipogenesis. Reverse transcriptase polymerase chain reaction (RT-PCR) and quantitative real-time PCR results showed reduction in PPARγ and perilipin gene expression levels compared to that of differentiated adipocytes without any treatment. So considering the binding with a major adipocyte transcription factor and the performed experiments, we suggest that ginsenoside F2 may reduce obesity via the inhibition of adipogenesis in the 3T3-L1 cell line.</P>

Structural investigation of ginsenoside Rf with PPARγ major transcriptional factor of adipogenesis and its impact on adipocyte

Fayeza Md Siraj,Sathishkumar Natarajan,Md Amdadul Huq,Yeon Ju Kim,Deok Chun Yang 고려인삼학회 2015 Journal of Ginseng Research Vol.39 No.2

Background: Adipocytes, which are the main cellular component of adipose tissue, are the building blocks of obesity. The nuclear hormone receptor PPARγ is a major regulator of adipocyte differentiation and development. Obesity, which is one of the most dangerous yet silent diseases of all time, is fast becoming a critical area of research focus. Methods: In this study, we initially aimed to investigate whether the ginsenoside Rf, a compound that is only present in Panax ginseng Meyer, interacts with PPARγ by molecular docking simulations. After we performed the docking simulation the result has been analyzed with several different software programs, including Discovery Studio, Pymol, Chimera, Ligplus, and Pose View. All of the programs identified the same mechanism of interaction between PPARγ and Rf, at the same active site. To determine the druglike and biological activities of Rf, we calculate its absorption, distribution, metabolism, excretion, and toxic (ADMET) and prediction of activity spectra for substances (PASS) properties. Considering the results obtained from the computational investigations, the focus was on the in vitro experiments. Results: Because the docking simulations predicted the formation of structural bonds between Rf and PPARγ, we also investigated whether any evidence for these bonds could be observed at the cellular level. These experiments revealed that Rf treatment of 3T3-L1 adipocytes downregulated the expression levels of PPARγ and perilipin, and also decreased the amount of lipid accumulated at different doses. Conclusion: The ginsenoside Rf appears to be promising compound that could prove useful in antiobesity treatments.

Ginseng and Obesity: Observations from Assorted Perspectives

Fayeza Md. Siraj,김연주,Sathishkumar Natarajan,정석규,양동욱,양덕춘 한국식품과학회 2014 Food Science and Biotechnology Vol.23 No.4

Ginseng is a well known herb used for variouspurposes that possesses many beneficial effects for thehuman body and aids in recovery or cure for severaldiseases. There has been much research and many clinicaltrials designed to ascertain what these beneficial effectsare. Studies have investigated ginseng effects on diabetes,osteoporosis, the immune system, and many other diseases. Research has also shown ginseng to be effective as anantiobesity treatment. Ginsenoside components inhibitdifferentiation inducers in adipocyte tissues. This reviewsummarizes the in vivo and in vitro effects of variousginseng crude extracts/ginsenosides on obesity via activationof AMPK- and/or cAMP-dependent pathways, which arenetworks of transcription factors through which PPARγand cofactors operate. Additional proteins, markers, andpathways are suggested for which the effects of ginsengsaponins may be promising.