ABSTRACT
Kidney cancer has emerged as a major medical problem in recent times. Multiple compounds are used to treat kidney cancer by triggering cancer-causing gene targets. For instance, isoquercitrin (quercetin-3-O-ß-d-glucopyranoside) is frequently present in fruits, vegetables, medicinal herbs, and foods and drinks made from plants. Our previous study predicted using protein-protein interaction (PPI) and molecular docking analysis that the isoquercitrin compound can control kidney cancer and inflammation by triggering potential gene targets of IGF1R, PIK3CA, IL6, and PTGS2. So, the present study is about further in silico and in vitro validation. We performed molecular dynamic (MD) simulation, gene ontology (GO), Kyoto Encyclopedia of Genes and Genomes (KEGG) analysis, cytotoxicity assay, and RT-PCR and qRT-PCR validation. According to the MD simulation (250 ns), we found that IGF1R, PIK3CA, and PTGS2, except for IL6 gene targets, show stable binding energy with a stable complex with isoquercitrin. We also performed gene ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) analyses of the final targets to determine their regulatory functions and signaling pathways. Furthermore, we checked the cytotoxicity effect of isoquercitrin (IQ) and found that 5 µg/mL and 10 µg/mL doses showed higher cell viability in a normal kidney cell line (HEK 293) and also inversely showed an inhibition of cell growth at 35% and 45%, respectively, in the kidney cancer cell line (A498). Lastly, the RT-PCR and qRT-PCR findings showed a significant decrease in PTGS2, PIK3CA, and IGF1R gene expression, except for IL6 expression, following dose-dependent treatments with IQ. Thus, we can conclude that isoquercitrin inhibits the expression of PTGS2, PIK3CA, and IGF1R gene targets, which in turn controls kidney cancer and inflammation.
ABSTRACT
BACKGROUND The gut microbial metabolites demonstrate significant activity against metabolic diseases including osteoporosis (OP) and obesity, but active compounds, targets, and mechanisms have not been fully identified. Hence, the current investigation explored the mechanisms of active metabolites and targets against OP and obesity by using network pharmacology approaches. MATERIAL AND METHODS The gutMGene database was used to collect gut microbial targets-associated metabolites; DisGeNET and OMIM databases were used to identify targets relevant to OP and obesity. A total of 63 and 89 overlapped targets were considered the final OP and obesity targets after creating a Venn diagram of metabolites-related targets and disease-related targets. Furthermore, the top 20% of degrees, betweenness, and closeness were used to form the sub-network of protein-protein interaction of these targets. Finally, the biotransformation-increased receptors and biological mechanisms were identified and validated using ADMET properties analysis, molecular docking, and molecular dynamic simulation. RESULTS GO, KEGG pathway analysis, and protein-protein interactions were performed to establish metabolites and target networks. According to the enrichment analysis, OP and obesity are highly linked to the lipid and atherosclerosis pathways. Moreover, ADMET analysis depicts that the major metabolites have drug-likeliness activity and no or less toxicity. Following that, the molecular docking studies showed that compound K and TP53 target have a remarkable negative affinity (-8.0 kcal/mol) among all metabolites and targets for both diseases. Finally, the conformity of compound K against the targeted protein TP53 was validated by 250ns MD simulation. CONCLUSIONS Therefore, we summarized that compound K can regulate TP53 and could be developed as a therapy option for OP and obesity.
Subject(s)
Drugs, Chinese Herbal , Gastrointestinal Microbiome , Ginsenosides , Osteoporosis , Humans , Molecular Docking Simulation , Network Pharmacology , Computational Biology , Molecular Dynamics Simulation , Obesity/drug therapy , Osteoporosis/drug therapyABSTRACT
SARS-CoV-2 is a novel coronavirus that emerged as an epidemic, causing a respiratory disease with multiple severe symptoms and deadly consequences. ACE-2 and TMPRSS2 play crucial and synergistic roles in the membrane fusion and viral entry of SARS-CoV-2 (COVID-19). The spike (S) protein of SARS-CoV-2 binds to the ACE-2 receptor for viral entry, while TMPRSS2 proteolytically cleaves the S protein into S1 and S2 subunits, promoting membrane fusion. Therefore, ACE-2 and TMPRSS2 are potential drug targets for treating COVID-19, and their inhibition is a promising strategy for treatment and prevention. This study proposes that ginsenoside compound K (G-CK), a triterpenoid saponin abundant in Panax Ginseng, a dietary and medicinal herb highly consumed in Korea and China, effectively binds to and inhibits ACE-2 and TMPRSS2 expression. We initially conducted an in-silico evaluation where G-CK showed a high affinity for the binding sites of the two target proteins of SARS-CoV-2. Additionally, we evaluated the stability of G-CK using molecular dynamics (MD) simulations for 100 ns, followed by MM-PBSA calculations. The MD simulations and free energy calculations revealed that G-CK has stable and favorable energies, leading to strong binding with the targets. Furthermore, G-CK suppressed ACE2 and TMPRSS2 mRNA expression in A549, Caco-2, and MCF7 cells at a concentration of 12.5 µg/mL and in LPS-induced RAW 264.7 cells at a concentration of 6.5 µg/mL, without significant cytotoxicity.ACE2 and TMPRSS2 expression were significantly lower in A549 and RAW 264.7 cells following G-CK treatment. These findings suggest that G-CK may evolve as a promising therapeutic against COVID-19.
ABSTRACT
Dendropanax morbifera (DM), a medicinal plant, is rich in polyphenols and commonly used to treat cancer, inflammation, and thrombosis. However, to date, no study has been conducted on DM regarding the enormous drift of secondary metabolites of plants in different regions of the Republic of Korea and their effects on antiobesity, to explore compounds that play an important role in two major obesity-related pathways. Here, we present an in-depth study on DM samples collected from three regions of the Republic of Korea [Jeju Island (DMJ), Bogildo (DMB), and Jangheung (DMJG)]. We used high-performance liquid chromatography (HPLC) and multivariate component analyses to analyze polyphenol contents (neochlorogenic acid, chlorogenic acid, cryptochlorogenic acid, and rutin), followed by discrimination of the samples in DMJG using single nucleotide polymorphism and chemometric analysis. In silico and in vitro evaluation of major compounds found in the plant extract on two major anti-obesity pathways (adipogenesis and thermogenesis) was carried out. Furthermore, two extraction methods (Soxhlet and ultrasound-assisted extraction) were used to understand which method is better and why. Upon quantifying plant samples in three regions with the polyphenols, DMJG had the highest content of polyphenols. The internal transcribed region (ITS) revealed a specific gel-based band for the authentication of DMJG. PCA and PLS-DA revealed the polyphenol's discriminative power of the region DMJG. The anti-obesity effects of plant extracts from the three regions were related to their polyphenol contents, with DMJG showing the highest effect followed by DMJ and DMB. Ultrasound-assisted extraction yielded a high number of polyphenols compared to that of the Soxhlet method, which was supported by scanning electron microscopy. The present work encourages studies on plants rich in secondary metabolites to efficiently use them for dietary and therapeutic purposes.
ABSTRACT
The gut microbiome is the community of healthy, and infectious organisms in the gut and its interaction in the host gut intestine (GI) environment. The balance of microbial richness with beneficial microbes is very important to perform healthy body functions like digesting food, controlling metabolism, and precise immune function. Alternately, this microbial dysbiosis occurs due to changes in the physiochemical condition, substrate avidity, and drugs. Moreover, various categories of diet such as "plant-based", "animal-based", "western", "mediterranean", and various drugs (antibiotic and common drugs) also contribute to maintaining microbial flora inside the gut. The imbalance (dysbiosis) in the microbiota of the GI tract can cause several disorders (such as diabetes, obesity, cancer, inflammation, and so on). Recently, the major interest is to use prebiotic, probiotic, postbiotic, and herbal supplements to balance such microbial community in the GI tract. But, there has still a large gap in understanding the microbiome function, and its relation to the host diet, drugs, and herbal supplements to maintain the healthy life of the host. So, the present review is about the updates on the microbiome concerns related to diet, drug, and herbal supplements, and also gives research evidence to improve our daily habits regarding diet, drugs, and herbal supplements. Because our regular dietary plan and traditional herbal supplements can improve our health by balancing the bacteria in our gut.
Subject(s)
Gastrointestinal Microbiome , Microbiota , Animals , Dysbiosis/microbiology , Dietary Supplements , Obesity/microbiologyABSTRACT
BACKGROUND: Ginseng (Panax ginseng Meyer) is a cultivated medicinal herb that has been widely available in the Asian region since the last century. Ginseng root is used worldwide in Oriental medicine. Currently, the global mortality and infection rates for lung cancer and inflammation are significantly increasing. Therefore, various preventative methods related to the activity of ginsenosides have been used for lung cancer as well as inflammation. METHODS: Web-based searches were performed on Web of Science, Springer, PubMed, and Scopus. A cancer statistical analysis was also conducted to show the current ratio of affected cases and death from lung cancer around the world. RESULTS: Ginsenosides regulate the enzymes that participate in tumor growth and migration, such as nuclear factor kappa B (NF-κB), mitogen-activated protein kinase (p38 MAPK), c-Jun N-terminal kinase (JNK), extracellular signalregulated kinases 1/2 (ERK1/2), the gelatinase network metalloproteinase-2 (MMP-2/9) and activator protein 1 (AP-1). In addition, ginsenosides also possess anti-inflammatory effects by inhibiting the formation of proinflammatory cytokines (tumor necrosis factor-α) (TNF-α) and interleukin-1ß (IL-1ß) and controlling the activities of inflammatory signalling pathways, such as NF-κB, Janus kinase2/signal transducer, and activator of transcription 3 (Jak2/Stat3). CONCLUSION: In several in vitro and in vivo models, P. ginseng showed potential beneficial effects in lung cancer and inflammation treatment. In this review, we provide a detailed and up-to-date summary of research evidence for antilung cancer and anti-inflammatory protective effects of ginsenosides and their potential molecular mechanisms.
Subject(s)
Ginsenosides , Neoplasms , Humans , NF-kappa B/metabolism , Ginsenosides/pharmacology , Ginsenosides/therapeutic use , Matrix Metalloproteinase 2 , Anti-Inflammatory Agents/pharmacology , Inflammation/drug therapy , Tumor Necrosis Factor-alpha , Lipopolysaccharides/therapeutic useABSTRACT
Ginsenoside Rh1 (G-Rh1), a possible bioactive substance isolated from the Korean Panax ginseng Meyer, has a wide range of pharmacological effects. In this study, we have investigated the anticancer efficacy of G-Rh1 via in silico and in vitro methodologies. This study mainly focuses on the two metastatic regulators, Rho-associated protein kinase 1 (ROCK1) and RhoA, along with other standard apoptosis regulators. The ROCK1 protein is a member of the active serine/threonine kinase family that is crucial for many biological processes, including cell division, differentiation, and death, as well as many cellular processes and muscle contraction. The abnormal activation of ROCK1 kinase causes several disorders, whereas numerous studies have also shown that RhoA is expressed highly in various cancers, including colon, lung, ovarian, gastric, and liver malignancies. Hence, inhibiting both ROCK1 and RhoA will be promising in preventing metastasis. Therefore, the molecular level interaction of G-Rh1 with the ROCK1 and RhoA active site residues from the preliminary screening clearly shows its inhibitory potential. Molecular dynamics simulation and principal component analysis give essential insights for comprehending the conformational changes that result from G-Rh1 binding to ROCK1 and RhoA. Further, MTT assay was employed to examine the potential cytotoxicity in vitro against human lung cancer cells (A549) and Raw 264.7 Murine macrophage cells. Thus, G-Rh1 showed significant cytotoxicity against human lung adenocarcinoma (A549) at 100 µg/mL. In addition, we observed an elevated level of reactive oxygen species (ROS) generation, perhaps promoting cancer cell toxicity. Additionally, G-Rh1 suppressed the mRNA expression of RhoA, ROCK1, MMP1, and MMP9 in cancer cell. Accordingly, G-Rh1 upregulated the p53, Bax, Caspase 3, caspase 9 while Bcl2 is downregulated intrinsic pathway. The findings from our study propose that the anticancer activity of G-Rh1 may be related to the induction of apoptosis by the RhoA/ROCK1 signaling pathway. As a result, this study evaluated the functional drug-like compound G-Rh1 from Panax ginseng in preventing and treating lung cancer adenocarcinoma via regulating metastasis and apoptosis.
Subject(s)
Ginsenosides , Lung Neoplasms , Panax , Humans , Mice , Animals , A549 Cells , rhoA GTP-Binding Protein/metabolism , rho-Associated Kinases/metabolism , Lung Neoplasms/drug therapy , Lung Neoplasms/metabolism , Ginsenosides/chemistry , Apoptosis , Panax/metabolismABSTRACT
For over 2000 years, ginseng (roots of Panax ginseng C.A. Meyer) has been used as a traditional herbal medicine. Ginsenosides are bioactive compounds present in ginseng responsible for the pharmacological effects and curing various acute diseases as well as chronic diseases including cardiovascular disease, cancer and diabetes. Structurally, ginsenosides consist of a hydrophobic aglycone moiety fused with one to four hydrophilic glycoside moieties. Based on the position of sugar units and their abundance, ginsenosides are classified into major and minor ginsenosides. Despite the great potential of ginsenosides, major ginsenosides are poorly absorbed in the blood circulation, resulting in poor bioavailability. Interestingly, owing to their small molecular weight, minor ginsenosides exhibit good permeability across cell membranes and bioavailability. However, extremely small quantities of minor ginsenosides extracted from ginseng plants cannot fulfill the requirement of scientific and clinical studies. Therefore, the production of minor ginsenosides in mass production is a topic of interest. In addition, their poor solubility and lack of targetability to tumor tissues limits their application in cancer therapy. In this review, various methods used for the transformation of major ginsenosides to minor ginsenoside compound K (CK) are summarized. For the production of CK, various transformation methods apply to major ginsenosides. The challenges present in these transformations and future research directions for producing bulk quantities of minor ginsenosides are discussed. Furthermore, attention is also paid to the utilization of nanoformulation technology to improve the bioavailability of minor ginsenoside CK.
ABSTRACT
Nanoscience is a multidisciplinary skill with elucidated nanoscale particles and their advantages in applications to various fields. Owing to their economical synthesis, biocompatible nature, and widespread biomedical and environmental applications, the green synthesis of metal nanoparticles using medicinal plants has become a potential research area in biomedical research and functional food formulations. Gynostemma pentaphyllum (GP) has been extensively used in traditional Chinese medicine to cure several diseases, including diabetes mellitus (DM). This is the first study in which we examined the efficacy of G. pentaphyllum gold nanoparticles (GP-AuNPs) against obesity and related inflammation. GP extract was used as a capping agent to reduce Au2+ to Au0 to form stable gold nanoparticles. The nanoparticles were characterized by using UV-VIS spectroscopy, and TEM images were used to analyze morphology. In contrast, the existence of the functional group was measured using FTIR, and size and shape were examined using XRD analysis. In vitro analysis on GP-AuNPs was nontoxic to RAW 264.7 cells and 3T3-L1 cells up to a specific concentration. It significantly decreased lipid accumulation in 3T3-L1 obese and reduced NO production in Raw 264.7 macrophage cells. The significant adipogenic genes PPARγ and CEPBα and a major pro-inflammatory cytokine TNF-α expression were quantified using RT-PCR. The GP-AuNPs decreased the face of these genes remarkably, revealing the antiadipogenic and anti-inflammatory activity of our synthesized GP-AuNPs. This study represents thorough research on the antiobesity effect of Gynostemma pentaphyllum gold nanoparticles synthesized using a green approach and the efficacy instead of related inflammatory responses.
Subject(s)
Gold , Metal Nanoparticles , Animals , Down-Regulation , Gene Expression , Gold/chemistry , Gold/pharmacology , Green Chemistry Technology/methods , Gynostemma , Inflammation/drug therapy , Inflammation/genetics , Metal Nanoparticles/chemistry , Mice , Obesity , PPAR gamma/genetics , Plant Extracts/chemistry , Plant Extracts/pharmacology , Tumor Necrosis Factor-alpha/geneticsABSTRACT
Ginseng is a traditional medicinal herb commonly consumed world-wide owing to its unique family of saponins called ginsenosides. The absorption and bioavailability of ginsenosides mainly depend on an individual's gastrointestinal bioconversion abilities. There is a need to improve ginseng processing to predictably increase the pharmacologically active of ginsenosides. Various types of ginseng, such as fresh, white, steamed, acid-processed, and fermented ginsengs, are available. The various ginseng processing methods produce a range ginsenoside compositions with diverse pharmacological properties. This review is intended to summarize the properties of the ginsenosides found in different Panax species as well as the different processing methods. The sugar moiety attached to the C-3, C-6, or C-20 deglycosylated to produce minor ginsenosides, such as Rb1, Rb2, Rc, RdâRg3, F2, Rh2; Re, RfâRg1, Rg2, F1, Rh1. The malonyl-Rb1, Rb2, Rc, and Rd were demalonylated into ginsenoside Rb1, Rb2, Rc, and Rd by dehydration. Dehydration also produces minor ginsenosides such as Rg3âRk1, Rg5, Rz1; Rh2âRk2, Rh3; Rh1âRh4, Rk3; Rg2âRg6, F4; Rs3âRs4, Rs5; RfâRg9, Rg10. Acetylation of several ginsenosides may generate acetylated ginsenosides Rg5, Rk1, Rh4, Rk3, Rs4, Rs5, Rs6, and Rs7. Acid processing methods produces Rh1âRk3, Rh4; Rh2âRk1, Rg5; Rg3âRk2, Rh3; Re, Rf, Rg2âF1, Rh1, Rf2, Rf3, Rg6, F4, Rg9. Alkaline produces Rh16, Rh3, Rh1, F4, Rk1, ginsenoslaloside-I, 20(S)-ginsenoside-Rh1-60-acetate, 20(R)-ginsenoside Rh19, zingibroside-R1 through hydrolysis, hydration addition reactions, and dehydration. Moreover, biological processing of ginseng generates the minor ginsenosides of Rg3, F2, Rh2, CK, Rh1, Mc, compound O, compound Y through hydrolysis reactions, and synthetic ginsenosides Rd12 and Ia are produced through glycosylation. This review with respect to the properties of particular ginsenosides could serve to increase the utilization of ginseng in agricultural products, food, dietary supplements, health supplements, and medicines, and may also spur future development of novel highly functional ginseng products through a combination of various processing methods.
Subject(s)
Ginsenosides/chemistry , Ginsenosides/isolation & purification , Panax/chemistryABSTRACT
Ginseng (Panax ginseng Meyer) is one of the most important medicinal herbs in Asia. Its pharmacological activity comes from ginsenosides, and its roots are produced commercially for traditional and Oriental medicine. Though 17 Panax species are available around the world, there was a need to develop cultivars adapted to different climatic conditions and resistant to various diseases while still producing high-quality, high-yield roots. Thus, 12 and 9 commercial P. ginseng cultivars have been registered in South Korea and China, respectively. Those varieties show superiority to local landraces. For example, Chunpoong is more highly resistant to rusty rot disease than the local Jakyungjong landrace and has a good root shape; it is highly cultivated to produce red ginseng. The Chinese cultivar Jilin Huangguo Renshen has higher ginsenoside content than its local landraces. This review provides information about P. ginseng cultivars and offers directions for future research, such as intra- and interspecific hybridization.
Subject(s)
Ginsenosides/analysis , Panax/chemistry , Panax/metabolism , China , Crops, Agricultural , Panax/classification , Republic of Korea , Species SpecificityABSTRACT
Root rot caused by Ilyonectria mors-panacis is a devastating fungal disease leading to defect in root quality and causes reduced yield during the perennial life cycle of Panax ginseng Meyer. This indicates the imperative need to understand the molecular basis of disease development and also to enhance tolerance against the fungus. With this idea, the protective effect of silicon (supplied as silica nanoparticles) in P. ginseng root rot pathosystem and its molecular mechanism was investigated in the current study. We have tested different concentrations of silicon (Si) to disease-infected ginseng and found that long term analysis (30 dpi) displayed a striking 50% reduction in disease severity index upon the treatment of Si. Expectedly, Si had no direct degradative effect against the pathogen. Instead, in infected roots it resulted in reduced expression of PgSWEET leading to regulated sugar efflux into apoplast and enhanced tolerance against I. mors-panacis. In addition, under diseased condition, both protopanaxadiol (PPD) and protopanaxatriol (PPT) type ginsenoside profile in roots were higher in Si treated plants. This is the first report indicating the protective role of Si in ginseng-root rot pathosystem, thereby uncovering novel features of ginseng mineral physiology and at the same time, enabling its usage to overcome root rot.
Subject(s)
Panax/microbiology , Plant Diseases/prevention & control , Plant Roots/microbiology , Silicon/pharmacology , Cyclopentanes/metabolism , Metabolic Networks and Pathways , Mevalonic Acid/metabolism , Nanoparticles , Oxylipins/metabolism , Panax/drug effects , Phytosterols/metabolism , Plant Diseases/microbiology , Plant Roots/drug effects , Silicon/administration & dosage , Sugars/metabolism , Triterpenes/metabolismABSTRACT
The obesity rate has been increasing worldwide, which is important because obesity has been linked to the development of various metabolic disorders, such as type 2 diabetes, hypertension, cancer, and stroke. Nanomedicine offers a new approach for treating many diseases, including metabolic disorders such as obesity. In this study, we explored the anti-adipogenic effects of spherical gold nanoparticles synthesized with fresh Panax ginseng leaves (P.g AuNPS) in vitro using 3T3-L1 mature adipocytes. Cell viability was assessed by quantitating preadipocyte growth at different time points. Furthermore, to assess the anti-adipogenic effects of P.g AuNPS, intracellular lipid accumulation was investigated in mature adipocytes. To this end, cells were observed under a microscope and OD measurements were taken after Oil Red O staining. In addition, transcriptional gene regulation was examined by performing real time PCR to assess the levels of adipogenic genes such as PPARγ, CEBPα, CEBPß, Jak2, STAT3, FAS, SREBP-1, and ap2. Moreover, protein levels were evaluated by immunoblotting. Altogether, these results confirm that P.g AuNPS exhibit anti-adipogenic effects at a concentration of 100 µg/ml and that these effects are mediated by the downregulation of PPARγ/CEBPα (major transcription factors) signaling in 3T3-L1 mature adipocytes.
Subject(s)
Adipocytes/drug effects , Adipogenesis/drug effects , CCAAT-Enhancer-Binding Proteins/genetics , Metal Nanoparticles , PPAR gamma/genetics , Plant Extracts/pharmacology , 3T3-L1 Cells , Adipogenesis/genetics , Animals , Cell Differentiation , Diabetes Mellitus, Type 2 , Gold , Mice , PanaxABSTRACT
A Gram-negative, non-motile, aerobic, catalase-, and oxidasepositive bacterial strain, designated DCY117T, was isolated from ginseng cultivated soil in Gochang-gun, Republic of Korea, and was characterized taxonomically using a multifaceted approach. 16S rRNA gene sequence analysis revealed that strain DCY117T showed highest similarity to Lysobacter ruishenii CTN-1T (95.3%). Phylogenetic analysis revealed that closely related relatives of strain DCY117T were L. aestuarii S2-CT (95.1%), L. daejeonensis GH1-9T (95.0%), and L. caeni BUT-8T (94.9%). Diphosphatidylglycerol (DPG), phosphatidylglycerol (PG), and phosphatidylethanolamine (PE) were the major polar lipids of strain DCY117T. The major isoprenoid quinone was Q-8. The major cellular fatty acids of strain DCY117T were iso-C15:0, iso-C16:0, and summed feature 9 (comprising iso-C17:1ω9c and/or 10-methyl-C16:0). Genomic DNA G + C content was 61.8 mol%. On the basis of our findings, strain DCY117T is a novel species in the genus Lysobacter. We propose the name Lysobacter panacihumi sp. nov., and the type strain is DCY117T (= KCTC 62019T = JCM 32168T).
Subject(s)
Lysobacter/classification , Panax/microbiology , Phylogeny , Soil Microbiology , Bacterial Typing Techniques , Base Composition , DNA, Bacterial/genetics , Fatty Acids/analysis , Lysobacter/genetics , Lysobacter/isolation & purification , Phospholipids/analysis , RNA, Ribosomal, 16S/genetics , Republic of Korea , Sequence Analysis, DNAABSTRACT
BACKGROUND: Bioactive compounds in plant extracts are able to reduce metal ions to nanoparticles through the process of green synthesis. Panax ginseng is an oriental medicinal herb and an adaptogen which has been historically used to cure various diseases. In addition, the P. ginseng leaves-mediated gold nanoparticles are the value-added novel materials. Its potential as a cosmetic ingredient is still unexplored. The aim of this study was to evaluate the antioxidant, moisture retention and whitening properties of gold nanoparticles (PgAuNPs) in cosmetic applications. METHODS: Cell-free experiments were performed to evaluate PgAuNP's antioxidant and moisture retention properties and inhibition activity on mushroom tyrosinase. Furthermore, in vitro cell cytotoxicity was evaluated using normal human dermal fibroblast and murine B16BL6 melanoma cells (B16) after treatment with increasing concentrations of PgAuNPs for 24 h, 48 h, and 72 h. Finally, in vitro cell assays on B16 cells were performed to evaluate the whitening effect of PgAuNPs through reduction of cellular melanin content and tyrosinase activity. RESULTS: In vitro DPPH radical scavenging assay results revealed that PgAuNPs exhibited antioxidant activity in a dose-dependent manner. PgAuNPs exhibited moisture retention capacity and effectively inhibited mushroom tyrosinase. In addition, 3-(4,5-dimethyl-thiazol-2yl)-2,5-diphenyl tetrazolium bromide results revealed that PgAuNPs were not toxic to human dermal fibroblast and B16 cells; in addition, they significantly reduced melanin content, tyrosinase activity, and mRNA expression of melanogenesis-associated transcription factor and tyrosinase in B16 cells. CONCLUSION: Our study is the first report to provide evidence supporting that P. ginseng leaves-capped gold nanoparticles could be used as multifunctional ingredients in cosmetics.
ABSTRACT
The current study highlights the rapid biosynthesis of gold nanoparticles (Gu-AuNps) and silver chloride nanoparticles (Gu-AgClNps) by aqueous root extract of Glycyrrhiza uralensis, a medicinal plant. G. uralensis has been reported for anticancer and hepatoprotective effects. The reduction of chloroauric acid and silver nitrate by the Glycyrrhiza root extract prompted the formation of Gu-AuNps and Gu-AgClNps within 4 and 40 min at 80 °C, respectively. The complete reaction did not require supplemental reducing and stabilizing agents, which demonstrated green synthesis. Field emission transmission electron microscopy (FE-TEM) revealed the spherical shape of Gu-AuNps and Gu-AgClNps. X-ray diffraction (XRD) showed face-centred cubic structure of Gu-AuNps and Gu-AgClNps with average crystallite size 12.25 nm and 8.01 nm, respectively. The biosynthesized Gu-AgClNps served as competent antimicrobial agent against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Salmonella enterica. Additionally, Gu-AuNps and Gu-AgClNps were analyzed for their catalytic ability to reduce methylene blue as model test pollutant. Likewise, both nanoparticles possessed free radical scavenging activity against 2,2-diphenyl-1-picrylhydrzyl (DPPH). Moreover, in vitro cytotoxicity in murine macrophage (RAW264.7) and human breast cancer (MCF7) cells were evaluated. Thus, the study proposes a green synthesis of Gu-AuNps and Gu-AgClNps by G. uralensis extract and in vitro biological applications. [Formula: see text].
Subject(s)
Glycyrrhiza uralensis/chemistry , Gold/chemistry , Gold/pharmacology , Metal Nanoparticles/chemistry , Nanotechnology , Plant Extracts/chemistry , Silver Compounds/chemistry , Animals , Anti-Bacterial Agents/chemical synthesis , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Antioxidants/chemical synthesis , Antioxidants/chemistry , Antioxidants/pharmacology , Catalysis , Chemistry Techniques, Synthetic , Green Chemistry Technology , Humans , MCF-7 Cells , Mice , RAW 264.7 CellsABSTRACT
Panax ginseng berry extract possess remarkable pharmacological effects on skin treatment such as anti-aging, antioxidant, promotor of collagen synthesis and alleviation against atopic dermatitis. In recent years, gold nanoparticles have gained much attention due to their extensive range of applications in particular in the field of drug delivery as a result of their biological compatibility and low toxicity. In a previous study, we designed and developed biocompatible gold and silver nanoparticles based on phytochemical profile and pharmacological efficacy of P. ginseng berry extract, we were able to reduce gold ions to nanoparticles through the process of green synthesis. However, its potential as a cosmetic ingredient is still unexplored. The aim of the present study is to investigate the moisture retention, in-vitro scavenging and whitening properties of gold nanoparticles synthesized from P. ginseng berry in cosmetic applications. Our findings confirm that P. ginseng berry mediated gold nanoparticles exhibited moisture retention capacity. In addition, MTT assay results confirmed that P. ginseng berry mediated gold nanoparticles are non-toxic to human dermal fibroblast and murine melanoma skin cells, possess scavenging activity, protect and provide alleviation against injured caused by H2O2-induced damage. In addition, P. ginseng berry mediated gold nanoparticles, significantly reduced melanin content and suppress tyrosinase activity in α-MSH-stimulated B16BL6 cells. We conclude that P. ginseng berry mediated gold nanoparticles are biocompatible and environmental affable materials and can be a potential novel cosmetic ingredient.
Subject(s)
Fruit/chemistry , Gold/chemistry , Gold/pharmacology , Metal Nanoparticles , Panax/chemistry , Plant Extracts/chemistry , Safety , Cell Line , Cell Survival/drug effects , Fibroblasts/cytology , Fibroblasts/drug effects , Free Radical Scavengers/adverse effects , Free Radical Scavengers/chemistry , Free Radical Scavengers/pharmacology , Gold/adverse effects , Humans , Hydrogen Peroxide/pharmacology , Melanins/metabolism , Monophenol Monooxygenase/metabolism , Skin Lightening Preparations/adverse effects , Skin Lightening Preparations/chemistry , Skin Lightening Preparations/pharmacologyABSTRACT
Pleuropterus multiflorus (Hasuo) is a widely used medicinal plant in Korea and China for treating amnesia, isnomia, heart throbbing etc. With the constructive idea of promoting the wide-spread usage of P. multiflorus, we propose its indirect usage in the form of biologically active silver (Pm-AgNPs) and gold nanoparticles (Pm-AuNPs). The synthesized nanoparticles were predominantly spherical, crystalline with the Z-average hydrodynamic diameter of 274.8nm and 104.8nm respectively. Also, proteins and phenols were identified as the major players involved in their synthesis and stability. Further, Pm-AgNPs at 25µg/mL were significantly cytotoxic to lung cancer cells, whereas, Pm-AuNPs were not cytotoxic to both normal keratinocyte and lung cancer cells even at 100µg/mL. In addition, further evaluation of the anti-cancer activity of these new nanoparticles, such as migration and apoptosis, shown that Pm-AgNPs have a potential therapeutic effect on A549 lung cancer cell treatment. To the best of our knowledge, this is the first report dissecting out the ability of the endemic P. multiflorus for the synthesis of bioactive silver and gold nanoparticle which would open up doors for its extensive usage in medicinal field.
Subject(s)
Gold/chemistry , Green Chemistry Technology/methods , Lung Neoplasms/pathology , Metal Nanoparticles/chemistry , Polygonaceae , Silver/chemistry , A549 Cells , Antineoplastic Agents, Phytogenic/isolation & purification , Antineoplastic Agents, Phytogenic/therapeutic use , Dose-Response Relationship, Drug , Drug Evaluation, Preclinical/methods , Gold/therapeutic use , Humans , Lung Neoplasms/drug therapy , Metal Nanoparticles/therapeutic use , Plant Extracts/isolation & purification , Plant Extracts/therapeutic use , Plant Roots , Silver/therapeutic useSubject(s)
Antineoplastic Agents, Phytogenic/therapeutic use , Ginsenosides/therapeutic use , Metal Nanoparticles/therapeutic use , Nanoconjugates/therapeutic use , Neoplasms/drug therapy , Panax/chemistry , Animals , Antineoplastic Agents, Phytogenic/administration & dosage , Antineoplastic Agents, Phytogenic/chemistry , Ginsenosides/administration & dosage , Ginsenosides/chemistry , Humans , Metal Nanoparticles/administration & dosage , Metal Nanoparticles/chemistry , Nanoconjugates/administration & dosage , Nanoconjugates/chemistryABSTRACT
There has been a growing interest in the design of environmentally affable and biocompatible nanoparticles among scientists to find novel and safe biomaterials. Panax ginseng Meyer berries have unique phytochemical profile and exhibit beneficial pharmacological activities such as antihyperglycemic, antiobesity, antiaging, and antioxidant properties. A comprehensive study of the biologically active compounds in ginseng berry extract (GBE) and the ability of ginseng berry (GB) as novel material for the biosynthesis of gold nanoparticles (GBAuNPs) and silver nanoparticles (GBAgNPs) was conducted. In addition, the effects of GBAuNPs and GBAgNPs on skin cell lines for further potential biological applications are highlighted. GBAuNPs and GBAgNPs were synthesized using aqueous GBE as a reducing and capping agent. The synthesized nanoparticles were characterized for their size, morphology, and crystallinity. The nanoparticles were evaluated for antioxidant, anti-tyrosinase, antibacterial, and cytotoxicity activities and for morphological changes in human dermal fibroblast and murine melanoma skin cell lines. The phytochemicals contained in GBE effectively reduced and capped gold and silver ions to form GBAuNPs and GBAgNPs. The optimal synthesis conditions (ie, temperature and v/v % of GBE) and kinetics were investigated. Polysaccharides and phenolic compounds present in GBE were suggested to be responsible for stabilization and functionalization of nanoparticles. GBAuNPs and GBAgNPs showed increased scavenging activity against 2,2-diphenyl-1-picrylhydrazyl free radicals compared to GBE. GBAuNPs and GBAgNPs effectively inhibited mushroom tyrosinase, while GBAgNPs showed antibacterial activity against Escherichia coli and Staphylococcus aureus. In addition, GBAuNPs were nontoxic to human dermal fibroblast and murine melanoma cell lines, and GBAgNPs showed cytotoxic effect on murine melanoma cell lines. The current results evidently suggest that GBAgNPs can act as potential agents for antioxidant, anti-tyrosinase, and antibacterial activities. In addition, GBAuNPs can be further developed into mediators in drug delivery and as antioxidant, anti-tyrosinase, and protective skin agents in cosmetic products. Consequently, the study showed the advantages of using nanotechnology and green chemistry to enhance the natural properties of GBs.