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The negative implications for weeds encourage the finding of novel sources of phytotoxic agents for sustainable management. While traditional herbicides are effective, especially at large scales, the environmental impact and proliferation of resistant biotypes present major challenges that natural sources could mitigate. In this study, the potential of ginger metabolites as phytotoxic agents has been investigated for the first time. Root extracts, prepared via various extraction techniques, showed phytotoxicity in wheat (Triticum aestivum L. cv. Burgos) coleoptile bioassays at 800–100 ppm, and the most active extract (prepared by sonication with ethyl acetate) was purified by chromatographic methods, yielding seven compounds: five phenolic metabolites with gingerol and shogaol structures, β-sitosterol, and linoleic acid. Some of the major phenolic metabolites, especially [6]-shogaol and [6]-gingerol, exerted phytotoxicity on wheat coleoptiles, Plantago lanceolata and Portulaca oleracea (broadleaf dicotyledon weeds). This promoted the study of a collection of derivatives, revealing that the 5-methoxy, oxime, and acetylated derivatives of [6]-shogaol and [6]-gingerol had interesting phytotoxicities, providing clues for improving the stability of the isolated structures. Ginger roots have been demonstrated to be a promising source of bioactive metabolites for weed control, offering novel materials with potential for the development of agrochemicals based on natural products. [ABSTRACT FROM AUTHOR]

Ginger (Zingiber officinale) is one of the most well-known spices and medicinal plants worldwide that has been used since ancient times to treat a plethora of diseases including cold, gastrointestinal complaints, nausea, and migraine. Beyond that, a growing body of literature demonstrates that ginger exhibits anti-inflammatory, antioxidant, anti-cancer and neuroprotective actions as well. The beneficial effects of ginger can be attributed to the biologically active compounds of its rhizome such as gingerols, shogaols, zingerone and paradols. Among these compounds, gingerols are the most abundant in fresh roots, and shogaols are the major phenolic compounds of dried ginger. Over the last two decades numerous in vitro and in vivo studies demonstrated that the major ginger phenolics are able to influence the function of various immune cells including macrophages, neutrophils, dendritic cells and T cells. Although the mechanism of action of these compounds is not fully elucidated yet, some studies provide a mechanistic insight into their anti-inflammatory effects by showing that ginger constituents are able to target multiple signaling pathways. In the first part of this review, we summarized the current literature about the immunomodulatory actions of the major ginger compounds, and in the second part, we focused on the possible molecular mechanisms that may underlie their anti-inflammatory effects. [ABSTRACT FROM AUTHOR]

The negative implications for weeds encourage the finding of novel sources of phytotoxic agents for sustainable management. While traditional herbicides are effective, especially at large scales, the environmental impact and proliferation of resistant biotypes present major challenges that natural sources could mitigate. In this study, the potential of ginger metabolites as phytotoxic agents has been investigated for the first time. Root extracts, prepared via various extraction techniques, showed phytotoxicity in wheat (Triticum aestivum L. cv. Burgos) coleoptile bioassays at 800–100 ppm, and the most active extract (prepared by sonication with ethyl acetate) was purified by chromatographic methods, yielding seven compounds: five phenolic metabolites with gingerol and shogaol structures, β-sitosterol, and linoleic acid. Some of the major phenolic metabolites, especially [6]-shogaol and [6]-gingerol, exerted phytotoxicity on wheat coleoptiles, Plantago lanceolata and Portulaca oleracea (broadleaf dicotyledon weeds). This promoted the study of a collection of derivatives, revealing that the 5-methoxy, oxime, and acetylated derivatives of [6]-shogaol and [6]-gingerol had interesting phytotoxicities, providing clues for improving the stability of the isolated structures. Ginger roots have been demonstrated to be a promising source of bioactive metabolites for weed control, offering novel materials with potential for the development of agrochemicals based on natural products.

Purpose (6)-Shogaol is the most prevalent bioactive compound in ginger. The aim of this study was to examine both the prophylactic and therapeutic effects of (6)-shogaol in an experimental periodontitis model. Materials and Methods Thirty-five male Wistar albino rats were divided into four groups. In the healthy group (n=5), no intervention was undertaken. In the periodontitis group (n=10), periodontitis was induced by ligature placement for 14 days. In the prophylaxis group (n=10), periodontitis was induced with ligature placement for 14 days, and during this time, 20 mg/kg/day of (6)-shogaol was administered via oral gavage. In the therapeutic group (n=10), periodontitis was induced with ligature placement for 14 days, and following the removal of the ligature, 20 mg/kg/day of (6)-shogaol was administered via oral gavage for 14 days. Alveolar bone loss was histometrically measured, and malondialdehyde (MDA), superoxide dismutase (SOD), glutathione peroxidase (GP), nuclear factor kappa B (NF-κB), receptor activator of nuclear factor kappa B ligand (RANKL), and osteoprotegerin (OPG) were immunohistochemically analyzed. Results Alveolar bone loss was significantly lower in the healthy group than in the remaining groups, as well as in the therapeutic group than in the periodontitis group (p<0.001). RANKL/OPG was significantly higher in the periodontitis group compared to the remaining groups and in the prophylaxis group compared to the therapeutic group (p<0.001). MDA was significantly lower in the healthy group than in the remaining groups (p<0.001). SOD was significantly lower in the periodontitis group than in the prophylaxis and therapeutic groups (p=0.039 and p=0.042, respectively). GP was significantly lower in the healthy group than in the prophylaxis and therapeutic groups (p=0.031 and p=0.002, respectively). Conclusion The administration of (6)-shogaol modulated the RANKL/OPG balance and antioxidant status in rats with ligature-induced periodontitis. [ABSTRACT FROM AUTHOR]

Ginger (Zingiber officinale) is one of the most well-known spices and medicinal plants worldwide that has been used since ancient times to treat a plethora of diseases including cold, gastrointestinal complaints, nausea, and migraine. Beyond that, a growing body of literature demonstrates that ginger exhibits anti-inflammatory, antioxidant, anti-cancer and neuroprotective actions as well. The beneficial effects of ginger can be attributed to the biologically active compounds of its rhizome such as gingerols, shogaols, zingerone and paradols. Among these compounds, gingerols are the most abundant in fresh roots, and shogaols are the major phenolic compounds of dried ginger. Over the last two decades numerous in vitro and in vivo studies demonstrated that the major ginger phenolics are able to influence the function of various immune cells including macrophages, neutrophils, dendritic cells and T cells. Although the mechanism of action of these compounds is not fully elucidated yet, some studies provide a mechanistic insight into their anti-inflammatory effects by showing that ginger constituents are able to target multiple signaling pathways. In the first part of this review, we summarized the current literature about the immunomodulatory actions of the major ginger compounds, and in the second part, we focused on the possible molecular mechanisms that may underlie their anti-inflammatory effects.

ABSTRACTThe rapid increase in agricultural waste is rising across the globe and is a big environmental challenge. The utilization of ginger waste as a valuable product is very limited. The up-cycling of ginger waste is an effective approach for valorization. Ginger waste contains many bio-active compounds. These bioactive compounds possess various functional and bio-active properties. The literature has indicated that ginger and its waste is a rich source of shogaol zingerone and gingerols, these bioactive components contribute to pungency and aroma characteristics These compounds have a wide range of antimicrobial, antioxidant, and anti-inflammatory properties. Furthermore, these have a key role in skin health and the digestive system. The current review consolidates the compositional, functional, medicinal, bioactive, and health-endorsing attributes of ginger waste. The use of ginger wastes for the development of various functional and nutraceutical products is also in the limelight of this paper.

Red ginger (Zingiber officinale var. Rubrum) is one of the traditional medicines of the Zingiberaceae family, which contains phenolic ketone compounds, including gingerol and shogaol. At high temperatures, gingerol compounds become unstable and will change into shogaol. This study optimized conditions for the simultaneous separation of 6-gingerol, 8-gingerol, 10-gingerol and 6-shogaol from the red ginger extract using the High-Performance Liquid Chromatography method. The analytical conditions consisted of five different methods by modifying the composition of the mobile phase, the elution system, the flow rate of the mobile phase and the optimum UV wavelength. The best conditions for the simultaneous separation using a ratio of water: acetonitrile mobile phase in method 4 with a gradient elution system including 0 min (65:35); 1.5 min (40:60); 5-6.5 min (10:90); 7.5–9 min (0:100); 9.5–12 min (65:35); the mobile phase flow rate was 1.1 mL/min at an optimum wavelength of 230 nm with a retention time of 6-gingerol compound, 6-shogaol, 8-gingerol and 10-gingerol respectively were 4.947; 6.168; 6.554; and 7.412 min and its resolution were 2.267; 1.575; 1.315; and 2.215. Then the tailings factor and asymmetry values were obtained with an average value of ± 1.

Ginger or Zingiber officinale Roscoe is a well-known herbal medicine and is widely used in Asian cuisine. Its major bioactive compounds, 6-gingerol and its dehydrated form, 6-shogaol, were reported to have potential medicinal properties. However, previous phytochemical studies on the compounds are limited to conventionally grown or soil-based ginger, neglecting soilless ginger grown through hydroponic techniques. This technique has been widely adopted as an alternative to circumvent soil-related complications. Therefore, this study aimed to compare both marker compounds in soil-based (SB) and soilless-grown hydroponic (HP) ginger extracted in different ethanol concentrations (95% and 100%) using high-performance liquid chromatography. The study initially found that 6-gingerol concentration in 95% SB ginger ethanolic extract (1.012%) was significantly higher (p< 0.05) than in 95% HP dried ginger (HP1) ethanolic extract (0.314%). The 6-gingerol content for both gingers were also significantly higher (p< 0.05) in 95% ethanolic extracts compared to 100% ethanolic extracts. The analysis was also performed with fresh-dried HP ginger (HP2), and it was found that the HP2 ginger (0.75%) has a significantly higher 6-gingerol concentration (p< 0.05) compared to HP1 ginger (0.314%), confirming that the previous results were implicated by storage conditions. The concentration of 6-gingerol in 95% SB ginger extract (1.012%) differ significantly compared to those in HP2 extract (0.75%) while both gingers have equivalent amount of low 6-shogaol concentrations (0.0004% and 0.0005% respectively). It is worth to note that HP ginger grown in soilless condition could still produce high amount of 6-gingerol. This finding encourages the usage of HP ginger in pharmacological studies considering the other economic and environmental benefits it offers. [ABSTRACT FROM AUTHOR]

Ginger (Zingiber officinale Rosc.) is a plant known all over the world that is used as a spice and as an ingredient in drinks, dietary supplements, and cosmetics. The growing availability of its fresh rhizomes makes it even more likely to be used in the diet, mainly due to its beneficial health properties and high content of polyphenols (gingerols and shogaols). The main goal and motivation of the authors was to assess the bioavailability of active substances contained in the extract from ginger rhizomes in the presence of various types of diets using the in vitro digestion method, enabling simulation of the processes occurring during the digestion and absorption of metabolites in the small intestine. For the qualitative and quantitative analyses, the HPLC-MS (High Performance Liquid Chromatography–Mass Spectrometry) and HPLC (High Performance Liquid Chromatography) techniques were used, respectively. Based on the obtained results, it was found that the best bioavailability of the selected ginger polyphenols (6-gingerol, 8-gingerdione, 8-shogaol, and 10-gingerdione) was estimated for a high-fiber diet, while the weakest results were obtained for standard and basic diets. In the case of the high-fiber diet, the bioavailability of the mentioned compounds was estimated as 33.3, 21.4, 6.73, and 21.0%, while for the basic diet, it was only 21.3, 5.3, 2.0, and 1.0%, respectively. [ABSTRACT FROM AUTHOR]

Ginger (Zingiber officinale Rosc.) is a plant recognized for its pungent taste and aromatic qualities, primarily derived from its underground rhizome. Apart from its widespread culinary applications, ginger is valued for its potential health benefits attributed to the presence of gingerols and shogaols. For this reason, this work proposes the development of a microwave-assisted extraction (MAE) method for the extraction of gingerols and shogaols present in ginger rhizomes. The influence of the extraction temperature (50–100 °C), the solvent composition (50–100% ethanol in water), and the sample-to-solvent ratio (0.3–0.7 g sample: 20 mL) on the extraction of these bioactive compounds has been studied. To this end, a Box–Behnken experimental design (BBD) in combination with a response surface methodology (RSM) has been applied. The optimum conditions for the total extraction of gingerols and shogaols were: 87% ethanol in water, 100 °C, and 0.431 g of ginger sample in 20 mL solvent. The developed method required short extraction times (5 min) and demonstrated favorable levels of repeatability and intermediate precision (CV < 5%). Finally, the MAE method was successfully used for the extraction of gingerols and shogaols from a variety of ginger samples. [ABSTRACT FROM AUTHOR]

Background: Cervical cancer has accounted for the top-four cancer incidences occurring among females worldwide. Despite the availability of anticancer drugs as one of its treatment modalities, they are not without adverse effects. It has come to researchers' attention that natural bioactive compounds have anticancer properties, as reported in many pre-clinical studies. Materials and Methods: This systematic review protocol conforms to the Preferred Reporting Items for Systematic Review and Meta-analysis Protocols-P guideline and Population, Intervention, Comparison Outcome and Study framework. Electronic databases, including PubMed, Scopus and ScienceDirect, will be searched from inception until May 2022 for articles published in English. Only studies that investigate the effects of curcumin, gingerol, shogaol and/or their combination in human cervical cancer cell lines and/or rodent animal models implanted with cervical cancer xenografts will be included. A customised risk-of-bias tool (RoB) and the Systematic Review Centre for Laboratory Animal Experimentation's RoB will be used to assess the quality of in vitro and in vivo studies, respectively. Where appropriate, a meta-analysis will be performed using RevMan version 5.4. Conclusions: Findings obtained from this review may be used as valuable evidence to guide and direct future studies pertaining chemopreventive effects of bioactive compounds in cervical cancer. [ABSTRACT FROM AUTHOR]

Background: Cervical cancer has accounted for the top-four cancer incidences occurring among females worldwide. Despite the availability of anticancer drugs as one of its treatment modalities, they are not without adverse effects. It has come to researchers' attention that natural bioactive compounds have anticancer properties, as reported in many pre-clinical studies. Materials and Methods: This systematic review protocol conforms to the Preferred Reporting Items for Systematic Review and Meta-analysis Protocols-P guideline and Population, Intervention, Comparison Outcome and Study framework. Electronic databases, including PubMed, Scopus and ScienceDirect, will be searched from inception until May 2022 for articles published in English. Only studies that investigate the effects of curcumin, gingerol, shogaol and/or their combination in human cervical cancer cell lines and/or rodent animal models implanted with cervical cancer xenografts will be included. A customised risk-of-bias tool (RoB) and the Systematic Review Centre for Laboratory Animal Experimentation's RoB will be used to assess the quality of in vitro and in vivo studies, respectively. Where appropriate, a meta-analysis will be performed using RevMan version 5.4. Conclusions: Findings obtained from this review may be used as valuable evidence to guide and direct future studies pertaining chemopreventive effects of bioactive compounds in cervical cancer. This protocol is registered on PROSPERO (CRD42022334940).

Identifying cancer biomarkers is imperative, as upregulated genes offer a better microenvironment for the tumor; hence, targeted inhibition is preferred. The theme of our study is to predict molecular interactions between cancer biomarker proteins and selected natural compounds. We identified an overexpressed potential molecular target (AKT1) and computationally evaluated its inhibition by four dietary ligands (isoliquiritigenin, shogaol, tehranolide, and theophylline). The three-dimensional structures of protein and phytochemicals were retrieved from the RCSB PDB database (4EKL) and NCBI's PubChem, respectively. Rational structure-based docking studies were performed using AutoDock. Results were analyzed based primarily on the estimated free binding energy (kcal/mol), hydrogen bonds, and inhibition constant, Ki, to identify the most effective anti-cancer phytomolecule. Toxicity and drug-likeliness prediction were performed using OSIRIS and SwissADME. Amongst the four phytocompounds, tehranolide has better potential to suppress the expression of AKT1 and could be used for anti-cancer drug development, as inhibition of AKT1 is directly associated with the inhibition of growth, progression, and metastasis of the tumor. Docking analyses reveal that tehranolide has the most efficiency in inhibiting AKT1 and has the potential to be used for the therapeutic management of cancer. Natural compounds targeting cancer biomarkers offer less rejection, minimal toxicity, and fewer side effects. [ABSTRACT FROM AUTHOR]

The rapid increase in agricultural waste is rising across the globe and is a big environmental challenge. The utilization of ginger waste as a valuable product is very limited. The up-cycling of ginger waste is an effective approach for valorization. Ginger waste contains many bio-active compounds. These bioactive compounds possess various functional and bio-active properties. The literature has indicated that ginger and its waste is a rich source of shogaol zingerone and gingerols, these bioactive components contribute to pungency and aroma characteristics These compounds have a wide range of antimicrobial, antioxidant, and anti-inflammatory properties. Furthermore, these have a key role in skin health and the digestive system. The current review consolidates the compositional, functional, medicinal, bioactive, and health-endorsing attributes of ginger waste. The use of ginger wastes for the development of various functional and nutraceutical products is also in the limelight of this paper. [ABSTRACT FROM AUTHOR]

Ginger (Zingiber officinale Rosc.) is a plant known all over the world that is used as a spice and as an ingredient in drinks, dietary supplements, and cosmetics. The growing availability of its fresh rhizomes makes it even more likely to be used in the diet, mainly due to its beneficial health properties and high content of polyphenols (gingerols and shogaols). The main goal and motivation of the authors was to assess the bioavailability of active substances contained in the extract from ginger rhizomes in the presence of various types of diets using the in vitro digestion method, enabling simulation of the processes occurring during the digestion and absorption of metabolites in the small intestine. For the qualitative and quantitative analyses, the HPLC-MS (High Performance Liquid Chromatography–Mass Spectrometry) and HPLC (High Performance Liquid Chromatography) techniques were used, respectively. Based on the obtained results, it was found that the best bioavailability of the selected ginger polyphenols (6-gingerol, 8-gingerdione, 8-shogaol, and 10-gingerdione) was estimated for a high-fiber diet, while the weakest results were obtained for standard and basic diets. In the case of the high-fiber diet, the bioavailability of the mentioned compounds was estimated as 33.3, 21.4, 6.73, and 21.0%, while for the basic diet, it was only 21.3, 5.3, 2.0, and 1.0%, respectively.

Ginger (Zingiber officinale Rosc.) is a plant recognized for its pungent taste and aromatic qualities, primarily derived from its underground rhizome. Apart from its widespread culinary applications, ginger is valued for its potential health benefits attributed to the presence of gingerols and shogaols. For this reason, this work proposes the development of a microwave-assisted extraction (MAE) method for the extraction of gingerols and shogaols present in ginger rhizomes. The influence of the extraction temperature (50–100 °C), the solvent composition (50–100% ethanol in water), and the sample-to-solvent ratio (0.3–0.7 g sample: 20 mL) on the extraction of these bioactive compounds has been studied. To this end, a Box–Behnken experimental design (BBD) in combination with a response surface methodology (RSM) has been applied. The optimum conditions for the total extraction of gingerols and shogaols were: 87% ethanol in water, 100 °C, and 0.431 g of ginger sample in 20 mL solvent. The developed method required short extraction times (5 min) and demonstrated favorable levels of repeatability and intermediate precision (CV < 5%). Finally, the MAE method was successfully used for the extraction of gingerols and shogaols from a variety of ginger samples.

Gingerol and shogaol are two bioactive compounds of ginger which exhibit several positive effects on human health. The conventional method for shogaol preparation is considered ineffective because it causes losses to the environmental system, and the efficiency of the process is low. Reactive extraction with subcritical water is a method that is considered environmentally friendly for the separation of slightly polar components without using organic solvents. The advantage of the reactive extraction process with subcritical water is that it does not require a catalyst because the process is able to form hydronium ions which can act as a catalyst to convert shogaol into gingerol. The effect of time and temperature on the yields of subcritical water reactive extraction of gingerol and shogaol were investigated in the present work. Experiments were carried out at a fixed pressure of 2 bar, and a varied temperature of reactive extraction from 130 to 140°C. Ginger and shogaol contents were analysed from the samples every 10 min. The chemical profiling of the resulting ginger extracts was performed using HPLC-MS. Results showed that the best subcritical water process was at 2 bar, 130°C, and 20 min; shogaol concentration increased to 15.345%, and gingerol to 5.113%. For the reactive extraction time of longer than 20 min, the shogaol concentration of the extract decreased. When temperature was above 120°C, and water hydrogen bonds weakened, thus resulting in high amounts of ionisation products of subcritical water. [ABSTRACT FROM AUTHOR]

Zingiber officinale var. rubrum is known as 'Halia bara' in the Southeast Asia region. Many herbal products containing Halia bara are in the market are being used for either cosmetic purposes or well-being. The present study aims to develop a simple, high-performance liquid chromatography (HPLC) method using a diode array detector for the quantification of predominant gingerols (4-, 6-, 8-, and 10-) and shogaols (6-, 8-, and 10-) in supercritical carbon dioxide extract of Halia bara. The optimum conditions for elution of seven compounds were: column, ODS Genesis; column temperature, 25 °C; elution, gradient elution consisting of acetonitrile and aqueous formic acid; detection wavelength, 282 nm; flow rate, 1 mL/min; injection volume, 20 µL; and run-time, 38 min. The optimized HPLC method was validated for linear range, accuracy, precision (repeatability and reproducibility), sensibility (limit of detection and quantification) and recovery. All the validation parameters were within the permissible limits stipulated by the International Council of Harmonization guidelines. In Halia bara supercritical fluid-carbon dioxide extract, the amounts of bioactive constituents are in the decreasing order of 10-gingerol, 6-gingerol, 6-shogaol, 8-gingerol, 8-shogaol, 10-shogaol and 4-gingerol. [ABSTRACT FROM AUTHOR]

Data BPS 2017, menunjukan bahwa jahe adalah tanaman biofarmaka kelompok rimpang yang mempunyai luas panen paling tinggi, yaitu sebesar 30 ton per tahun dengan kondisi produksi yang relatif stabil. Ekstraksi pada rimpang jahe adalah penyarian zat-zat aktif dari bagian tanaman obat yang bertujuan untuk menarik komponen kimia yang terdapat dalam simplisia yang didasarkan pada perpindahan massa komponen zat padat ke dalam pelarut. Tujuan dari penelitian ini adalah menganalisis pengaruh proses pengeringan terhadap aktivitas senyawa 6-gingerol pada ekstrak jahe dengan metode ekstraksi maserasi menggunakan pelarut etanol berkonsentrasi 30%, 70%, dan 96%. Hasil dari analisa kadar 6-gingerol dengan menggunakan LC-MS didapatkan bahwa kandungan tertinggi terdapat pada sampel yang diekstraksi dengan etanol 96%, yaitu 2,01%. Sedangkan, kadar terendah terdapat pada etanol 30%, yaitu 0,64%. Di lain sisi, sampel jahe yang diekstraksi dengan etanol 70% memiliki kandungan 6-gingerol sebesar 1,21%. Hal ini disebabkan oleh semakin pekatnya konsentrasi suatu pelarut, maka akan mengakibatkan semakin tingginya konstanta dielektriknya.

Objectives Dried ginger and ginger are the same type of medicine and food. The differential components of ginger and dried ginger, dried ginger and ginger charcoal were investigated. Materials and Methods The experimental materials were divided into three sample groups: the ginger group, dried ginger group, and ginger charcoal group. The ginger group, dried ginger group, and ginger charcoal group were qualitatively analyzed by ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry. The data were processed by Marker View Software. Principal component analysis and orthogonal partial least-square discriminant analysis were performed with SIMCA 13.0 Software. The differential components of the ginger and dried ginger groups as well as the dried ginger and ginger charcoal groups with a variable importance in the projection > 2 (P < 0.05) were identified with PeakView 1.2 Software. Results Ten differential components, including 6-gingerol, 8-gingerol, and 10-gingerol, were identified between the ginger group and dried ginger group; 13 differential components, including 6-shogaol, 10-gingerol, and zingiberone, were identified between the dried ginger group and ginger charcoal group. Conclusions The main differential components between the ginger and dried ginger groups and the dried ginger and ginger charcoal groups were gingerols and diphenylheptanes. Based on metabolomics analysis of the chemical composition of ginger's medicinal materials, effects, and other related factors, it is recommended that 6-gingerol, 6-shogaol, and zingiberone should be used as indicative components for the respective quality evaluation of ginger, dried ginger and ginger charcoal. The results of this study may provide a basis for the reasonable quality evaluation of ginger medicinal materials. [ABSTRACT FROM AUTHOR]

Objective(s): This study aimed to investigate the effect of Shogaol on dextran sodium sulfate (DSS)- induced ulcerative colitis (UC) in mice compared to an immune-suppressant chemotherapeutic medicine, known as 6-thioguanine (6-TG). Materials and Methods: Thirty-six adult BALB/c mice were divided into six groups: group 1 (positive control): no DSS exposure and no treatment; group 2 (negative control): DSS exposure without treatment; group 3 (vehicle control): DSS exposure and olive oil treatment; group 4: DSS exposure and 0.3 mg/kg 6-TG treatment; group 5: DSS exposure and 20 mg/kg Shogaol treatment; and group 6: DSS exposure and 40 mg/kg Shogaol treatment. At day 16, the mice were euthanized and UC was evaluated according to colon length, histologically index score and expression scores of the epidermal growth factor receptor (EGFR).Results: The disease activity index (DAI) and histological index scores of mice treated with 40 mg/kg body weight (BW) Shogaol were approximately lower than the corresponding scores of mice treated with 6-TG. In addition, the rate of healing in the former mice was approximately 3 folds higher than that of the latter ones as indicated by the lack of EGFR expression in colonic glands and macrophages. Conclusion: These findings showed that the therapeutic effect of 40 mg/kg BW Shogaol could be better than 6-TG in the treatment of UC, and it may draw the attention regarding the priority of using this cheap plant-derived substance for treatment of the inflammatory bowel diseases because treatment with 6-TG is usually associated with adverse side effects.

Abstract Background Antibiotic resistance is a defense mechanism, harbored by pathogens to survive under unfavorable conditions. Among several antibiotic resistant microbial consortium, Staphylococcus aureus is one of the most havoc microorganisms. Staphylococcus aureus encodes a unique enzyme 6-hydroxymethyl-7,8-dihydropterin pyrophosphokinase (SaHPPK), against which, none of existing antibiotics have been reported. Methods Computational approaches have been instrumental in designing and discovering new drugs for several diseases. The present study highlights the impact of ginger phytochemicals on Staphylococcus aureus SaHPPK. Herein, we have retrieved eight ginger phytochemicals from published literature and investigated their inhibitory interactions with SaHPPK. To authenticate our work, the investigation proceeds considering the known antibiotics alongside the phytochemicals. Molecular docking was performed employing GOLD and CDOCKER. The compounds with the highest dock score from both the docking programmes were tested for their inhibitory capability in vitro. The binding conformations that were seated within the binding pocket showing strong interactions with the active sites residues rendered by highest dock score were forwarded towards the molecular dynamic (MD) simulation analysis. Results Based on molecular dock scores, molecular interaction with catalytic active residues and MD simulations studies, two ginger phytochemicals, gingerenone-A and shogaol have been proposed as candidate inhibitors against Staphylococcus aureus. They have demonstrated higher dock scores than the known antibiotics and have represented interactions with the key residues within the active site. Furthermore, these compounds have rendered considerable inhibitory activity when tested in vitro. Additionally, their superiority was corroborated by stable MD results conducted for 100 ns employing GROMACS package. Conclusions Finally, we suggest that gingerenone-A and shogaol may either be potential SaHPPK inhibitors or can be used as fundamental platforms for novel SaHPPK inhibitor development.

Ginger had been reported to ameliorate painful diabetic neuropathy (PDN) in an animal model. Gingerol and shogaol were active compounds of ginger that potentially act on transient receptor potential cation channel subfamily V member 1 (TRPV1), a key receptor in PDN. This study aims to predict the binding of gingerol and shogaol to TRPV1 using an in silico model. The ligands of the docking study were 3 chemical compounds of each gingerol and shogaol, i.e. 6-shogaol, 8-shogaol, 10-shogaol, 6-gingerol, 8 gingerol and 10-gingerol. Capsaicin, a TRPV1 agonist, was used as a native ligand. The TRPV1 structure was taken from Protein Data Bank (ID 3J9J). The docking analysis was performed using Autodock Vina. The result showed that among the ginger active compounds, 6-shogaol had the strongest binding energy (-7.10 kcal/mol) to TRPV1. The 6-shogaol lacked the potential hydrogen bond to Ile265 of TRPV1 protein, which capsacin had. However, it's binding energy towards TRPV1 was not significantly different compared to capsaicin. Therefore, 6-shogaol had potential to be developed as a treatment for PDN.

Herbal medicinal plants are used to treat various disorders in many traditional medicinal systems around the world. Usage of this herb found in Indian and Chinese medicinal systems. The availability of ginger herb is Universal these days, where it is cultivated for its underground stem (Pseudo-stem). Most commonly used part is rhizome. This ginger rhizome has many therapeutic uses including anti-inflammatory, antidiabetics, antioxidant, anti-microbial and also curing in vomiting, constipation, indigestion, cold, fever, cough, nausea, reparatory conditions, bronchitis etc., these activities were checked using different solvents of different polarity. Arthritis is known for its extreme joint pain and swelling may be treated by using ginger essential oil extract. It was studied that it has the capacity to reducing the pro-inflammatory molecules by lowering the RA-F, CRP, ESR level in the blood. The essences of ginger are due to the chemicals present in them. The products obtained from the ginger like essential oil and oleoresin are used all around the world for its food and pharmaceutical properties. The bioactive compounds like [6]- gingerol and its dehydrated form [6]- shogaol can inhibits the production of free radicals and oxidative stress, along with this properties it can reduce the pro-inflammatory molecules like prostaglandins by inhibiting COX-1 and COX-2.It also observed by the recent studies that the ginger and its extract have the capacity of suppressing the leukotriene biosynthesis by inhibiting 5-lipoxygenase. To this effect in-vitro study conducted in the lab shows the maximum inhibition as well as maximum protection by the ginger essential oil extract. The essential oil extraction were administered external apply and the variation in the certain proteins and inflammation related antibodies were studied. [ABSTRACT FROM AUTHOR]

Yavagu or rice gruels are used as daily food items in Kerala and southern part of India. “Panchakola siddha yavagu” is a medicated rice gruel mentioned in classical Ayurveda book Charaka Samhita, in Sutrasthana “Apamarga tanduliya” chapter. Additionally, it is used in inflammatory conditions such as Gout arthritis. It contains drugs such as Pippali (Piper longum), Pippalimoola (Root of Piper nigrum), Nagara (Zingiber officinale), Chavya (Piper chaba) and Chitraka (Plumbago zeylanica) along with six parts of water and one part of rice. In the case of Gouty arthritis, from an Ayurvedic point of view, it is caused by improper digestion of food in the body associated with doshas such as vata and rakta. It causes reddish discolouration, debility, looseness and cutting or pulsating types of pain in the knees, ankles, hips, shoulders, fingers and toes. The drugs mentioned in Panchakola Siddha Yavagu, i.e., Shogaol present in dry ginger (Nagara), Plumbagin present in fire plant (Chitraka), Piperine present in Long pepper (Pippali), Long pepper root (Pippali moola), and Wild pepper (Chavya) were proved to have anti-inflammatory properties. Therefore, it is understood that consuming rice gruel containing these drugs will help to reduce symptoms such as inflammation, looseness and pain present in joints in conditions such as Gouty arthritis.

Abstract: This study investigated the ability of formulation containing Zingiber officinale (ginger) to reverse health changes promoted by unhealthy diet in Wistar rats. Five compounds from the gingerol family and three from the shogaol family were identified in the chromatographic analyzes of the extract. The animals were fed a combination of unhealthy foods, the cafeteria diet, which promoted increases in body weight, hepatocyte nucleus area, total hepatocyte area and liver fat accumulation, as well as reduced hepatic glutathione S-transferase concentration, compared to the control group, which received commercial chow. The treatment with ginger improved all these results, highlighting the reduction of 10% of body weight and 66% of the total area of lipid droplets deposited, compared to the group that received the cafeteria diet. Ginger treatments also attenuated lipid peroxidation, with a mean reduction of 41% in malondialdehyde levels and a mean increase of 222% in glutathione S-transferase activity in the liver. The cafeteria diet and ginger extract did not promote significant changes in glycemic and lipid profile, liver weight and liver enzymes compared to the control group. We suggest that ginger can have beneficial effects on health complications associated with unhealthy diet, such as excessive adiposity, oxidative stress and hepatic injury.

Aim. This study is aimed at investigating the effect of Shogaol, a phenolic constituent of ginger, on dextran sodium sulfate- (DSS-) induced ulcerative colitis (UC) in mice in comparison with 6-thioguanine (6-TG), an immune-suppressant chemotherapeutic medicine used for treatment of ulcerative colitis. Material & Methods. Thirty-six adult, male and female BALB/c mice were randomly divided into six groups: group 1 (control negative) not exposed to DSS and did not receive any treatment, group 2 (control positive) exposed to DSS but did not receive any treatment, group 3 exposed to DSS and treated by 0.1 mg/kg of 6-thioguanine, and groups 4, 5, and 6 exposed to DSS and treated by 10, 20, and 40 mg/kg b.w. Shogaol, respectively. At day 56, the mice were checked for their disease activity index (DAI) and they were sacrificed. The colons of the mice were examined for length measurement, histological index score, and the expression of CD133 and CD34 stem cell markers. Results. Shogaol showed a better curative effect than did 6-TG in repairing the colonic mucosal damages in DSS-exposed mice as indicated by the levels of CD133 and CD34 expression in the colonic crypts and by the DAI score, colon length measurements, & histological index score which were significantly reduced in mice treated by Shogaol, particularly the 20 and 40 mg/kg BW doses. Conclusion. The results of this study indicated that oral treatment with the ginger-derived substance Shogaol could be better than the conventional immunosuppressive chemotherapeutic remedy 6-TG in treatment of DSS-induced UC. [ABSTRACT FROM AUTHOR]

Ginger, the rhizome of Zingiber officinale, which is used as a spice globally has a long history of medicinal use that stimulates investigators to assess its potential roles as an adjuvant therapy or alternative medicine in a range of diseases. Anti‐inflammatory, antioxidant, antitumor, and antiulcer effects of ginger have been proven in many scientific studies, and some of the ancient applications of ginger as a home remedy has been confirmed in human. In this review, we summarized the current evidence on the effects of ginger consumption on gastrointestinal disorders based on clinical trials. Our data indicate that divided lower daily dosage of 1500 mg ginger is beneficial for nausea relief. Because of limited number of studies on some other gastrointestinal disorders, the results may not be as much powered as to find significant results. Therefore, more extensive and well‐controlled human studies of ginger or its standard extracts are required to demonstrate its efficacy as a gastroprotective agent. Dose‐finding studies should be undertaken to accurately determine the effective dose and preparation of ginger in further clinical trials protocol. This review shows that ginger is a useful supplement for many gastrointestinal symptoms such as nausea, vomiting, bloating. It can be used at 1000 mg/day without any side effects. [ABSTRACT FROM AUTHOR]

Candida albicans is an opportunistic pathogen and responsible for candidiasis. C. albicans readily forms biofilms on various biotic and abiotic surfaces, and these biofilms can cause local and systemic infections. C. albicans biofilms are more resistant than its free yeast to antifungal agents and less affected by host immune responses. Transition of yeast cells to hyphal cells is required for biofilm formation and is believed to be a crucial virulence factor. In this study, six components of ginger were investigated for antibiofilm and antivirulence activities against a fluconazole-resistant C. albicans strain. It was found 6-gingerol, 8-gingerol, and 6-shogaol effectively inhibited biofilm formation. In particular, 6-shogaol at 10 μg/ml significantly reduced C. albicans biofilm formation but had no effect on planktonic cell growth. Also, 6-gingerol and 6-shogaol inhibited hyphal growth in embedded colonies and free-living planktonic cells, and prevented cell aggregation. Furthermore, 6-gingerol and 6-shogaol reduced C. albicans virulence in a nematode infection model without causing toxicity at the tested concentrations. Transcriptomic analysis using RNA-seq and qRT-PCR showed 6-gingerol and 6-shogaol induced several transporters (CDR1, CDR2, and RTA3), but repressed the expressions of several hypha/biofilm related genes (ECE1 and HWP1), which supported observed phenotypic changes. These results highlight the antibiofilm and antivirulence activities of the ginger components, 6-gingerol and 6-shogaol, against a drug resistant C. albicans strain.

Daily exposure of humans to nanoparticles from edible plants is inevitable, but significant advances are required to determine whether edible plant nanoparticles are beneficial to our health. Additionally, strategies are needed to elucidate the molecular mechanisms underlying any beneficial effects. Here, as a proof of concept, we used a mouse model to show that orally given nanoparticles isolated from ginger extracts using a sucrose gradient centrifugation procedure resulted in protecting mice against alcohol-induced liver damage. The ginger-derived nanoparticle (GDN)–mediated activation of nuclear factor erythroid 2-related factor 2 (Nrf2) led to the expression of a group of liver detoxifying/antioxidant genes and inhibited the production of reactive oxygen species, which partially contributes to the liver protection. Using lipid knock-out and knock-in strategies, we further identified that shogaol in the GDN plays a role in the induction of Nrf2 in a TLR4/TRIF-dependent manner. Given the critical role of Nrf2 in modulating numerous cellular processes, including hepatocyte homeostasis, drug metabolism, antioxidant defenses, and cell-cycle progression of liver, this finding not only opens up a new avenue for investigating GDN as a means to protect against the development of liver-related diseases such as alcohol-induced liver damage but sheds light on studying the cellular and molecular mechanisms underlying interspecies communication in the liver via edible plant–derived nanoparticles.

Red ginger (Zingiber officinale var. Rubrum) is among the most widely consumed medicinal herbs in Indonesia. Ginger rhizome contains phenol compounds including gingerol and shogaol. 10-gingerol has been reported to exhibit the greatest anti-inflammatory and anti-oxidant activities compared with those of other gingerols. Pharmacokinetic studies on ginger have been reported, but there is a lack of such study on red ginger. The present work studied the pharmacokinetics of 10-gingerol and 6-shogaol in the plasma of healthy subjects treated with a single dose of red ginger suspension. Healthy subjects (n=19) were given a single dose of red ginger suspension (2 g/15 ml), and blood samples were taken at baseline (0 min), 30, 60, 90, 120, and 180 min. Analysis of 10-gingerol and 6-shogaol was performed by dissolving 200 µl of the subjects' plasma in 800 µl acetonitrile. The mixture was vortexed and centrifuged at 20,440 × g for 15 min at room temperature. The supernatant was filtered using Millipore membrane (pore size 0.2 µm) and injected into an RP-C18 column for liquid chromatography-mass spectrometry. A mixture of 0.1% (v/v) formic acid in water and acetonitrile (38:62) was used as the mobile phase. The maximum plasma concentration (Cmax) and time to reach Cmax of 10-gingerol and 6-shogaol were 160.49 ng/ml (38 min) and 453.40 ng/ml (30 min), respectively. The elimination half-lives were 336 and 149 min for 10-gingerol and 6-shogaol, respectively. Thus, 10-gingerol and 6-shogaol were absorbed after per oral single dose of red ginger suspension and could be quantified in the plasma of the healthy subjects. Additionally, the red ginger analytes exhibited relatively slow elimination half-lives. [ABSTRACT FROM AUTHOR]

Systemic studies dealing with 6-Shogaol (C17H24O3) safety in experimental animals is lacking. Therefore, the aim of current study was to determine the safe dose of 6- Shogaol that can be used in mice model and to assess the potential toxicity that may be initiated by the higher concentrations of this substance by means of clinical observations and evaluation of histopathological changes in liver, kidney and spleen. Sixty mice were divided into 6 groups; groups 1 and 2 served as negative and vehicle control respectively, whereas animals of groups 3, 4, 5 and 6 were treated with 10, 20, 40, and 100 mg/kg b.w. Shogaol respectively. The animals were investigated daily for any sign indicative for activity alterations and toxicity along with their body weight measurement throughout experiment for 14 days. At the end of the experiment, the animals were euthanized and the liver, spleen and kidney were collected for histopathological examination. The results obtained from this study showed that the 10, 20 and 40 mg/kg b.w. doses of Shogaol were safe compared to the 100 mg/kg b.w. dose which resulted in mild clinical activity alterations, reduction in body weight gain and histopathological changes, probably attributed to Shogoal toxicity, in 30% of the total mice treated by this dose. No mortality was observed in all groups. These results may provide a new insight into the safe doses of this phenolic constituent of ginger in experimental animals and open the way for more future studies related to its medicinal benefits. [ABSTRACT FROM AUTHOR]

Objective(s): This study aimed to investigate the effect of Shogaol on dextran sodium sulfate (DSS)- induced ulcerative colitis (UC) in mice compared to an immune-suppressant chemotherapeutic medicine, known as 6-thioguanine (6-TG). Materials and Methods: Thirty-six adult BALB/c mice were divided into six groups: group 1 (positive control): no DSS exposure and no treatment; group 2 (negative control): DSS exposure without treatment; group 3 (vehicle control): DSS exposure and olive oil treatment; group 4: DSS exposure and 0.3 mg/kg 6-TG treatment; group 5: DSS exposure and 20 mg/kg Shogaol treatment; and group 6: DSS exposure and 40 mg/kg Shogaol treatment. At day 16, the mice were euthanized and UC was evaluated according to colon length, histologically index score and expression scores of the epidermal growth factor receptor (EGFR). Results: The disease activity index (DAI) and histological index scores of mice treated with 40 mg/kg body weight (BW) Shogaol were approximately lower than the corresponding scores of mice treated with 6-TG. In addition, the rate of healing in the former mice was approximately 3 folds higher than that of the latter ones as indicated by the lack of EGFR expression in colonic glands and macrophages. Conclusion: These findings showed that the therapeutic effect of 40 mg/kg BW Shogaol could be better than 6-TG in the treatment of UC, and it may draw the attention regarding the priority of using this cheap plant-derived substance for treatment of the inflammatory bowel diseases because treatment with 6-TG is usually associated with adverse side effects. [ABSTRACT FROM AUTHOR]

Candida albicans is an opportunistic pathogen and responsible for candidiasis. C. albicans readily forms biofilms on various biotic and abiotic surfaces, and these biofilms can cause local and systemic infections. C. albicans biofilms are more resistant than its free yeast to antifungal agents and less affected by host immune responses. Transition of yeast cells to hyphal cells is required for biofilm formation and is believed to be a crucial virulence factor. In this study, six components of ginger were investigated for antibiofilm and antivirulence activities against a fluconazole-resistant C. albicans strain. It was found 6-gingerol, 8-gingerol, and 6-shogaol effectively inhibited biofilm formation. In particular, 6-shogaol at 10 μg/ml significantly reduced C. albicans biofilm formation but had no effect on planktonic cell growth. Also, 6-gingerol and 6-shogaol inhibited hyphal growth in embedded colonies and free-living planktonic cells, and prevented cell aggregation. Furthermore, 6-gingerol and 6-shogaol reduced C. albicans virulence in a nematode infection model without causing toxicity at the tested concentrations. Transcriptomic analysis using RNA-seq and qRT-PCR showed 6-gingerol and 6-shogaol induced several transporters (CDR1, CDR2 , and RTA3), but repressed the expressions of several hypha/biofilm related genes (ECE1 and HWP1), which supported observed phenotypic changes. These results highlight the antibiofilm and antivirulence activities of the ginger components, 6-gingerol and 6-shogaol, against a drug resistant C. albicans strain. [ABSTRACT FROM AUTHOR]

Gingerols and shogaols are compounds found in ginger (Zingiber officinale Roscoe); shogaols are found in lower concentration than gingerols but exhibit higher biological activities. This work studied the effects of different drying methods including open sun drying (OSD) solar tunnel drying (STD) and hot air drying (HAD) with various temperature on the formation of six main active compounds in ginger rhizomes, namely 6-, 8-, and 10-gingerols and 6-, 8-, and 10-shogaols, as well as essential oil content. Antioxidant and antimicrobial activity of dried ginger was also evaluated. High performance liquid chromatography (HPLC) analysis showed that after HAD with variable temperature (120, 150 and 180 °C), contents of 6-, 8-, and 10-gingerols decreased, while contents of 6-, 8-, and 10-shogaol increased. High formation of 6-, 8-, and 10-shogaol contents were observed in HAD (at 150 °C for 6 h) followed by STD and OSD, respectively. OSD exhibited high content of essential oil followed by STD and HAD method. Ginger-treated with HAD exhibited the highest DPPH (IC50 of 57.8 mg/g DW) and FRAP (493.8 µM of Fe(II)/g DM) activity, compared to STD and OSD method. HAD ginger exhibited potent antimicrobial activity with lower minimum inhibition concentration (MIC) value against bacteria strains followed by STD and OSD, respectively. Ginger extracts showed more potent antimicrobial activity against Gram positive bacteria than Gram negative bacteria strains. Result of this study confirmed that conversion of gingerols to shogaols was significantly affected by different drying temperature and time. HAD at 150 °C for 6 h, provides a method for enhancing shogaols content in ginger rhizomes with improving antioxidant and antimicrobial activities. [ABSTRACT FROM AUTHOR]

Nine new gingerols, including three 6-oxo-shogaol derivatives [(Z)-6-oxo-[6]-shogaol (1), (Z)-6-oxo-[8]-shogaol (2), (Z)-6-oxo-[10]-shogaol (3)], one 6-oxoparadol derivative [6-oxo-[6]-paradol (4)], one isoshogaol derivative [(E)-[4]-isoshogaol (5)], and four paradoldiene derivatives [(4E,6Z)-[4]-paradoldiene (8), (4E,6E)-[6]-paradoldiene (9), (4E,6E)-[8]-paradoldiene (10), (4E,6Z)-[8]-paradoldiene (11)], together with eight known analogues, were isolated from the rhizoma of Zingiber officinale. Their structures were elucidated on the basis of spectroscopic data. It was noted that the isolation of 6-oxo-shogaol derivatives represents the first report of gingerols containing one 1,4-enedione motif. Their structures were elucidated on the basis of spectroscopic and HRESIMS data. All the new compounds were evaluated for their cytotoxic activities against human cancer cells (MCF-7, HepG-2, KYSE-150). [ABSTRACT FROM AUTHOR]

Nuclear factor-kappaB (NF-κB) and activator protein 1 (AP-1) is a major transcription factor which regulates many biological and pathological processes such as inflammation and cell proliferation, which are major implicates in cancer progression. [6]-Shogaol ([6]-SHO) is a major constituent of ginger, exhibits various biological properties such as anti-oxidants, anti-inflammation and anti-tumor. Recently, we proven that [6]-SHO prevents oral squamous cell carcinoma by activating proapoptotic factors in in vitro and in vivo experimental model. However, the preventive efficacy of [6]-SHO in 7,12-dimethylbenz[ a ]anthracene (DMBA) induced hamster buccal pouch carcinogenesis (HBP) has not been fully elucidated, so far. Hence, we aimed to investigate the effect of [6]-SHO on inflammation and cell proliferation by inhibiting the translocation of NF-κB and AP-1 in DMBA induced HBP carcinogenesis. In this study, we observed upregulation of inflammatory markers (COX-2, iNOS, TNF-α, interleukin-1 and -6), cell proliferative markers (Cyclin D1, PCNA and Ki-67) and aberrant activation of NF-κB, AP-1, IKKβ, c-jun, c-fos and decreased IκB-α in DMBA induced hamsters. Conversely, oral administration of [6]-SHO strongly inhibited constitutive phosphorylation and degradation of IκB and inhibit phosphorylation of c-jun, c-fos, resulting in inhibition of nuclear translocation of NF-κBp65 and AP-1. Thus, inhibition of NF-κB and AP-1 activation by [6]-SHO attenuates inflammation and cell proliferative response in DMBA induced hamsters. Our finding suggested that [6]-SHO is a novel functional agent capable of preventing DMBA induced inflammation and cell proliferation associated tumorigenesis by modulating multiple signalling molecules. [ABSTRACT FROM AUTHOR]

The prevalence of obesity has increased rapidly worldwide. Obesity is characterized by excessive adipose tissue in the body, which is related to hyperplasia and hypertrophy in adipocytes. Ginger (Zingiber officinale Roscoe) is a medicinal plant that possesses an anti-obesogenic effect mostly attributed to gingerols, the most abundant bioactive compounds in ginger. The anti-adipogenic and lipolytic effects of these phenols have been shown when investigated individually. Therefore, the present study aimed to evaluate the lipolytic and anti-adipogenic activity of a mix of the main ginger phenols 6-gingerol, 8-gingerol, 10-gingerol, 6-shogaol, 8-shogaol and 10-shogaol on the 3T3-L1 cell line. A total of four study groups were designed: Negative control (3T3-L1 preadipocytes); positive control (mature 3T3-L1 adipocytes); phenols-pre (3T3-L1 cells stimulated with the phenols mix during adipogenic differentiation); and phenols-post (mature 3T3-L1 adipocytes stimulated with the phenols mix). MTT viability cell assay and Oil Red O staining were performed. Glycerol concentration supernatants were determined using the VITROS 350 Chemistry System. Expression of mRNA was measured using qPCR. The treatment with a 2 µg/ml ginger phenol dose reduced the lipid content by 45.52±7.8 and 35.95±0.76% in the phenols-pre and -post group, respectively, compared with that in the positive control group. The phenols-post group presented a higher glycerol concentration in the supernatant compared with that in the positive control and the phenols-pre groups. The mRNA expression levels of CCAAT/enhancer-binding protein alpha, peroxisome proliferator activated receptor-γ, fatty acid-binding protein 4 and fatty acid synthase were higher in the phenols-pre and lower in the phenols-post groups, compared with those in the positive control group. To the best of our knowledge, the current study demonstrated for the first time the anti-adipogenic and lipolytic effects of a mix of the main bioactive compounds found in ginger, and it also established the basis to use this mix of phenols in in vivo studies and clinical trials. [ABSTRACT FROM AUTHOR]

Inflammation is the natural way our bodies respond to infection or injury. However, if it fails to subside, inflammation can damage the body and contribute to several illnesses. Although non-resolving inflammation is not the primary factor, it is still considered to significantly contribute to several diseases such as chronic obstructive pulmonary disease (COPD), asthma, inflammatory bowel disease, rheumatoid arthritis, cancer, neurodegenerative disease, and so on. Phosphodiesterase 4 inhibitor is an established treatment to treat inflammation worldwide. However, the non-selective PDE4 was reported to exhibit adverse reactions such as nausea and diarrhoea. This study aims to identify compounds with higher selectivity for PDE4B over PDE4D and determine their binding mode and interaction through molecular docking. In this present study, three x-ray crystall structures representing PDE4B and PDE4D each were downloaded from Protein Data Bank and redock with their co-crytallized ligand to calculate the RMSD as the validation step for the docking procedure. The protein structures with the lowest RMSD (PDB ID: 3W5E for PDE4B and PDB ID: 3G58 for PDE4D) were docked with gingerols and shogaols. Binding energies were obtained and the ratios between the binding energy of PDE4B and PDE4D were calculated. 10-gingerol had been found to have the lowest binding energy and the highest selectivity of PDE4B compared to PDE4D among the compounds. Thus, the binding interaction was further investigated, and found that 10-gingerol form a hydrogen bond with invariant glutamine residue which is GLN 443 in PDE4B and GLN 535 in PDE4D. Besides, 10-gingerol also formed hydrophobic bonds between PHE 446 in PDE4B and PHE 538 in PDE4D while with isoleucine and phenylalanine residues (ILE410 and PHE414 in PDE4B and ILE502 and PHE506) on the other side. 10-gingerol also showed hydrophobic interaction with non-conserved residues in CR3 region, which is with LEU502 in PDE4B. This interaction was absent with the CR3 region in PDE4D which in turn determined the PDE4B selectivity of 10-gingerol. These results showed that 10-gingerol is a potential candidate as a selective PDE4B inhibitor as a new anti-inflammatory drug. [ABSTRACT FROM AUTHOR]