Rheological properties, biochemical changes, and potential health benefits of dehulled and defatted industrial hempseeds after fermentation.

Dehulled hempseed (DHS), fermented dehulled hempseed (FDHS), hempseed cake (HSC), and fermented HSC (FHSC) were examined for their phytochemical composition, health benefits, and rheological characteristics. At 500 µg/mL concentration, DHS, FDHS, HSC, and FHSC extracts exhibited the ability to inhibit DPPH radicals, with 32.46 %, 47.35 %, 33.85 %, and 47.41 %, respectively. Similarly, they demonstrated potential to scavenge ABTS radicals by 13.7 %, 27.87 %, 14.40 % and 25.70 %, respectively. For lipase inhibition activity, FDHS (72.92 %) and FDHS (85.89 %) outperformed DHS (52.94 %) and HSC (43.08 %). Furthermore, FHSC enhanced the survival and reduced fat accumulation in glucose-supplemented Caenorhabditis elegans. We used HPLC and UHPLC-ESI-QTOF-MS for metabolite analysis, quantifying eight polyphenols using HPLC and identifying thirty-four metabolites with UHPLC-ESI-QTOF-MS. Generally, metabolomics indicated an improved metabolite profile after fermentation. Fermentation also showed impact on rheological characteristics, modifying viscosity, loss modulus, and storage modulus. These findings collectively demonstrate the ability of fermentation in enhancing overall value of hempseed.

Moracin E and M isolated from Morus alba Linné induced the skeletal muscle cell proliferation via PI3K-Akt-mTOR signaling pathway.

Twigs of Morus alba have been used in traditional medicine to treat muscle-related symptoms such as aches, numbness, and stiffness. Despite its clinical use in traditional medicine, its active compounds and mode of action have not yet been investigated. Therefore, we aimed to isolate the compounds from the twigs of M. alba and deduce active compounds, key gene targets, and mechanism of action against sarcopenia using network pharmacology analysis. Using various isolation techniques and spectroscopic methods, 43 phytochemicals, including 3 new flavonoids, were isolated and performed network pharmacology analysis. According to the computational-assistant analysis, 28 compounds, 9 genes, and the PI3K-Akt-mTOR signaling pathway were deduced as expected active compounds (EAC), key targets, and the main signaling pathway. To verify the predicted results, the cell proliferation activities of the EAC were evaluated. Especially, moracin E and M significantly increased by 130% (p < 0.001) and 57% (p < 0.05), respectively, which have more than 2- and 1.5-fold stronger effects compared to the control. Furthermore, both increased the expression level of proteins involved in the PI3K-Akt-mTOR signaling pathway and myogenic proteins, including myogenin and MyoD. This study demonstrated that moracin E and M exhibit cell proliferative effects on skeletal muscle cells through the PI3K-Akt-mTOR signaling pathway.

Three Undescribed Iridoid Derivatives Isolated from the Fruits of Vitex trifolia with Their Cytotoxic and Antimicrobial Activities.

Vitex trifolia L. is a medicinal plant and widely distributed in the northern mountainous areas of Vietnam. Phytochemical study on the fruits of this plant led to the isolation of nine iridoid derivatives (1-9) including three undescribed compounds (1-3). Their structures were elucidated to be 3''-hydroxyscrophuloside A1 (1), 3''-hydroxycallicoside D (2), 2'-p-hydroxybenzoylaucubin (3), 6'-p-hydroxybenzoylmussaenosidic acid (4), nishindaside (5), agnuside (6), 10-O-vanilloylaucubin (7), 6'-O-p-hydroxybenzoyl-gardoside (8), and buddlejoside B (9) based on extensive analyses of HR-ESI-MS, 1D and 2D NMR spectra. Compounds 1, 2, 4, and 8 significantly posessed anti-barterial activity against Enterococcus faecalis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa strains with MIC values in range of 16-64 µg/mL. At concentration of 20 µM, compounds 1-9 did not show cytotoxic effects against human lung cancer cells (PC9).

Phytochemical profiling, in vitro antioxidants, and antidiabetic efficacy of ethyl acetate fraction of Lespedeza cuneata on streptozotocin-induced diabetic rats.

In the recent past, phytomolecules are exponentially applied in discovering the antidiabetic drug due to less adverse effects. This work screened the active solvent fraction of Lespedeza cuneata based on the phytochemical, enzyme inhibition, and antioxidant properties. The antioxidant efficacy of the different fractions of the L. cuneata was assessed by 1,1-diphenyl-2-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), ferric reducing power, hydrogen peroxide, and hydroxyl radical scavenging assays. The digestive enzyme (α-amylase and α-glucosidase) inhibitory activity was also evaluated. The phytochemical composition of ethyl acetate fraction of L. cuneata (Lc-EAF) was studied by UHPLC-QTOF-MS/MS. The effect of Lc-EAF treatments on glucose uptake was studied in insulin resistance HepG2 cells (IR-HepG2). Further, the antidiabetic effect of Lc-EAF in streptozotocin (STZ)-induced diabetic mice were demonstrated. Ethyl acetate, hexane, and methanol fractions of the L. cuneata showed notable antioxidant, α-amylase, and α-glucosidase inhibitory properties. Among the fractions, Lc-EAF was found to be the most potent. The Lc-EAF exhibited an IC50 of 205.32 ± 23.47 µg/mL and 105.32 ± 13.93 µg/mL for α-amylase and α-glucosidase inhibition, respectively. In addition, 75 µg/mL of Lc-EAF exposure enhanced glucose uptake (68.23%) in IR-HepG2 cells. In vivo study indicated that treatment of Lc-EAF (100 mg/kg b.wt) maintained the blood glucose level through reduced insulin level while improving the lipid profile, hepatic, and renal markers. These findings suggest that Lc-EAF could be considered a prominent source for antidiabetic, anti-hyperlipidemic, and anti-ROS potentials.

Anti-inflammatory activity of Echinosophora koreensis nakai root extract in lipopolysaccharides-stimulated RAW 264.7 cells and carrageenan-induced mouse paw edema model.

ETHNOPHARMACOLOGICAL RELEVANCE: Echinosophora koreensis Nakai is an endemic plant species distributed in a limited area within the Korean province of Gangwon, including the Yanggu-gun, Inje-gun, Cheorwon-gun, Chuncheon-si, and Hongcheon-gun counties. It is used in traditional medicine to treat various disorders, such as fever, skin diseases, diuresis, and neuralgia. MATERIALS AND METHODS: This study demonstrated the effects of E. koreensis Nakai root extract (EKRE) on lipopolysaccharide (LPS)-induced inflammatory responses in vitro and in vivo. Cell viability was assessed through a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Nitric oxide (NO) production was measured using Griess reagent. Interleukin (IL)-6 and tumor necrosis factor (TNF) levels were assessed using enzyme-linked immunosorbent assays. Inducible nitric oxide synthase (iNOS), nuclear factor kappa-B (NF-κB), and mitogen-activated protein kinase (MAPK) expression were assessed using Western blot analysis. To examine the effects of EKRE in vivo, it was administered orally at doses of 50 or 200 mg/kg for 3 days in mice. Edema in the paws was induced through λ-carrageenan injection and measured hourly for up to 5 h using calipers. RESULTS: EKRE markedly suppressed LPS-generated NO, IL-6, and iNOS production in RAW 264.7 cells. Moreover, it suppressed the activation of the NF-κB and MAPK in LPS-stimulated cells. Furthermore, EKRE significantly inhibited carrageenan-induced edema in mouse paws. There were no significant differences in IL-6 and TNF production in paw tissue harvested from mice, but levels decreased at high EKRE concentrations (200 mg/kg). CONCLUSION: The results of this study provided validation for EKRE-induced inhibition of inflammatory responses in vitro and in vivo. This research suggested that EKRE is a promising treatment for inflammatory disorders.

Anti-Inflammatory Activity of 4-((1R,2R)-3-Hydroxy-1-(4-hydroxyphenyl)-1-methoxypropan-2-yl)-2-methoxyphenol Isolated from Juglans mandshurica Maxim. in LPS-Stimulated RAW 264.7 Macrophages and Zebrafish Larvae Model.

Juglans mandshurica Maxim., a traditional folk medicinal plant, is widely distributed in Korea and China. In our previous study, we isolated a new phenylpropanoid compound, 4-((1R,2R)-3-hydroxy-1-(4-hydroxyphenyl)-1-methoxypropan-2-yl)-2-methoxyphenol (HHMP), from J. mandshurica. In the present study, we evaluated the anti-inflammatory activity of HHMP on lipopolysaccharide (LPS)-stimulated RAW 264.7 cells and zebrafish larvae. HHMP significantly inhibited LPS-induced nitric oxide (NO) and prostaglandin E2 production in a dose-dependent manner. Moreover, HHMP treatment considerably suppressed LPS-induced expression of inducible nitric oxide synthase and cyclooxygenase-2. We also demonstrated the mechanisms of HHMP inhibition of inflammatory responses in LPS-stimulated RAW 264.7 cells via Western blot analysis and immunofluorescence staining. Furthermore, HHMP significantly inhibited NO production in LPS-stimulated zebrafish larvae. Consequently, we established that HHMP significantly inhibited the LPS-induced activation of NF-κB and MAPK and the nuclear translocation of p65 in RAW 264.7 cells. Taken together, our findings demonstrate the effect of HHMP on LPS-induced inflammatory responses in vitro and in vivo, suggesting its potential to be used as a natural anti-inflammatory agent.

Chemical composition, antioxidant, and anti-diabetic activities of ethyl acetate fraction of Stachys riederi var. japonica (Miq.) in streptozotocin-induced type 2 diabetic mice.

This work analysed the chemical composition, antioxidant, and enzyme inhibitory activities of solvent extract (SJ-ME) and fractions (SJ-HF, SJ-EAF, and SJ-MF) of the Stachys riederi var. japonica (Miq.) (SJ). Furthermore, the effect of SJ-EAF in STZ induced type 2 diabetic mice was examined. Among the samples, SJ-EAF exhibited a lower IC50 concentration of 64.2 ± 0.48 µg/mL for DPPH and 82.6 ± 0.09 µg/mL for ABTS+. The SJ-EAF concentration of 2.89 ± 0.03 µg and 2.27 ± 0.98 µg was equivalent to 1 µg of acarbose mediated enzyme inhibitory effect against α-amylase and α -glucosidase, respectively. The SJ-EAF did not show cytotoxicity (<80%) to NIH3T3 nor HepG2 cells but enhanced the glucose uptake in the IR-HepG2. LC-MS/MS of SJ-EAF showed the presence of a total of 16 compounds. Among the identified compounds, rosmarinic acid, caffeic acid, oleanolic acid, and ursolic acid showed high catalytic activity of α-amylase and α-glucosidase. The treatments of SJ-EAF restored the level of blood glucose, body weight, insulin, HDL and mRNA level of IRS1, GLUT2, GLUT4 and Akt whereas it reduced the excess elevation of total cholesterol, total triglycerides, LDL, AST, ALT, ALP, BUN, and creatinine in STZ induced diabetic mice. Overall, the present study concluded that the SJ-EAF exhibited promising antidiabetic activity.

Protective Effect of Brassica napus L. Hydrosols against Inflammation Response in RAW 264.7 Cells.

OBJECTIVE: To demonstrate the anti-inflammatory activity of Brassica napus L. hydrosols (BNH) in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. METHODS: Composition analysis of BNH was conducted via gas chromatography-mass spectrometry after BNH were extracted. The nitric oxide (NO) production was measured using the Griess assay. Prostaglandin E2 (PGE2) production was evaluated with enzyme-linked immunosorbent assay. The effects of BNH on LPS-induced pro-inflammatory enzymes including inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) were evaluated using Western blot analysis. Furthermore, phosphorylation of nuclear factor-kappa B (NF-κB) and nuclear translocation of NF-κB p65 were evaluated with Western blot analysis and immunofluorescence staining, respectively. RESULTS: Compared with LPS-stimulated cells, BNH markedly decreased the generation of NO and PGE2 in LPS-stimulated RAW 264.7 cells (P<0.01 or P<0.05). Moreover, BNH inhibited protein levels of iNOS and COX-2 (P<0.01). Phosphorylation of NF-κB and nuclear translocation of NF-κB p65 was significantly inhibited by BNH (P<0.01 or P<0.05). CONCLUSION: The anti-inflammatory activities of BNH were mediated via blockage of the NF-κB signaling pathways in LPS-stimulated RAW 264.7 cells.

Phytochemicals in Chinese Chive (Allium tuberosum) Induce the Skeletal Muscle Cell Proliferation via PI3K/Akt/mTOR and Smad Pathways in C2C12 Cells.

Chinese chive (Allium tuberosum) is a medicinal food that is cultivated and consumed mainly in Asian countries. Its various phytochemicals and physiological effects have been reported, but only a few phytochemicals are available for skeletal muscle cell proliferation. Herein, we isolated a new compound, kaempferol-3-O-(6″-feruloyl)-sophoroside (1), along with one known flavonoid glycoside (2) and six amino acid (3-8) compounds from the water-soluble fraction of the shoot of the Chinese chive. The isolated compounds were identified using extensive spectroscopic methods, including 1D and 2D NMR, and evaluated for their proliferation activity on skeletal muscle cells. Among the tested compounds, newly isolated flavonoid (1) and 5-aminouridine (7) up-regulated PI3K/Akt/mTOR pathways, which implies a positive effect on skeletal muscle growth and differentiation. In particular, compound 1 down-regulated the Smad pathways, which are negative regulators of skeletal muscle growth. Collectively, we suggest that major constituents of Chinese chive, flavonoids and amino acids, might be used in dietary supplements that aid skeletal muscle growth.

The Chemical Constituents from Fruits of Catalpa bignonioides Walt. and Their α-Glucosidase Inhibitory Activity and Insulin Secretion Effect.

Catalpa pod has been used in traditional medicine for the treatment of diabetes mellitus in South America. Studies on the constituents of Catalpa species have shown that it is rich in iridoids. In the present study, three previously undescribed compounds (2-4), including two secoiridoid derivatives along with twelve known compounds, were isolated from the fruits of Catalpa bignonioides Walt. In addition, fully assigned 13C-NMR of 5,6-dihydroxy-7,4'-dimethoxyflavone-6-O-sophoroside (1) is reported for the first time in the present study. The structures of compounds were determined on the basis of extensive spectroscopic methods, including UV, IR, 1D, and 2D NMR, mass spectroscopy, and CD spectroscopic data. All the isolated compounds were evaluated for α-glucosidase inhibitory activity. Among the tested compounds, compounds 2, 3, and 9 exhibited significant inhibitory activity against α-glucosidase enzyme assay. Meanwhile, the effect of compounds 2, 3, and 9 on glucose-stimulated insulin secretion (GSIS) was measured using pancreatic ß-cells. Compounds 2, 3, and 9 exhibited non-cytotoxicity-stimulated insulin secretion in INS-1 cells. The expression levels of proteins associated with ß-cell function and insulin secretion such as phosphorylation of total insulin receptor substrate-2 (IRS-2), phosphatidylinositol 3-kinase (PI3K), Akt, activated pancreatic duodenal homeobox-1 (PDX-1), and peroxisome proliferator-activated receptor-γ (PPAR-γ) were increased in INS-1 cells after treatment with compounds 2, 3, and 9. The findings of the present study could provide a scientific warrant for their application as a potential antidiabetic agent.

Ethyl Acetate Fraction of Helianthus tuberosus L. Induces Anti-Diabetic, and Wound-Healing Activities in Insulin-Resistant Human Liver Cancer and Mouse Fibroblast Cells.

Traditional, complementary, and integrative medicine are globally accepted alternative methods for the treatment of diabetes mellitus (DM). However, the mechanism of anti-diabetic effects of Helianthus tuberosus L. remains unproven. In the present study, antioxidant and anti-diabetic activity of the tubers of H. tuberosus were studied in detail. Methanolic extracts of H. tuberosus tubers were subjected to solvent fractionation method by increasing the polarity of the solvent using n-hexane, and ethyl acetate. The obtained methanol extracts and its fractions were subjected to free radical scavenging activity (DPPH and ABTS assay) and in vitro enzyme (α-amylase and α-glucosidase) inhibition assay. Moreover, glucose uptake in insulin-resistant HepG2 cell line was analyzed. The preliminary phytochemical analysis confirmed the presence of phenolic and flavonoid compounds in the active fraction. The radical scavenging and in vitro diabetic related enzyme inhibitory activities were found to be dose dependent. The maximum ABTS+ and DPPH scavenging activity was documented in ethyl acetate fraction of the H. tuberosus followed by methanol extract, hexane fraction, and methanol fraction. We also found that H. tuberosus showed a less toxicity in mouse fibroblast cells and enhance the glucose uptake in insulin-resistant HepG2 cells. Besides, the ethyl acetate fraction of the H. tuberosus analyzed by UPLC-QTOF-MS-MS and GC/MS revealed the presence of phenolic compounds such as neochlorogenic acid, chlorogenic acid, caffeic acid, 5-O-(4-coumaroyl)-quinic acid, feruloylquinic acid, caffeoylquinic acid, isoxazolidine, salicylic acid ß-D-glucoside, dicaffeoylquinic acid isomers, salvianolic acid derivative isomers, and 1,4 dicaffeoylquinic acid etc. Among the identified phytochemicals, six were chosen for molecular docking study to explore their its inhibitory interactions with α-amylase and α-glucosidase. Taken together, the findings of the present study suggested that phytocompounds of EAF were responsible for the significant in vitro antioxidant, wound-healing, and anti-diabetic activities.

Isolation of amylase regulators from the leaves of Ixeridium dentatum.

Two new compounds, one sesquiterpene lactone (1) and one phenylethanoid tautomer (2), together with eleven known compounds (3-13) were isolated from the leaves of Ixeridium dentatum. Their structures were determined by extensive spectroscopic methods, including 1D-, 2D-NMR, and mass spectrometry. All compounds were evaluated for their amylase secretion activity in human salivary gland cells after treatment in 40 mM of high glucose. All compounds showed increased amylase secretion activity. Moreover, previously undescribed compounds (1-2), luteolin 7-O-ß-D-glucopyranoside (10), quercimeritrin (11), and quercetin 3-O-ß-D-xylopyranoside (13) exhibited significant amylase activity, which is comparable to the positive control.

1-Cinnamoyltrichilinin from Melia azedarach Causes Apoptosis through the p38 MAPK Pathway in HL-60 Human Leukemia Cells.

Acute myeloid leukemia (AML) is an aggressive type of human leukemia with a low survival rate, and its complete remission remains challenging. Although chemotherapy is the first-line treatment of AML, it exerts toxicity in noncancerous cells when used in high doses, thus necessitating the development of novel compounds with a high therapeutic window. This study aimed to investigate the anticancer effects of several compounds derived from the fruits of Melia azedarach (a tree with medicinal properties). Among them, 1-cinnamoyltrichilinin (CT) was found to strongly suppress the viability of HL-60 human leukemia cells. CT treatment induced apoptosis and increased nuclear fragmentation and fractional DNA content in HL-60 cells in a dose-dependent manner. CT induced phosphorylation of p38 mitogen-activated protein kinases (p38), though not of c-Jun N-terminal kinase (JNK) and extracellular signal-regulated kinase (ERK), and activated Bcl-2 family proteins towards the proapoptosis and cleavage of caspase-3 and poly (ADP-ribose) polymerase. Both CT-mediated apoptosis and apoptotic protein expression were reversed by treatment with the p38 inhibitor, thereby indicating the p38 pathway to be critical in CT-stimulated apoptosis. The results collectively indicated CT to suppress HL-60 survival by activating the p38 pathway and inducing apoptosis, hence being a novel potential therapeutic agent for AML.

Five New Pregnane Glycosides from Gymnema sylvestre and Their α-Glucosidase and α-Amylase Inhibitory Activities.

Gymnema sylvestre, a medicinal plant, has been used in Indian ayurvedic traditional medicine for the treatment of diabetes. Phytochemical investigation of Gymnema sylvestre led to the isolation of five new pregnane glycosides, gymsylosides A-E (1-5) and four known oleanane saponins, 3ß-O-ß-D-glucopyranosyl (1→6)-ß-D-glucopyranosyl oleanolic acid 28-O-ß-D-glucopyranosyl ester (6), gymnemoside-W1 (7), 3ß-O-ß-D-xylopyranosyl-(1→6)-ß-D- glucopyranosyl-(1→6)-ß-D-glucopyranosyl oleanolic acid 28-O-ß-D-glucopyranosyl ester (8), and alternoside XIX (9). Their structures were identified based on spectroscopic evidence and comparison with those reported in the literature. All compounds were evaluated for their α-glucosidase and α-amylase inhibitory activities. Compounds 2-4 showed significant α-amylase inhibitory activity, with IC50 values ranging from 113.0 to 176.2 µM.

Chemical components from the twigs of Caesalpinia latisiliqua and their antiviral activity.

Three new compounds, (3S)-dihydrobonducellin 8-O-ß-D-glucopyranoside (1), 3',5'-dimethoxy-jezonolid (2), and latisilinoid (3), along with 16 known compounds, were isolated from the twigs of Caesalpinia latisiliqua (Leguminosae). The known compounds were identified as flavonoids, stilbenes, and phenolics as determined by extensive spectroscopic methods, including 1D and 2D NMR. All the isolated compounds were evaluated for their antiviral activity in HRV1B-, CVB3-, and EV71-infected cells. Among the tested compounds, three flavonoids (4-6) and two stilbenes (12 and 14) exhibited significant antiviral activity. This is the first phytochemical investigation of C. latisiliqua twigs.

Chemical constituents from the fruits of Schisandra sphenanthera and their cytotoxicity activity

Abstract Schisandra sphenanthera Rehder & E.H. Wilson, Schisandraceae, is well known as a type of traditional medicine for the treatment of hepatitis, diarrhea and insomnia in Asia. It was also reported to have antiviral and anti-HIV activities. Using various chromatographic resins and isolation techniques, a new lignan (1), erythro-4-(3,4-dimethoxyphenyl)-4-hydroxy-3-methylbutan-2yl-3,4-dimethoxybenzoate, along with fifteen known compounds, were isolated from fruits of S. sphenanthera. The structures of the compounds were identified by extensive spectroscopic and spectrometric methods including 1D and 2D NMR and MS data. All the isolated compounds were evaluated for their cytotoxicity activity against Hela, HepG2 and HCT-116 cells. Among them, compound schisanlactone C showed significant cytotoxicity activity.

Stilbenes contribute to the anticancer effects of Rheum undulatum L. through activation of apoptosis.

Rheum undulatum L. (R. undulatum) is a medicinal plant used for the treatment of inflammatory diseases in East Asian countries. Numerous stilbenes isolated from R. undulatum have been revealed to possess anticancer effects. The aim of the present study was to evaluate the effect of extracts and compounds isolated from R. undulatum on human gastric cancer cell viability and to elucidate their molecular mechanism of action on the apoptosis pathway. The results demonstrated that aloe-emodin and chrysophanol 1-O-ß-D-glucopyranoside, isolated from the methanolic extract of dried rhizomes of R. undulatum, exhibited anti-proliferative effects on the human gastric carcinoma cell line AGS, with IC50 values of 84.66±0.44 and 68.28±0.29 µM, respectively. The percentage of apoptotic cells increased significantly following treatment with each compound at a concentration of 100 µM, compared with that in the non-treated group in the image-based cytometry assay. Western blot analysis revealed that these compounds activated the caspase cascade and inhibited B-cell lymphoma-2, an anti-apoptotic protein.

A chemical compound from fruit extract of Juglans mandshurica inhibits melanogenesis through p-ERK-associated MITF degradation.

BACKGROUND: Trials for regulation of abnormal hyperpigmentation from the use of natural products have been going on for years. Leaf and root extracts from Juglans mandshurica are reported to function as antioxidants and to suppress allergic dermatitis. However, studies evaluating its fruit extract and the chemical compounds from the fruit extract are lacking in dermatology fields, including melanogenesis. PURPOSE: The aim of this study is to understand the effect of the fruit extract from J. mandshurica on pigmentation and to search for specific chemical compounds that affect melanogenesis. METHODS: After screening out any anti-melanotic effects of the fruit extract from J. mandshurica in B16F10 melanoma cells, three major phenolic compounds isolated from the fruit extract were tested by western blot analysis for expression of microphthalmia-associated transcription factor (MITF) and tyrosinase. Their effect on B16F10 melanoma cells with regard to melanogenesis was also confirmed in primary human epidermal melanocytes (PHEMs). PD98059 was tested to observe the compounds' signaling role in the extracellular signal-regulated protein kinase (ERK)-pathway. RESULTS: Fruit extract from J. mandshurica showed anti-melanotic effects in B16F10 melanoma cells. After chemical compounds were isolated from the fruit extracts, three phenolic compounds were evaluated for anti-melanotic effects. 2-[4-(3-hydroxypropyl)-2-methoxyphenoxy]-1,3-propanediol (compound 1) showed the highest suppression effect among the three compounds. In B16F10 melanoma cells and PHEMs, reduced melanin contents were observed after treatment with the compound (1). Experiments using a blocker of ERK showed that the inhibitory effect of the compound (1) on melanogenesis was dependent on ERK-associated MITF degradation. CONCLUSION: A chemical constituent of Juglans mandshurica Maxim. induces an inhibitory mechanism to melanogenesis. It has the potential to become a whitening agent in the medical field, though this requires further clinical investigation.

A new naphthoquinone analogue and antiviral constituents from the root of Rhinacanthus nasutus.

Rhinacanthus nasutus (L.) Kurz (Acanthaceae) is known as traditional medicine for the treatment of fungal and herpes virus infections. A new naphthoquinone racemate, rhinacasutone (1) together with seven known compounds, rhinacanthone (2), rhinacanthins C, D, N, Q, and E (3-7), and heliobuphthalmin (8) were isolated from root of R. nasutus. Their structures were determined on the basis of extensive spectroscopic methods, including 1D-, 2D-NMR and MS data. All the isolated compounds were tested for their antiviral activities against PR8, HRV1B, and CVB3-infected vero cells. Compounds 3-6 exhibited significant antiviral activities with the IC50 value ranging from 0.03 to 23.7 µM in all three infections.

Cycloartane-type triterpenoid derivatives and a flavonoid glycoside from the burs of Castanea crenata.

Five undescribed cycloartane-type triterpenoids, which were isolated for the first time from the genus, and a flavonoid glycoside together with 11 known compounds were isolated from the burs of Castanea crenata. The structures were elucidated based on the spectroscopic analysis of 1D and 2D NMR and MS data. All isolated compounds were evaluated for antiviral activities against HRV1B-, CVB3-, and PR8-infected cells. Most kaempferol derivatives showed statistically significant antiviral activities against HRV1B-infected cells. Among the tested compounds, kaempferol-3-O-[2″,6″-di-O-Z-p-coumaroyl]-ß-d-glucopyranoside exhibited the most consistent and effective antiviral activities against all infections.