The impact of varying doses of moringa leaf methanolic extract supplementation in the cryopreservation media on sperm quality, oxidants, and antioxidant capacity of frozen-thawed ram sperm.

To increase rams' post-thaw semen quality following cryopreservation, this study used enriched Tris-based diluent with varying amounts of moringa leaf methanolic extract (MLME). The antioxidant activity, total phenolic, and total flavonoid content were all assessed in MLME. The sperm of five healthy Awassi rams were collected, divided into 4 equal aliquots, and diluted [1:5; (v/v)] in Tris-citrate-glucose extender supplemented with 0.48, 0.56, and 0.64 mg MLME/ml or without MLME supplementation (control). The percentages of sperm total motility (STM, %), sperm progressive motility (SPM, %) and viability (V, %), abnormal morphology (AM, %), membrane functional integrity (MFI, %), and acrosome integrity (AI %) were measured. Malondialdehyde (MDA), nitric oxide (NO), ascorbic acid (AA), superoxide dismutase (SOD), glutathione peroxidase (GPx), total cholesterol (TC), low-density lipoproteins (LDL), lactate dehydrogenase (LDH), alkaline phosphatase (ALP), zinc (Zn), and copper (Cu) were measured. The total phenolic gallic acid and flavonoid catechin (equivalent) contents were 19.78 mg/g and 11.94 mg/g, respectively. 2,2-Diphenyl-1-picrylhydrazyl (34.37 mM TE/g) and 2,2'-azino-bis/3-ethylbenzothiazoline-6-sulfonic acid (53.47 mM TE/g) were found in MLME. MLME had a 64.59 mM TE/g ferric-reducing power. In comparison to control, the addition of 0.64 mg/ml MLME to Tris-based extender resulted in the highest (P < 0.001) STM (55.22 ± 0.98), SPM (45.41 ± .70), SV (60.01 ± 1.05), MFI (75.23 ± 0.77), and AI (73.13 ± 0.72) and the lowest (P < 0.001) AM (21.34 ± 0.72) values. In comparison to the control, the addition of 0.56 mg/ml semen extender resulted in lower STM, SPM, SV, MFI, and AI with higher AM percentages. MDA (P = 0.03), NO (P = 0.012), CHO (P = 0.0001), and LDL (P = 0.004) were reduced by 0.64 mg/ml MLME, while AA (P = 0.017) and SOD (P = 0.0001) were elevated. In conclusion, the highest copper (P = 0.006) and lowest zinc concentrations in MLME (0.48 mg/ml extender) deteriorated the post-thaw semen quality, prompting us to suggest the addition of 0.64 mg MLME to rams' Tris-based semen extender.

Efficacy of Sishen Wan on dinitrobenzene sulfonic acid-induced ulcerative colitis and its effect on toll-like receptor 2/interleukin-1 receptor-associated kinase-4/nuclear factor-κB signal pathway.

OBJECTIVE: To investigate the therapeutic effect of Sishen Wan (, SSW) on ulcerative colitis (UC) induced by dinitrobenzene sulfonic acid and its effect on toll-like receptor 2/interleukin-1 receptor-associated kinase-4/nuclear factor-κB (TLR2/IRAK4/NF-κB) sig-naling pathway in colonic tissue. METHODS: In this study, 120 Sprague-Dawley rats were randomly divided into blank and model groups. The experimental UC model in rats was established by subcutaneous injection of hydrocortisone + senna gavage for 21 d + dinitrobenzene sulfonic acid (DNBS)/ ethanol solution enema. The successful model rats were randomly divided into the model group; mesalazine (0.36 g/kg) group; and high-, medium-, and low- dose SSW (24, 12, and 6 g/kg) groups. The model and blank groups were gavaged with equal volumes of distilled water once a day for 21 d. The general condition of the rats was observed, and the body mass, fecal properties, and occult blood were recorded for calculating the disease activity index (DAI) score. The colonic tissue of the rats was collected, and its general morphology and pathological form were noted for obtaining the colonic mucosal injury index (CMDI) score. Hematoxylin-eosin staining was used to view the pathological changes of the colon tissue in each group, apoptosis of the cells was detected using terminal deoxynucleotidyl transferase-mediated dUTP nick-end labeling staining, and quantitative real-time polymerase chain reaction was used to measure the expressions of TLR2, myeloid differentiation primary response gene 88 (MyD88), IRAK4, and NF-κB p65 mRNA in the colon tissue. The expressions of TLR2, MyD88, IRAK4, and NF-κB p65 protein were detected using western blotting and immunohistochemistry assay, and the levels of interleukin-1ß (IL-1ß) and tumor necrosis factor-α (TNF-α) in the colon tissue were determined using enzyme linked immunosorbent assay. RESULTS: Compared with the blank group, the general condition of the model group was relatively poor. The DAI and CMDI scores of the model group increased significantly (< 0.01), the glands and intestinal mucosa disappeared partially, and several inflammatory cells infiltrated and gathered in the mucosal layer and base layer of the rats in the model group. Furthermore, the cell apoptosis and expression levels of TLR2, MyD88, IRAK4, and NF-κB p65 mRNA and protein in the colon tissue of rats in the model group increased significantly (< 0.01). The levels of IL-1ß and TNF-α increased significantly in the colon tissue of rats in the model group (< 0.01). After treatment with SSW, compared with the model group, the general condition of the UC rats improved. Moreover, the DAI and CMDI scores of the UC rats decreased significantly (< 0.05), and the pathological changes in the colon tissue of the UC rats tended to be normal. The cell apoptosis and expression levels of TLR2, MyD88, IRAK4, and NF-κB p65 mRNA and protein in the colon tissue of the UC rats decreased gradually ( < 0.01), and the levels of IL-1ß and TNF-α decreased significantly (< 0.01). CONCLUSION: SSW can improve the general condition and alleviate the intestinal mucosal injury of UC model rats. Additionally, SSW can inhibit the TLR2/IRAK4/ NF-κB signaling pathway, but further studies are required to confirm it.

A fluorescence-based, gain-of-signal, live cell system to evaluate SARS-CoV-2 main protease inhibition.

The likelihood of continued circulation of COVID-19 and its variants, and novel coronaviruses due to future zoonotic transmissions, combined with the current paucity of coronavirus antivirals, emphasize the need for improved screening in developing effective antivirals for the treatment of infection by SARS-CoV-2 (CoV2) and other coronaviruses. Here we report the development of a live-cell based assay for evaluating the intracellular function of the critical, highly-conserved CoV2 target, the Main 3C-like protease (Mpro). This assay is based on expression of native wild-type mature CoV2 Mpro, the function of which is quantitatively evaluated in living cells through cleavage of a biosensor leading to loss of fluorescence. Evaluation does not require cell harvesting, allowing for multiple measurements from the same cells facilitating quantification of Mpro inhibition, as well as recovery of function upon removal of inhibitory drugs. The pan-coronavirus Mpro inhibitor, GC376, was utilized in this assay and effective inhibition of intracellular CoV2 Mpro was found to be consistent with levels required to inhibit CoV2 infection of human lung cells. We demonstrate that GC376 is an effective inhibitor of intracellular CoV2 Mpro at low micromolar levels, while other predicted Mpro inhibitors, bepridil and alverine, are not. Results indicate this system can provide a highly effective high-throughput coronavirus Mpro screening system.

GC-MS, LC-MS/MS, Docking and Molecular Dynamics Approaches to Identify Potential SARS-CoV-2 3-Chymotrypsin-Like Protease Inhibitors from Zingiber officinale Roscoe.

This study aims to identify and isolate the secondary metabolites of Zingiber officinale using GC-MS, preparative TLC, and LC-MS/MS methods, to evaluate the inhibitory potency on SARS-CoV-2 3 chymotrypsin-like protease enzyme, as well as to study the molecular interaction and stability by using docking and molecular dynamics simulations. GC-MS analysis suggested for the isolation of terpenoids compounds as major compounds on methanol extract of pseudostems and rhizomes. Isolation and LC-MS/MS analysis identified 5-hydro-7, 8, 2'-trimethoxyflavanone (9), (E)-hexadecyl-ferulate (1), isocyperol (2), N-isobutyl-(2E,4E)-octadecadienamide (3), and nootkatone (4) from the rhizome extract, as well as from the leaves extract with the absence of 9. Three known steroid compounds, i.e., spinasterone (7), spinasterol (8), and 24-methylcholesta-7-en-3ß-on (6), were further identified from the pseudostem extract. Molecular docking showed that steroids compounds 7, 8, and 6 have lower predictive binding energies (MMGBSA) than other metabolites with binding energy of -87.91, -78.11, and -68.80 kcal/mole, respectively. Further characterization on the single isolated compound by NMR showed that 6 was identified and possessed 75% inhibitory activity on SARS-CoV-2 3CL protease enzyme that was slightly different with the positive control GC376 (77%). MD simulations showed the complex stability with compound 6 during 100 ns simulation time.

Evaluating the Antioxidants, Whitening and Antiaging Properties of Rice Protein Hydrolysates.

Plant-derived protein hydrolysates have potential applications in nutrition. Rice protein hydrolysates (RPHs), an excellent source of proteins, have attracted attention for the development of cosmeceuticals. However, few studies have reported the potential application of RPH in analysis, and this study examined their antioxidant activities and the inhibitory activities of skin aging enzymes. The results indicated that the total phenolic and flavonoid concentrations were 2.06 ± 0.13 mg gallic acid equivalent/g RPHs and 25.96 ± 0.52 µg quercetin equivalent/g RPHs, respectively. RPHs demonstrated dose-dependent activity for scavenging free radicals from 1,1-diphenyl-2-picrylhydrazyl [half-maximal inhibitory concentration (IC50) = 42.58 ± 2.1 mg/g RPHs] and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (IC50 = 2.11 ± 0.88 mg/g RPHs), dose-dependent reduction capacity (6.95 ± 1.40 mg vitamin C equivalent/g RPHs) and oxygen radical absorbance capacity (473 µmol Trolox equivalent/g RPHs). The concentrations of the RPH solution required to achieve 50% inhibition of hyaluronidase and tyrosinase activities were determined to be 8.91 and 107.6 mg/mL, respectively. This study demonstrated that RPHs have antioxidant, antihyaluronidase, and antityrosinase activities for future cosmetic applications.

Cosmetic and Dermatological Properties of Selected Ayurvedic Plant Extracts.

Due to the constantly growing interest in ingredients of natural origin, this study attempts to evaluate the possibility of using extracts from three Ayurvedic plants in preparations for the care and treatment of skin diseases. Therefore, studies of antioxidant properties were carried out using DPPH and ABTS radicals, obtaining 76% and 88% of these radical scavenging, respectively. A significant decrease in the intracellular level of free radicals and an increase in the activity of the antioxidant enzyme-superoxide dismutase by almost 60% were also observed. In addition, the extracts were assessed for anti-inflammatory and anti-aging properties, obtaining over 70% inhibition of lipoxygenase activity and almost 40% of collagenase. Additionally, the cytoprotective properties of the obtained extracts on skin cells, keratinocytes and fibroblasts, were demonstrated. To assess the content of biologically active compounds, HPLC-electrospray ionization (ESI)-MS/MS multiple reaction monitoring (MRM) analyses were performed. The obtained results show that all three analyzed plants are a valuable source of biologically active substances with desired properties in the context of skin cell protection. Particularly noteworthy is the extract of Epilobium angustifolium L., for which the most promising results were obtained.

Design and synthesis of 3-benzylaminocoumarin-7-O-sulfamate derivatives as steroid sulfatase inhibitors.

Steroid sulfatase (STS) is a sulfatase enzyme that catalyzes the conversion of sulfated steroid precursors to free steroid. The inhibition of STS could abate estrogenic steroids that stimulate the proliferation and development of breast cancer, and therefore STS is a potential target for adjuvant endocrine therapy. In this study, a series of 3-benzylaminocoumarin-7-O-sulfamate derivatives targeting STS were designed and synthesized. Structure-relationship activities (SAR) analysis revealed that attachment of a benzylamino group at the 3-position of coumarin improved inhibitory activity. Compound 3j was found to have the highest inhibition activity against human placenta isolated STS (IC50  0.13 µM) and MCF-7 cell lines (IC50 1.35 µM). Kinetic studies found compound 3j to be an irreversible inhibitor of STS, with KI and kinact value of 86.9 nM and 158.7 min-1, respectively.

Capsaicin in Hot Chili Peppers: In Vitro Evaluation of Its Antiradical, Antiproliferative and Apoptotic Activities.

Capsaicin is a spicy capsaicinoid, produced as secondary metabolite by Capsicum fruits. This alkaloid has been used for years in folk medicine for its analgesic and antinflammatory properties although most data is referred to the raw fruit. In this study, the antiradical activity of the pure capsaicin has been studied using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) assays as well as its antiproliferative activity, using MTT assay, against two human tumour cell lines, the colorectal Caco-2 and the oesophageal OE19 cells. Furthermore, the antiproliferative activity observed on tumoral cells was compared with that of the human normal-like fibroblast cell line TelCOFS02MA. In addition, the apoptotic activity was evaluated using TUNEL assay. A higher radical scavenging activity was observed against ABTS radical cation than DPPH. Capsaicin showed also a higher cytotoxicity against cancer cells than normal-like cells with Selectivity index values greater than 2 at 72 h. Capsaicin induced apoptosis especially in OE19 cell line.

Evaluation of chemical property, cytotoxicity and antioxidant activity in vitro and in vivo of polysaccharides from Fuzhuan brick teas.

Fuzhuan brick tea (FBT) possesses various health-promoting functions. However, the available information regarding biological activity of polysaccharides from FBT (FBTPS) is still limited. In this work, the chemical property, cytotoxicity and antioxidant activity in vitro and in vivo of FBTPS were evaluated. It was found that FBTPSs were typical acidic heteropolysaccharides mainly composed of Man, Rha, GalA, Glc, Gal and Ara with little molar content of Rib and GlcA. FBTPS showed little toxicity to human hepatic epithelial (L-02) cell. FBTPS exhibited antioxidant activities, including limited scavenging activity on DPPH free radicals (ranged from 54.3 ±â€¯1.9 to 67.8 ±â€¯2.5%), noticeable scavenging activity on superoxide radicals (over 85%), superior scavenging activity on ABTS radicals (near 100%), and protective effect on H2O2-induced oxidative injury in rat pheochromocytoma line 12 (PC12) cell. Moreover, FBTPS showed significant amelioration of high-fat diet-induced oxidative injury in mice. The results suggest that FBTPS, as natural safe antioxidants, may have potential application in functional foods.

Steroid sulfatase inhibition success and limitation in breast cancer clinical assays: An underlying mechanism.

Steroid sulfatase is detectable in most hormone-dependent breast cancers. STX64, an STS inhibitor, induced tumor reduction in animal assay. Despite success in phase І clinical trial, the results of phase II trial were not that significant. Breast Cancer epithelial cells (MCF-7 and T47D) were treated with two STS inhibitors (STX64 and EM1913). Cell proliferation, cell cycle, and the concentrations of estradiol and 5α-dihydrotestosterone were measured to determine the endocrinological mechanism of sulfatase inhibition. Comparisons were made with inhibitions of reductive 17ß-hydroxysteroid dehydrogenases (17ß-HSDs). Proliferation studies showed that DNA synthesis in cancer cells was modestly decreased (approximately 20%), accompanied by an up to 6.5% in cells in the G0/G1 phase and cyclin D1 expression reduction. The concentrations of estradiol and 5α-dihydrotestosterone were decreased by 26% and 3% respectively. However, supplementation of 5α-dihydrotestosterone produced a significant increase (approximately 35.6%) in the anti-proliferative effect of sulfatase inhibition. This study has clarified sex-hormone control by sulfatase in BC, suggesting that the different roles of estradiol and 5α-dihydrotestosterone can lead to a reduction in the effect of sulfatase inhibition when compared with 17ß-HSD7 inhibition. This suggests that combined treatment of sulfatase inhibitors with 17ß-HSD inhibitors such as the type7 inhibitor could hold promise for hormone-dependent breast cancer.

Antibacterial and Antioxidant Capacities and Attenuation of Lipid Accumulation in 3T3-L1 Adipocytes by Low-Molecular-Weight Fucoidans Prepared from Compressional-Puffing-Pretreated Sargassum Crassifolium.

In this study, we extracted fucoidan from compressional-puffing-pretreated Sargassum crassifolium by hot water. The crude extract of fucoidan (SC) was degraded by various degradation reagents and four low-molecular-weight (LMW) fucoidans, namely SCO (degradation by hydrogen peroxide), SCA (degradation by ascorbic acid), SCOA (degradation by hydrogen peroxide + ascorbic acid), and SCH (degradation by hydrogen chloride) were obtained. The degradation reagents studied could effectively degrade fucoidan into LMW fucoidans, as revealed by intrinsic viscosity, agarose gel electrophoresis, and molecular weight analyses. These LMW fucoidans had higher uronic acid content and sulfate content than those of SC. It was found that SCOA exhibited antibacterial activity. All LMW fucoidans showed antioxidant activities as revealed by DPPH (2,2-diphenyl-1-picrylhydrazyl), ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt), and FRAP (ferric reducing antioxidant power) methods. Biological experiments showed that SC and SCOA had relatively high activity for the reversal of H2O2-induced cell death in 3T3-L1 adipocytes, and SCOA showed the highest effect on attenuation of lipid accumulation in 3T3-L1 adipocytes. Therefore, for the LMW fucoidans tested, SCOA showed antibacterial activity and had a high fucose content, high sulfate content, high activity for the reversal of H2O2-induced cell death, and a marked effect on attenuation of lipid accumulation. It can thus be recommended as a natural and safe antibacterial and anti-adipogenic agent for food, cosmetic, and nutraceutical applications.

Anthelmintic activity of Tunisian chamomile (Matricaria recutita L.) against Haemonchus contortus.

The chemical treatment of gastrointestinal parasitic diseases has been undermined by increasing resistance and high toxicity. There is an urgent need to search for alternative natural sources for the treatment of such parasites. In this respect, the present study aims to quantify phenolic compounds of chamomile (Matricaria recutita L.) and to study their in vitro anti-oxidant and anthelmintic activities in solvents with increasing polarity. In vitro determination of anti-oxidant capacity was carried out using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2-azino-bis-(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) radical cation methods. In vitro anthelmintic activity was investigated on egg-hatching inhibition and loss of motility of adult worms of Haemonchus contortus from sheep. The results showed that methanolic and aqueous extracts contain more total polyphenols, total flavonoids and condensed tannins than chloroformic and hexanic extracts. ABTS and DPPH assays showed that methanolic extracts had the highest anti-oxidant potency (IC50 = 1.19 µg/ml and 1.18 µg/ml, respectively). In vitro anthelmintic activity showed that both methanolic (IC50 = 1.559 mg/ml) and aqueous (IC50 = 2.559 mg/ml) extracts had the greatest effect on egg hatching and motility of worms (100% after 8 h post exposure at 8 mg/ml). A significant and positive correlation between DPPH and ABTS tests was observed for all tested extracts. Therefore, total phenolic, total flavonoid and condensed tannin values were correlated with IC50 from both ABTS and DPPH, and with inhibition of egg hatching. To our knowledge, this report is the first of its kind to deal with in vitro anthelmintic activities of chamomile extracts.

Wound healing and anti-inflammatory activity of some Ononis taxons.

Ononis species are used for their laxative, diuretic, analgesic, anti-inflammatory, antiviral, cytotoxic and antifungal effects as well as against skin diseases for wound healing activity. In the light of this information n-hexane, ethylacetate and methanol extracts prepared from Ononis spinosa L. subsp. leiosperma (Boiss.) Sirj., Ononis variegata L., Ononis viscosa L. subsp. brevifolia (DC) Nym. and Ononis natrix L. subsp. natrix L. were tested for their wound healing, anti-inflammatory and antioxidant activities. Linear incision and circular excision wound models and hydroxypyroline estimation assay were used for the wound healing activity. For the assessment of chronic inflammation FCA-induced arthritis and for acute inflammation carrageenan-induced hind paw edema, TPA-induced ear edema and acetic acid-induced increase in capillary permeability tests were conducted. 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay, 2,2-azino-bis-(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) scavenging activity assay, reducing power assay and hydroxyl radical (OH-) scavenging assay were used for determining antioxidant activities of the extracts. Results showed that O. spinosa subsp. leiosperma roots ethyl acetate extract exhibited remarkable wound healing activity with the 42.6% tensile strength value on the linear incision wound model and 60.1% reduction of the wound area at the day 12 on the circular excision wound model. Hydroxyproline content of the tissue treated by O. spinosa subsp. leiosperma roots ethyl acetate extract was found to be 41.3µg/mg. Acetic acid induced increase in capillary permeability test results revealed that O. spinosa subsp. leiosperma roots ethyl acetate extract and O. spinosa subsp. leiosperma roots methanol extract inhibited inflammation by 40.4% and 35.4% values respectively. O. spinosa subsp. leiosperma roots ethyl acetate extract showed 21.2-27.2% inhibition in carrageenan-induced hind paw edema test while did not posses activity on TPA-induced ear edema and FCA-induced arthritis models.

Antifungal properties of hypericin, hypericin tetrasulphonic acid and fagopyrin on pathogenic fungi and spoilage yeasts.

CONTEXT: The role of hypericin-mediated photodynamic antimicrobial properties on pathogenic fungi and photodynamic therapy for human cancer cells is known. Antifungal properties of Hypericum perforatum L. (Hypericaceae) and Fagopyrum esculentum Moench. (Polygonaceae) extracts were also studied. The different polarities of solvents can cause complication in the identification of antifungal effects of separate biologically active compounds. In recent experimental work, we compared antifungal properties of purified hypericin, hypericin tetrasulphonic acid (hypericin + S) and fagopyrin, which is analogue of hypericin. OBJECTIVE: The antifungal properties of aromatic polyketide derivatives such as hypericin, hypericin + S and fagopyrin on the selected pathogenic fungi and spoilage yeasts have been studied. MATERIALS AND METHODS: The antifungal properties of hypericin, hypericin + S and fagopyrin were determined using the broth microdilution method against a set of pathogenic fungi and spoilage yeasts including: Microsporum canis, Trichophyton rubrum, Fusarium oxysporum, Exophiala dermatitidis, Candida albicans, Kluyveromyces marxianus, Pichia fermentans and Saccharomyces cerevisiae. The tested concentrations of hypericin, hypericin + S and fagopyrin ranged from 750 to 0.011 µg/mL and MIC values were evaluated after 48 h incubation at 30 °C. RESULTS: The results confirm different antifungal properties of hypericin, hypericin + S and fagopyrin on the selected pathogenic fungi and spoilage yeasts. For pathogenic fungi, the minimum inhibitory concentrations of hypericin ranged 0.18-46.9 µg/mL, hypericin + S 0.18-750 µg/mL and fagopyrin 11.7-46.9 µg/mL. For spoilage yeasts, the MICs of hypericin and hypericin + S ranged 0.18-46.9 and 0.011-0.73 µg/mL, respectively. DISCUSSION AND CONCLUSION: The results obtained herein indicate that various chemical structures of hypericin, hypericin + S and fagopyrin can develop different antifungal properties.

HPLC profiling, antioxidant and in vivo anti-inflammatory activity of the ethanol extract of Syzygium jambos available in Bangladesh.

BACKGROUND: Syzygium jambos has been used as a traditional medicine for the treatment of inflammatory diseases in Bangladesh. The study investigates the high performance liquid chromatography (HPLC) profiling of phenolic compounds, and evaluates the antioxidant and anti-inflammatory activities of ethanol extract of S. jambos available in Bangladesh. METHODS: The extract was subjected to HPLC for the identification and quantification of the major bioactive polyphenols present in S. jambos. Antioxidant activity was determined using 2, 2'-azino bis-3-ethylbenzothiazoline-6-sulfonic acid (ABTS) radical scavenging, reducing power assay, total antioxidant capacity, total phenolic and flavonoid content. Furthermore, the anti-inflammatory effect of the extract in rats for two different test models: carrageenan and histamine-induced paw edema was inspected. RESULTS: High levels of catechin hydrate and rutin hydrate (99.00 and 79.20 mg/100 g extract, respectively) and moderate amounts of ellagic acid and quercetin (59.40 and 69.30 mg/100 g extract, respectively) were quantified in HPLC. Catechin hydrate from this plant extract was determined for the first time through HPLC. For ABTS scavenging assay, the median inhibition concentration (IC50) value of S. jambos was 57.80 µg/ml, which was significant to that of ascorbic acid (12.01 µg/ml). The maximum absorbance for reducing power assay was found to be 0.4934. The total antioxidant capacity, phenolic and flavonoid contents were calculated to be 628.50 mg/g of ascorbic acid, 230.82 mg/g of gallic acid and 11.84 mg/g of quercetin equivalent, respectively. At a dose of 400 mg/kg, a significant acute anti-inflammatory activity (P < 0.01) was observed in rats for both the test models with a reduction in the paw volume of 58.04 and 53.95 %, in comparison to those of indomethacin (62.94 and 65.79 %), respectively. CONCLUSIONS: The results suggest that the phenolic and flavonoid compounds are responsible for acute anti-inflammatory and antioxidant activities of S. jambos.

Designing anti-diabetic ß-cells microcapsules using polystyrenic sulfonate, polyallylamine, and a tertiary bile acid: Morphology, bioenergetics, and cytokine analysis.

PURPOSE: Recently sodium alginate (SA)-poly-l-ornithine (PLO) microcapsules containing pancreatic ß-cells that showed good morphology but low cell viability (<27%) was designed. In this study, two new polyelectrolytes, polystyrenic sulfonate (PSS; at 1%) and polyallylamine (PAA; at 2%) were incorporated into a microencapsulated-formulation, with the aim of enhancing the physical properties of the microcapsules. Following incorporation, the structural characteristics and cell viability were investigated. The effects of the anti-inflammatory bile acid, ursodeoxycholic acid (UDCA), on microcapsule morphology, size, and stability as well as ß-cell biological functionality was also examined. METHODS: Microcapsules were prepared using PLO-PSS-PAA-SA mixture and two types of microcapsules were produced: without UDCA (control) and with UDCA (test). Microcapsule morphology, stability, and size were examined. Cell count, microencapsulation efficiency, cell bioenergetics, and activity were also examined. RESULTS: The new microcapsules showed good morphology but cell viability remained low (29% ± 3%). UDCA addition improved cell viability post-microencapsulation (42 ± 5, P < 0.01), reduced swelling (P < 0.01), improved mechanical strength (P < 0.01), increased Zeta-potential (P < 0.01), and improved stability. UDCA addition also increased insulin production (P < 0.01), bioenergetics (P < 0.01), and decreased ß-cell TNF-α (P < 0.01), IFN-gamma (P < 0.01), and IL-6 (P < 0.01) secretions. CONCLUSIONS: Addition of 4% UDCA to a formulation system consisting of 1.8% SA, 1% PLO, 1% PSS, and 2% PAA enhanced cell viability post-microencapsulation and resulted in a more stable formulation with enhanced encapsulated ß-cell metabolism, bioenergetics, and biological activity with reduced inflammation. This suggests potential application of UDCA, when combined with SA, PLO, PSS, and PAA, in ß-cell microencapsulation and diabetes treatment. © 2016 American Institute of Chemical Engineers Biotechnol. Prog., 32:501-509, 2016.

Sulfotanone, a new alkyl sulfonic acid derivative from Streptomyces sp. IFM 11694 with TRAIL resistance-overcoming activity.

One new alkyl sulfonic acid derivative, sulfotanone (1), and the known panosialin wA (2) were isolated from the methanolic extract of mycelium of Streptomyces sp. 11694. The structure of the new compound (1) was established by a combination of spectroscopic techniques, including HRESIMS, IR, 1D and 2D NMR measurements. Compound 1 (40 µM) in combination with TRAIL showed synergistic activity in sensitizing TRAIL-resistance in human gastric adenocarcinoma cell lines.

Lignosulfonic Acid-Induced Inhibition of Intestinal Glucose Absorption.

Lignosulfonic acid is a waste lignin produced from the sulfite pulping of softwood. We investigated the effect of lignosulfonic acid on α-glucosidase and found that lignosulfonic acid produced a reversible and non-competitive inhibition of the enzyme activity. Moreover, in human colorectal adenocarcinoma cells, lignosulfonic acid inhibited 2-deoxyglucose uptake, while in vivo studies demonstrated a significant reduction in the blood glycemic response to sucrose or glucose ingestion in rats treated with lignosulfonic acid. Feces of rats fed a diet supplemented with 5% lignosulfonic acid had higher sugar content compared to those of rats fed a control diet. These results suggest that lignosulfonic acid suppresses the rise in blood glucose levels through inhibition of α-glucosidase activity and intestinal glucose absorption.

Study on the antioxidant and antimicrobial activities of Allium ursinum L. pressurised-liquid extract.

Allium ursinum L. is widely used as a spice as well as a traditional medicine. The aim of this work was to evaluate the antioxidant and antimicrobial activities (AMAs) of A. ursinum extract, obtained by pressurised-liquid extraction. Several reliable procedures such as 2,2-diphenyl-1-picrylhydrazyl, 2,2-azinobis-3ethyl benxothiazoline-6-sulphonic acid, ferric-reducing antioxidant power assay and oxygen radical absorbance capacity assays were carried out. Vegetable oil stability was evaluated by using Rancimat test. Moreover, AMA was performed on different microorganisms. On the basis of the results obtained, it is confirmed that the A. ursinum extract could be used as a natural ingredient in food and/or pharmaceutical industries.

A novel phenolic acid from the fruits of Rosa soulieana.

From the n-BuOH-soluble fraction of a MeOH extract of the fruits of Rosa soulieana, one new phenolic glucoside (1) was isolated along with five known compounds, comprising two lignin glycosides, two flavonoid glycosides and a phenolic glycoside. The chemical structure of the new compound was elucidated by extensive spectroscopic analyses, including ESI-MS, UV, IR, (1)H and (13)C NMR, DEPT and 2D NMR (HSQC and HMBC). All the isolated compounds were evaluated for their antioxidant activity by using ABTS (2,2'-azino-bis(3-ethylbenzoline-6-sulfonic acid)) assay. Among these compounds, 1, 3 and 6 exhibited strong scavenging activity in ABTS(·+)(SC50 = 102.10, 193.85, 65.38 µmol/L, respectively) compared with the positive control l-ascorbic acid (Vc) (SC50 = 117.16 µmol/L).