Discovery of new aliphatic metabolites with antibacterial activities from a soil-derived Streptomyces antifungus.

Fifteen new aliphatic metabolites, 2-methylpyrimidin-4(3H)-ones (1,2), 2-methoxy-2-methyl-1,2-dihydro-3H-pyrrol-3-ones (4a/4b, 5a/5b), butyrolactones (6-9), and aliphatic metabolites (16-20) as well as known pyridin-2(1H)-one (3) and butyrolactone analogues (10-15) were obtained from the fermentation broth of Streptomyces antifungus isolated from the forest soil sample collected in Tengchong, China. Pyrimidin-4(3H)-one derivatives (1, 2) with an individual 2-methylpyrimidin-4(3H)-one skeleton is a kind of rarely reported compound and were firstly obtained from natural source. The structures of the new metabolites were elucidated by comprehensive spectroscopic analysis including data from experimental and calculated ECD spectra as well as Mosher's reagent derivative method.

Discovery of structurally diverse sesquiterpenoids from Streptomyces fulvorobeus isolated from Elephas maximus feces and their antifungal activities.

Thirty-six structurally diverse sesquiterpenoids, including caryolanes (1-12), germacranes (13-16), isodaucane (17), cadinanes (18-22), epicubenols (23, 24), oplopanane (25), pallenanes (26, 27), and eudesmanes (28-36), were isolated from the fermentation broth of Streptomyces fulvorobeus derived from Elephas maximus feces. Pallenane is a kind of rarely reported sesquiterpene with a distinctive C5/C3 bicyclic skeleton and was firstly found from microbial source. The structures of fifteen new compounds (1-4, 13-15, 17, 18, 22, 23, 25-28) were established through detailed spectroscopic data analysis, which included data from experimental and calculated ECD spectra as well as Mosher's reagent derivative method.

Caseinate-coated zein nanoparticles as potential delivery vehicles for guavinoside B from guava: Molecular interactions and encapsulation properties.

Guavinoside B (GUB) is a characteristic constituent from guava with strong antioxidant activity; however, its low water solubility limits its utilization. Herein, we investigated the interaction between GUB and zein, a prolamin with self-assembling property, using multiple spectroscopic methods and fabricated GUB-zein-NaCas nanoparticles (GUB-Z-N NPs) via the antisolvent coprecipitation approach. GUB caused fluorescence quenching to zein via the static quenching mechanism.

Discovery of Antifungal Norsesquiterpenoids from a Soil-Derived : Targeting Biofilm Formation and Synergistic Combination with Amphotericin B against Yeast-like Fungi.

Thirty-five norsesquiterpenoids were isolated from the fermentation broth of from the forest soil of Ailaoshan in China. The structures of new compounds (-, -) were elucidated by comprehensive spectroscopic analysis including data from experimental and calculated ECD spectra, as well as Mosher's reagent derivatives method. Norsesquiterpenoids showed different levels of antifungal activity with MIC values ranging from 25 to 200 μg/mL against , , and .

Structure-activity relationship and biofilm formation-related gene targets of oleanolic acid-type saponins from Pulsatilla chinensis against Candida albicans.

In the course of our investigations of antifungal natural products, the structure-activity relationship and antifungal activities of oleanolic acid-type saponins (1-28) from Pulsatilla chinensis against human and plant pathogenic fungi were elucidated. The analysis of structure-activity relationship of oleanolic acid-type saponins showed that the free carboxyl at C-28 was essential for their antifungal activities; the free hydroxyl group at the C-23 site of oleanolic acid-type saponins played a crucial role in their antifungal activities; the oligosaccharide chain at C-3 oleanolic acid-type saponins showed significant effects on antifungal efficacy and a disaccharide or trisaccharide moiety at position C-3 displayed optimal antifungal activity. The typical saponin pulchinenoside B3 (16, PB3) displayed satisfactory antifungal activity against human and plant pathogenic fungi, especially, C.

Discovery, synthesis, and cytotoxic evaluation of isoquinolinequinones produced by derived from lichen.

Four isoquinolinequinones (1-4) were isolated from the fermentation broth of which were derived from lichens. Among them, mansouramycin H (1) was identified as a new isoquinolinequinone by comprehensive spectroscopic data analysis. The mansouramycins from presented broad cytotoxic activities, especially against MDA-MB-231, but the SAR and mechanism were still unclear.

Senkyunolide B exhibits broad-spectrum antifungal activity against plant and human pathogenic fungi via inhibiting spore germination and destroying the mature biofilm.

Background: Aspergillus infection seriously jeopardizes the health and safety of life of immunocompromised patients. The emergences of antifungal resistance highlight a demand to find new effective antifungal drugs. Angelica sinensis is a medicine-food herb and phthalides are its characteristic components.

Levistolide A ameliorates fibrosis in chronic kidney disease via modulating multitarget actions in vitro and in vivo.

Aims: The increasing incidence of chronic kidney disease (CKD) urgently calls for effective nephroprotective agents. Traditional Chinese Medicine Angelica sinensis and its formula are well known for CKD therapy, but the underlying mechanisms and effective substances of reno-protective effects remain unclear. To this end, we isolated eleven ligustilide dimers (1-11) from A.

Discovery, Preliminary Structure-Activity Relationship, and Evaluation of Oleanane-Type Saponins from for the Treatment of Ulcerative Colitis.

To discover ulcerative colitis (UC) treatment agents, 28 oleanane-type triterpenoid saponins (-) including three new saponins, pulsatillosides P-R (-), were isolated from . The isolated saponins could observably ameliorate UC by improving the intestinal epithelial cell barrier and intestinal flora . The structure-activity relationship indicated that the oligosaccharide chain at C-28 was essential for their anti-UC activities; the methyl group at the C-23 site of triterpene saponins showed important effects on anti-UC efficacy; the chain length of oligosaccharides at position C-28 had little effect on their anti-UC activities.

The Anti-inflammatory Effects of Isoflavonoids from Radix Astragali in Hepatoprotective Potential against LPS/D-gal-induced Acute Liver Injury.

Radix Astragali (RA) is an important Traditional Chinese Medicine widely used in the treatment of various diseases, such as pneumonia, atherosclerosis, diabetes, kidney and liver fibrosis. The role of isoflavonoids from RA in the treatment of liver injury remains unclear. The study aimed to explore hepatoprotective and anti-inflammatory effects of isoflavonoids from .

Phenolipid JE improves metabolic profile and inhibits gluconeogenesis via modulating AKT-mediated insulin signaling in STZ-induced diabetic mice.

Phenolipids are characteristic phytochemicals of Syzygium genus. However, the antidiabetic potential and underlying molecular mechanism of these components are not fully elucidated. Herein, we studied the anti-diabetic effects of jambone E (JE), a phenolipid from S.

Effect of treatment with Fufang Huangqi decoction on dose reductions and discontinuation of pyridostigmine bromide tablets, prednisone, and tacrolimus in patients with type I or II myasthenia gravis.

Objective: To investigate the clinical efficacy of Fufang Huangqi decoction in combination with pyridostigmine bromide tablets, prednisone, and tacrolimus in the treatment of type I and II myasthenia gravis (MG) through changes in the clinical symptom scores of 100 patients with type I and II MG. This study also aimed to examine dose reductions and dis-continuation of these 3 Western medicines after administration of Fufang Huangqi decoction.

Methods: The clinical data on 100 patients with type I or II MG who were treated in the outpatient department of the Affiliated Hospital of Liaoning University of Traditional Chinese Medicine, China, between June 2017 and June 2020 were collected.

Novel melatonin-trientine conjugate as potential therapeutic agents for Alzheimer's disease.

Researchers continue to explore drug targets to treat the characteristic pathologies of Alzheimer's disease (AD). Some drugs relieve the pathological processes of AD to some extent, but the failed clinical trials indicate that multifunctional agents seem more likely to achieve the therapy goals for this neurodegenerative disease. Herein, a novel compound named melatonin-trientine (TM) has been covalently synthesized with the natural antioxidant compounds melatonin and the metal ion chelator trientine.

Discovery of antibacterial agents targeting biofilm formation: total synthesis and investigation of amycolasporins.

Three monoterpene alkaloids amycolasporin A and (±) amycolasporins B and C have been synthesized for the first time from commercially available materials in yields of 31%, 14% and 21%, respectively. Their six analogues (18, 19, 30a and 30d-30f) were synthesized through a similar protocol. Meanwhile, the antibacterial activity of all synthesized molecules was evaluated, showing different levels of bioactivity.

Comparative and functional analyses of fecal microbiome in Asian elephants.

Asian elephant is large herbivorous animal with elongated hindgut. To explore fecal microbial community composition with various ages, sex and diets, and their role in plant biomass degrading and nutrition conversation. We generated 119 Gb by metagenome sequencing from 10 different individual feces and identified 5.

Discovery, preparation and characterization of lipid-lowering alkylphenol derivatives from Syzygium jambos fruit.

The chemical characteristics and hypolipidemic effects of alkylphenols in the fruit of Syzygium jambos were investigated in this study. Three cardanols (1-3; 1 as a new compound) and three alkylresorcinols (4-6) were isolated and identified from S. jambos fruit.

The crude guava polysaccharides ameliorate high-fat diet-induced obesity in mice via reshaping gut microbiota.

Guava is a popular fruit consumed worldwide with beneficial effects in regulation of glucose and lipid metabolism. Although polysaccharides are a major phytochemical component of guava, to date, the alleviative effects of polysaccharides from the guava fruit against diet-induced obesity remain unclear. The relationship between the anti-obesity effects of guava polysaccharide (GP) and gut microbiota is unknown.

Oxazolomycins produced by and their cytotoxic activity.

Six oxazolomycins (1-6) were isolated from the fermentation broth of a soil-borne bacterial strain, . The structures of the new compounds, oxazolomycins D-F (1-3) and glaucumycins A, B (6a/6b), were elucidated by detailed spectroscopic data analysis. Oxazolomycins 1, 2, 4, and 5 demonstrated weak or modest cytotoxic activities against four human cancer cell lines, with IC values ranging from 10.

The discovery of germacradienol synthase: Construction of genetically-engineered strain, glycosylated modification, bioactive evaluation of germacradienol.

Germacradienol is a main precursor in the biosynthesis of geosmin-type terpenes by a variety of microbes, but its biological activities are still unknown. In the biosynthetic mechanism study of an antifungal degraded sesquiterpenoid (1β,4β,4aβ,8aα)-4,8a-dimethyloctahydronaphthalene-1,4a(2H)-diol (5) with a geosmin scaffold, the germacradienol synthase B7C62_00490 was identified. To exploit the synthetic potential of the enzyme to create germacradienol, engineered strains were constructed by introducing key synthases of farnesyl diphosphate, germacradienol synthase B7C62_00490 and glycosyltransferase UGT73C5 in Escherichia coli BL21(DE3).

New Monoterpene Acid and Gallic Acid Glucose Esters with Anti-Inflammatory Activity from Blue Gum () Leaves.

Blue gum () is a widely used botanical in the cosmeceutical and food industries. Although blue gum leaves are known for abundant essential oils, their nonvolatile phytochemical constituents and bioactivities remain unclear. Herein, a phytochemical investigation of blue gum leaves led to the identification of eight new monoterpene acid and gallic acid glucose esters ( and ; glubosides A-H, respectively) and 12 known analogues ( and ).

Effect of Fufang Huangqi Decoction on the Gut Microbiota in Patients With Class I or II Myasthenia Gravis.

Objective: To investigate the effect of Fufang Huangqi Decoction on the gut microbiota in patients with class I or II myasthenia gravis (MG) and to explore the correlation between gut microbiota and MG (registration number, ChiCTR2100048367; registration website, http://www.chictr.org.

Riligustilide alleviates hepatic insulin resistance and gluconeogenesis in T2DM mice through multitarget actions.

Riligustilide (RG), one of the dimeric phthalides of Angelica sinensis and Ligusticum chuanxiong, was confirmed effective against many diseases. However, its effects on type 2 diabetes mellitus (T2DM) and the underlying molecular mechanisms have not been clearly elucidated yet. The current study was designed to investigate the hypoglycemic potential by which RG affects the pathogenesis of T2DM.

Downregulating expression of OPTN elevates neuroinflammation via AIM2 inflammasome- and RIPK1-activating mechanisms in APP/PS1 transgenic mice.

Background: Neuroinflammation is thought to be a cause of Alzheimer's disease (AD), which is partly caused by inadequate mitophagy. As a receptor of mitophagy, we aimed to reveal the regulatory roles of optineurin (OPTN) on neuroinflammation in the pathogenesis of AD.

Methods: BV2 cells and APP/PS1 transgenic (Tg) mice were used as in vitro and in vivo experimental models to determine the regulatory roles of OPTN in neuroinflammation of AD.

Chemical characterization, antiproliferative and antifungal activities of Clinacanthus nutans.

Clinacanthus nutans Lindau (Family: Acanthaceae) is a medicinal herb widely distributed in the tropic and subtropic areas of Asia. C. nutans is traditionally consumed as vegetable or herbal tea, as well as a folk medicine for anticancer and antifungal activities.