One new naphthalenone, didymelol A (1), and three new naphthols, didymelol B‐D (5‐7), together with three known naphthalenones, (3S,4R)‐3,4,6,8‐tetrahydroxy‐3,4‐dihydronaphthalen‐1(2H)‐one (2), (S)‐4,6,8‐trihydroxy‐3,4‐dihydronaphthalen‐1(2H)‐one (3), (S)‐4,8‐dihydroxy‐3,4‐dihydronaphthalen‐1(2H)‐one (4), were isolated from the Saussurea laniceps endophytic fungus Didymella glomerate X223. The structures

Squalene has been used as a dietary supplement for a long history due to its potential cancer‐preventive function. However, the mechanism has not yet been investigated in detail. Therefore, the aim of this study is to see if the plasma coenzyme Q 10 (CoQ 10 ) level will be altered by gavage of squalene and oxidosqualenes to rats. In the present work, a sensitive and simple high‐performance analytical

Mints are the most popular economic and traditional herbs. The aim of this paper was chemical characterization of volatile compounds from wild populations of Mentha aquatica , M . arvensis , M . longifolia , M . microphylla, M . pulegium , M . spicata , M . × dumetorum , M . × gentillis and M . × verticillata , as well as cultivated samples of M . spicata , M . × piperita 'Alba' and M . × piperita

Drug resistance tuberculosis is one of the challenging tasks that dictates the desperate need for the development of new anti‐tubercular agents which operate via novel modes of action. Here, we are reporting the 4‐amino quinazolines as M. tuberculosis N ‐acetylglucosamine‐1‐phosphate uridyltransferase (GlmU MTB) inhibitors to overcome the problem of the MDR‐TB. Amongst the synthesized compounds HMP‐05

Somatostatin (SST) analogues have aroused the interest of scientists for years. This group of compounds is used in the diagnosis and treatment of neuroendocrine tumors. However, new molecules useful as radiopharmaceuticals in targeted therapy are still searched for. Bicyclic peptides seem to be very interesting in this context. These molecules are associated with beneficial properties. In this work

The chemical components and antioxidant activity of 16 Rehmannia glutinosa samples were investigated to reveal the high‐quality raw resource for pharmaceutical products. 22 main chemical components were detected, with significant content differences ( P <0.05). 14 substances contents reached the maximum in S1 sample, such as catalpol (6.74 mg g ‐1 ), rehmaionoside A (1.93 mg g ‐1 ) and rehmannioside

Methionine sulfoxide reductase A (MsrA), an efflux pump belonging to ATP-binding cassette (ABC) transporter family that conferred resistance to macrolides, was detected in Methicillin-Resistant Staphylococcus aureus (MRSA) RN4220 strain. Herein we report isolation of phytoconstituents from Piper cubeba fruit methanol extract and investigated their efflux pump inhibitory potential against MsrA pump

Fungi have especially captured the interest and fascination of natural product chemists in that they produce a dizzying array of natural organic molecules with many unique functional groups and atom arrangements. In the review, we focus on a genus Talaromyces which have been the hot spot of natural product studies over the last three decades. This review summarized the discovery, structures, and bioactivities

Dysregulation of miRNAs is connected with a multitude of diseases for which antagomirs and miRNA replacement are discussed as therapeutic options. Here, we suggest an alternative concept based on the redirection of RISC complexes to non-native target sites. Metabolically stable DNA-LNA mixmers are used to mediate the binding of RISCs to mRNAs without any direct base complementarity to the presented

The biological characterization of Microdochium majus, M. nivale, and M. seminicola strains with wide geographical origins showed the diversity of their pathogenic properties and metabolite compounds, allowing them to exist in their habitats. Significant differences in the ability of Microdochium fungi to cause lesions on wheat and oat leaves were found. The intensity of symptoms depended on the species

A series of novel α-(diphenylphosphoryl)- and α-(diphenylphosphorothioyl)cycloalkanone oximes have been synthesized in search for novel bioactive molecules. Their structures were characterized by various spectroscopic methods including IR, NMR ( 1 H, 31 P, 13 C), mass spectrometry and single crystal X-ray diffraction. The newly synthesized phosphorus-containing oximes were screened for their in vitro

Cholinergic disorder, oxidative stress, and neuroinflammation play important roles in the pathology of Alzheimer's disease. To explore the healthy potential of the edible seaweed Hizikia fusiforme on this aspect, a functional oil (HFFO) was extracted from this alga and investigated on its constituents by gas chromatography-mass spectrometry (GC-MS) in this study. Its anti-Alzheimer's related bioactivities

Herbal medicines are widely used for the treatment of different types of diseases like skin and throat infections and other diseases in developing countries. Syzygium cumini (L.) Skeels fruit, leaves and bark were used for the remedies of different diseases anciently. The aim of the present study was to evaluate the chemical profile of Syzygium cumini (L.) leaves essential oil (EO) from Punjab, Pakistan

Lipophilic extractive metabolites from needles and defoliated twigs of Pinus armandii and P. kwangtungensis were studied by GC-MS. Needles of P. armandii contained predominantly 15- O -functionalized labdane type acids (anticopalic acid), fatty acids, nonacosan-10-ol, sterols, nonacosan-10-ol and sterol saponifiable esters, and acylglycerols. While P. kwangtungensis needles comprised no anticopalic

Two new norlignans ( 1 - 2 ), together with two known phenylpropanoids ( 3 - 4 ) were isolated from whole herb of Anemone vitifolia. All compounds were reported from this plant for the first time. The structures of these compounds were identified by comprehensive HR-ESI-MS, 1D and 2D NMR spectroscopic data analysis and comparison with literature data. Additionally, bioactivity study results showed

The Acknowledgment part in this article should include the sentence: The authors thank Dr. İsmet Öztük (Erciyes University) who kindly provided the yeast strains used in this study.

Pithecellobium dulce has been used in traditional medicine to treat various ailments owing to its restorative properties. The biological activities and chemical profiles of the lipophilic fraction of P. dulce bark and leaves were assessed herein. Fatty acid methyl esters (FAME) and unsaponifiable matter (USM) were prepared and analyzed by GC/MS. A total of 40 compounds were identified in the bark saponifiable

Two sulfated fucoidan fractions (Lj3 and Lj5) were extracted from Saccharina japonica and then subjected to acid hydrolysis to obtain Lj3h and Lj5h. Lj3h and Lj5h were characterized using IR, methylation analysis, and mass spectrometry. It was found that Lj3h and Lj5h were homogeneous low molecular weight fucoidans. Specifically, Lj3h was composed of the main chain of 1,3-linked α-L-fucopyranose residues

Penicimutanin C (1), a new alkaloidal compound, was isolated from the neomycin-resistant mutant strain 3-f-31 of the marine-derived fungus, Penicillium purpurogenum G59, together with four known compounds 2-5. The structure of penicimutanin C (1), including the absolute configuration, was determined by spectroscopic and chemical methods. The absolute configuration of penicimutanin A (2) was also re-confirmed

Zea mays L. (ZM) has anticancer and anti-inflammatory activites, but its biological activities such as skin regeneration and wound healing in human skin have not reported. In the present study, we tested the effects of ZM flower (ZMF) absolute on proliferation and migration of human keratinocytes (HaCaTs) and identified its components by using gas chromatography/mass spectrometry (GC/MS) analysis.

20( S )-protopanaxadiol ginsenosides Rg3, Rh2 and PPD have been demonstrated for their anticancer activity. However, the underlying mechanism of their anti-tumor activity remains unclear. In the present study, we investigated the role of these three ginsenosides on cell proliferation and death of human gastric cancer cells (HGC-27 cells). The sulforhodamine B (SRB) assay, western blot analysis, fluorescence

Novel enamine derivatives (7a-o) were synthesized from the reaction of lactone (6) and chalcones (3a-o) and their antiproliferative and cell cytotoxicity activities against six cancer cell lines (e.g., HeLa, HT29, A549, MCF7, PC3 and Hep3B) and one normal cell line (e.g., FL) were investigated along with their mode of interactions with CT-DNA. Most of the enamine derivatives (7a-o) with 86-168 µM IC50

Carpodesmia tamariscifolia is a brown alga rich in (poly)phenols with important cytotoxic and antioxidant effects. However, the relationship between its chemical composition and its effects is unknown. The aim of this study is to identify the potential compounds and mechanisms responsible for its main effects. The alga was extracted consecutively with hexane, dichloromethane and methanol and further

A synthesis method of novel N -cycloalkylcarbonyl- N ' -aryl-thioureas was developed. It consists of sequential addition of equimolecular amounts of ammonium isothiocyanate and substituted anilines to cycloalkylcarbonyl chlorides. The identity and purity of products were confirmed by LC-MS spectra, their structure by elemental analysis, IR and 1 H NMR spectra. Preliminary antimicrobial screening for

The essential oils (EOs) from leaves, stems, and whole plant of Piper boehmeriifolium were analyzed using GC/FID and GC/MS. The main constituents of P. boehmeriifolium EOs were β -caryophyllene, caryophyllene oxide, β -elemene, spathulenol, germacrene D, β -selinene, and neointermedeol. The antioxidant potential of the EOs were determined using DPPH • , ABTS •+ and FRAP assays. In ABTS •+ assay, the

Two new meroterpenoids, tricycloalternarenes X and Y ( 1 and 2 ), together with one known meroterpenoid, tricycloalternarene I, were isolated from the sponge-associated fungus Alternaria sp. JJY-32. The structures including absolute configurations were established on the basis of comprehensive spectroscopic data, electronic circular dichroism (ECD) spectral analyses, and biosynthesis consideration

N6-methyladenosine (m6A) is one of the most important RNA modifications in epigenetics. The development of detection method for m6A is limited by its abundance and structure. Although it has been previously reported that its presence has an impact on the complementary pairing of RNA, few assays have been developed using this finding. We used this discovery and designed a detection method based on cas13a

A small library of 120 compounds was established with seventy new alkylated derivatives 2-71 of the natural product terphenyllin (1), together with the previous reported derivatives 72-116 and natural p-terphenyl analogues 117-120. The new derivatives 2-71 were semisynthesized and evaluated for cytotoxic activities against four cancer cell lines. Interestingly, 2',4''-diethoxyterphenyllin (6), 2',4

A series of tetrapeptide amides containing two aminoisobutyric acids (Aib) and two a-methylphenylalanine ((aMe)Phe) units were prepared via the 'azirine/oxazolone method'. New 2-benzyl-2-methyl-2 H -azirine-3-amines have been used for the selective introduction of ( S )- and ( R )-(aMe)Phe, respectively. The solid-state conformations of five tetrapeptide amides were determined by X-ray crystallography

13-( N -alkyl)-aminomethyl-8-oxo-dihydrocotisines were synthesized to evaluate antibacterial activity against Clostridium difficile and activating x-box-binding protein 1 activity, biological properties both associated with ulcerative colitis. Improving structural stability and ameliorating biological activity were major concerns. Different substituents on the structural modification site were involved

Two series of 3-((1-benzyl-1 H -1,2,3-triazol-4-yl)methyl)quinazolin-4(3H)-ones ( 4a-j ) and N-(1-benzylpiperidin-4-yl)quinazolin-4-amines ( 6a-j ) were designed initially as potential acetylcholine esterase inhibitors. Biological evaluation demonstrated that series 6a-j significantly inhibited AChE activity. Especially compounds 6c and 6e were found to be the most potent with relative AChE inhibition

(-)-5-Epieremophilene, an epimer of the versatile sesquiterpene (+)-valencene, is an inaccessible natural product catalyzed by three sesquiterpene synthases (SmSTPSs1-3) of the Chinese medicinal herb Salvia miltiorrhiz , and its biological activity remains less explored. In this study, three metabolically engineered Escherichia coli strains were constructed for (-)-5-epieremophilene production, with

The in situ application of iChip cultivation in mangrove sediment from Hainan province, China, led to the isolation of a novel bacterial species Gallaecimonas mangrovi HK-28. The extract of G. mangrovi HK-28 exhibited antibiotic activity against the aquatic pathogen Vibrio harveyi, and its chemical constituents were further investigated by bioactivity-guided isolation. Three new diketopiperazines,

(20S, 21S)-7-Cyclohexyl-21-fluorocamptothecin 6 was discovered by a fluorine drug design strategy with potent antitumor activity and increased metabolic stability. In continuous efforts to find novel antitumor agents derived from natural product camptothecin, 20-carbamates of active compound 6 have been designed and synthesized. Among them, compound 10g with diethyl group shows greater antiproliferative

In this study, total flavonoids and total triterpenoid acid were extracted with ethyl acetate from Hedyotis Diffusa Willd , hepatoprotective activities of them and five compounds from total flavonoids against H 2 O 2 induced hepatocyte damage on HL-02 was determined. In particular, amentoflavone and total flavonoids had influence on the leakage of ALT, AST, LDH, the activities of SOD and the content

Two chitosan extracts were prepared by chemical and enzymatic treatment of Ganoderma lucidum mushroom, as an alternative source to crustacean shells. The molecular weight of the enzymatic extract was lower than that of the chemical one and of shrimp chitosan, as determined by viscosity measurements. Characteristic signals were identified in the 1 H-NMR spectra and high deacetylation degree indicated

Six new eudesmane-type sesquiterpene derivatives, artemargyinins A-F ( 1 - 6 ) were isolated from the leaves of Artemisia argyi . Their structures were elucidated based on the extensive analysis of spectroscopic data. Compounds 1 - 6 feature a lactone ring-opening eudesmane-type sesquiterpene with an isoprenoid group at C(8). All compounds were tested for their inhibitory effects on lipopolysaccharide-induced

Three new diterpenoids (a cephalotane, an abietane and a 9(10→20)-abeo-abietane) and one new flavonoid, together with 11 known compounds, were isolated from the twigs of Cephalotaxus fortunei var. alpina. The new compounds were identified by comprehensive spectroscopic (including 1D and 2D-NMR and HR-ESI-MS) analysis. Anti-inflammatory, immunosuppresive and cytotoxic activities of three new compounds

Helicid suppresses inflammatory factors and protects nerve cells in the hippocampus of rats with depression, but the mechanisms underlying its protective effects are unclear at present. In this investigation, we conducted gene silencing, helicid intervention and rescue experiments to explore the protective actions of PNOC , the prepronociception gene known to regulate inflammatory processes, and helicid

A large number of biologically active compounds are present in ripe citrus fruits . However, few studies have been focused on the changes in flavonoids and the evolution of antioxidant activity during citrus fruit growth. In this study, fruits of five citrus cultivars cultivated in China were sampled at 60 - 210 days post-anthesis (DPA) at intervals of 30 days. The contents of main flavonoids in the

In this work we explored the possible polypharmacological potential of the already established antimicrobials against gastrointestinal pathogens, 4-(alkylamino)-3-nitrocoumarins, as antianxiety agents, using a battery of in vivo experiments. Three chosen coumarin derivatives, differing in the substituent (sec-butylamino, hexadecylamino, or benzylamino) at position 4, at the doses of 25, 50 and 100