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Investigation of the fruits of Rhododendron molle G. Don led to the isolation of three new grayanane-type diterpenoids, rhodomolleins LIV-LVI (1-3). The structures and absolute configurations of new compounds were fully elucidated by spectroscopic analysis and single-crystal X-ray diffraction, including HRESIMS, 1 D and 2 D NMR data. Compounds 1-3 were evaluated for analgesic activities utilizing an acetic acid-induced writhing test in mice. Compound 1 showed a significant antinociceptive effect with writhe inhibition rates of 72.9% and 100% at doses of 6 mg/kg and 20 mg/kg in mice, respectively. The binding mode of 1 to N-ethylmaleimide-sensitive factor (NSF, PDB: 6IP2) was explored by molecular docking, indicating the presence of hydrogen bond interactions which account for its analgesic activity. [ABSTRACT FROM AUTHOR]

A new 14-membered resorcylic acid lactone (RAL14), chaetolactone A (1), along with three known ones (2−4), was obtained from the fermentation of the soil-derived fungus Chaetosphaeronema sp. SSJZ001. Their structures were established based on extensive spectroscopic data analyses (UV, IR, HRESIMS, 1D, and 2D NMR),13C NMR chemical shifts calculations coupled with the DP4+ probability method, theoretical calculations of ECD spectra, as well as X-ray diffraction analysis. All compounds were evaluated for their cytotoxic effects against A549, HO-8910, and MCF-7 cell lines. [ABSTRACT FROM AUTHOR]

Polyether ether ketone (PEEK) is a biocompatible material that lacks antimicrobial activity and bioactivity; therefore, is not appropriate for use as a dental implant. To overcome these deficiencies, a novel composite coating of bioactive glass and graphene oxide was prepared. PEEK discs were polished, cleaned, and the surface treated with sulfuric acid for 15 min. The composite coating consisted of bioactive glass produced by the sol‐gel route and doped with 0.75 wt% graphene oxide. X‐ray diffraction, Fourier transform infrared spectroscopy, and scanning electron microscopy‐energy dispersive spectroscopy analyses were employed to characterize the composite coating, and the coating adhesion strength quantified using a pull‐off test. Cytotoxicity was assessed using osteoblast‐like cells and gingival fibroblasts. The wettability of the coated and non‐coated samples was determined by optical contact angle assessment, and bioactivity was assessed by immersion in simulated body fluid. The results revealed that the bioactive glass/graphene oxide composite coating, approximately 7 μm thick, was transparent, homogenous with few microcracks and microporosities, but adhered strongly and was not cytotoxic to either osteoblast‐like cells or gingival fibroblasts. The wettability of the PEEK sample was increased to <20° after coating with the composite, and apatite formation was detectable after 14 days of immersion in simulated body fluid. [ABSTRACT FROM AUTHOR]

Objective: This investigation evaluated the effect of two sintering modes of a translucent zirconia (Y‐TZP) on its surface roughness, topography, phase‐transformation (t → m), translucency and biaxial flexure fatigue strength. Materials and Methods: To do so, 50 Y‐TZP discs (Ø = 15 mm; thickness = 1.2 mm; IPS e.max ZirCAD LT) were prepared and divided into two groups: Standard mode (SM) and Fast mode (FM). Staircase fatigue testing was performed (piston‐on‐three balls set‐up, ISO 6872:2015), as well as surface roughness, profilometry, scanning electron microscopy (SEM‐FEG), energy dispersive X‐ray spectroscopy (EDX), phase transformation (t → m) using X‐ray diffraction analysis (XRD), translucency parameter analysis (TP and TP00) and fractography. Results: The results showed no statistical significant differences for roughness parameters (p > 0.05, SM: Ra = 0.13 ± 0.02, Rz = 1.21 ± 0.26 and RSm = 24.91 ± 2.19; FM: Ra = 0.14 ± 0.03, Rz = 1.32 ± 0.25 and RSm = 24.68 ± 2.16) or flexural fatigue strength (SM: 512 (464–560) MPa; FM: 542 (472–611) MPa) between the groups. In addition, similarity in surface morphological features (SEM and profilometry), composition and phases (EDX and XRD) was observed between the firing protocols. Fractography showed that the failure origin occurred on the tensile side. Sintering mode did not affect the TP (F = 0.001, p = 0.97) and TP00 (F = 0.12, p = 0.72). Conclusions: Therefore, the fast‐sintering mode is suggested as a viable alternative to the standard mode since it does not influence the evaluated surface morphology, microstructure, fatigue strength and translucency of a translucent monolithic zirconia. Clinical Significance: The fast sintering mode is a viable alternative for zirconia without compromising its topography, microstructure, mechanical performance or translucency. [ABSTRACT FROM AUTHOR]

Simple Summary: Radiation-based anticancer therapies are often ineffective as cancer cells may acquire radioresistance. Moreover, such therapies can cause unwanted side effects, affecting normal tissues. This problem may be remedied by the use of nanometric radiosensitizers. These compounds in non-toxic concentrations improve the effectiveness of therapy while reducing the total dose of radiation used. In this work, we checked the radiosensitizing properties of bimetallic palladium-platinum nanoparticles with different nanostructures: nano-alloy and core-shell. It has been found that nano-alloy structures are more promising radiosensitizers in vitro, and their effect is more satisfactory when using X-rays than high-energy protons. Thus, by appropriately designing the microstructure of nanomaterials, it is possible to modulate their radiosensitizing potential and enhance the therapy′s effectiveness. Nano-sized radiosensitizers can be used to increase the effectiveness of radiation-based anticancer therapies. In this study, bimetallic, ~30 nm palladium-platinum nanoparticles (PdPt NPs) with different nanostructures (random nano-alloy NPs and ordered core-shell NPs) were prepared. Scanning transmission electron microscopy (STEM), selected area electron diffraction (SAED), energy-dispersive X-ray spectroscopy (EDS), zeta potential measurements, and nanoparticle tracking analysis (NTA) were used to provide the physicochemical characteristics of PdPt NPs. Then, PdPt NPs were added to the cultures of colon cancer cells and normal colon epithelium cells in individually established non-toxic concentrations and irradiated with the non-harmful dose of X-rays/protons. Cell viability before and after PdPt NPs-(non) assisted X-ray/proton irradiation was evaluated by MTS (3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium) assay. Flow cytometry was used to assess cell apoptosis. The results showed that PdPt NPs significantly enhanced the effect of irradiation on cancer cells. It was noticed that nano-alloy PdPt NPs possess better radiosensitizing properties compared to PtPd core-shell NPs, and the combined effect against cancer cells was c.a. 10% stronger for X-ray than for proton irradiation. Thus, the radio-enhancing features of differently structured PdPt NPs indicate their potential application for the improvement of the effectiveness of radiation-based anticancer therapies. [ABSTRACT FROM AUTHOR]

A new aromatic glycoside (1) and twelve (2–13) known aromatic glycosides were isolated from the n-butyl alcohol of the 70% EtOH extract of the aerial part of Bupleurum chinense. Among them, compounds 4–7, 9, 11–13 were isolated from Umbelliferae plants for the first time. Their structures were elucidated by NMR and MS spectroscopy, and the absolute configuration of compound 1 was elucidated by single-crystal X-ray diffraction. Compounds 6 and 10 showed moderate cytotoxic activities on MGC-803 cell lines with IC50 values of 8.63 ± 0.08 and 13.65 ± 1.73 μM, respectively. [ABSTRACT FROM AUTHOR]

Four new ionones and ionone glycosides (1–4) were isolated from the whole plant of Rehmannia piasezkii Maxim. Their planar structures as well as absolute configuration were confirmed via spectroscopic analysis, ECD calculation, and X-ray crystallography. Compounds 1–4 were tested for their cytotoxicity against five human tumor cell lines and ability to inhibit LPS-activated NO production in the BV2 cell line. [ABSTRACT FROM AUTHOR]

Background: The present study was aimed at phyto-synthesized silver nanoparticles (AgNPs) using Amygdalus spinosissima ( A. spinosissima) extract and to investigate the antibacterial, antioxidant effects, anticancer and apoptotic effects of phyto-synthesized AgNPs. Methods: The bio-fabricated AgNPs were characterized using UV-visible spectroscopy (UV-visible), X-ray Diffraction (XRD), Fourier Transform Infrared (FTIR), Transmission Electron Microscopy (TEM), Scanning Electron Microscopy (SEM) and Energy Dispersive X-ray (EDX). Results: The phyto-synthesized AgNPs showed maximum absorption in 438 nm, in the UV-visible spectrum. XRD peaks were observed at 2θ values in 38.20°, 44.40°, 64.60°, and 77.50° which are indexed as (111), (200), (220), and (311) bands of Face-Centered Cubic (FCC) structures of silver. FTIR analysis indicated that the AgNPs were capped with A. spinosissima extract. SEM and TEM micrographs revealed that the fabricated AgNPs were spherical and the average size range was 17.89 nm. Also, the EDX results show that the content of Ag was 90%. Conclusion: The phyto-synthesized AgNPs had significant antibacterial activity against Gram-negative bacteria, as well as, the AgNPs exhibited great inhibitory effects on DPPH radicals and their antioxidant properties were favorably comparable to the antioxidant outcomes of ascorbic acid. Moreover, the AgNPs showed anticancer activity against the MCF-7 cell line with the IC50=6.1 µg/ml. Moreover, the phyto- synthesized AgNPs could induce apoptosis in the MCF-7 cell line significantly. The GC-MS analysis of the A. spinosissima extract showed that 102 bioactive phytochemical compounds, which be of use to the synthesis of AgNPs. [ABSTRACT FROM AUTHOR]

A comparison of the analysis of respirable crystalline silica direct-on-filter methods using X-ray diffraction (XRD) and Fourier transform infrared (FT-IR) spectroscopy was undertaken using 253 real workplace air samples from road construction and tunnelling, coal mining, and kitchen benchtop manufacturing in Australia. Using pure α-quartz standards, XRD and FT-IR direct-on-filter analyses produced identical test results, however, the real workplace samples showed a clear discrepancy between FT-IR and XRD results with on average a 9% positive bias of the FT-IR results. The cause of the positive bias was due to matrix interferences which was confirmed by using synthetic mixture air samples. Approximately a third of the data by direct-on-filter method using FT-IR was assessed to be invalid based on the peak height ratio criterion due to excessive interferences and weight overload limitations. The XRD method showed better results due to less interference from the common matrices. XRD could handle up to twice the sample loading and at higher loadings up to 7 mg when a correction was applied. It was also able to achieve a lower limit of detection of 2 µg filter−1 when a slower scan condition was utilized. [ABSTRACT FROM AUTHOR]

Five new Erythrina alkaloids and five known E. alkaloids were isolated from a 95% ethanol extract of the stems of Erythrina corallodendron L. Their chemical structures were elucidated by UV, IR, HRESIMS, NMR and X-ray. Furthermore, the analgesic activities of E. alkaloids 1, 2 and 6 were evaluated by using an acetic acid-induced writhing test in mice, and their writhing inhibition rates were 67.9%, 64.6% and 70.3% at doses of 20 mg/kg, respectively. [ABSTRACT FROM AUTHOR]

Phytochemical investigations of the twig and leaf extracts of Uvaria dac Pierre ex Finet & Gagnep. resulted in the isolation and identification of five new highly oxygenated cyclohexenes, uvaridacols M − Q (1 – 3 , 5 , and 6), and six known compounds (4 and 7 – 11). All new structures were elucidated by spectroscopic methods and HRESITOFMS data. The absolute configuration of 1 , 5 , and 6 was confirmed by single X-ray diffraction analysis with Cu Kα radiation. In contrast, other compounds were established by comparing their specific rotation and ECD spectra with those of known compounds. Some of the isolated compounds with sufficient quantity were evaluated for their α-glucosidase inhibitory activity. Of these, (−)-1,6-desoxypipoxide (10) showed α-glucosidase inhibitory activity with an IC 50 value of 28.6 μM. The in silico molecular docking of active compounds was also studied. Phytochemical investigations of the twig and leaf extracts of Uvaria dac Pierre ex Finet & Gagnep. resulted in the isolation and identification of five new highly oxygenated cyclohexenes and six known compounds. Some of the isolated compounds with sufficient quantity were evaluated for their α-glucosidase inhibitory activity. Of these, (−)-1,6-desoxypipoxide (10) showed α-glucosidase inhibitory activities with an IC 50 value of 28.6 μM. [Display omitted] • Five new oxygenated cyclohexenes were isolated from Uvaria dac. • The absolute configuration of uvaridacol M, P, Q were confirmed by single X-ray diffraction analysis with Cu Kα radiation. • Oxygenated cyclohexenes containing a cinnamoyl moiety, such as uvaridacols N and P first reported here. • 1,6-Desoxypipoxide showed α -glucosidase inhibitory activity. • 1,6-Desoxypipoxide was docked into α -glucosidase (PDB ID: 2QMJ) in silico molecular docking. [ABSTRACT FROM AUTHOR]

An extensive phytochemical investigation on the rare medicinal plant Semiliquidambar cathayensis (family: Hamamelidaceae) led to the isolation of four new (1 – 4 , named semiliquidacids A–D, respectively) and 25 related known pentacyclic triterpenoids. The new structures with absolute configurations were elucidated by spectroscopic methods, electronic circular dichroism (ECD) calculations, and single-crystal X-ray diffraction analysis. Compound 1 represents the first naturally occurring ursane-type triterpenoid featuring an uncommon C-25 formyl group. Compound 4 and oleanolic acid (13) exhibited remarkable inhibitory effects against the ATP-citrate lyase (ACL, an emerging drug target for hyperlipidemia and related metabolic disorders) with IC 50 values of 6.5 and 11.9 μM, respectively. The molecular interaction and binding mode between the bioactive triterpenoids and ACL were elaborated by conducting a molecular docking study. Meanwhile, the chemotaxonomic significance of the isolated triterpenoids has been briefly discussed. [Display omitted] • The rare medicinal plant Semiliquidambar cathayensis was phytochemically investigated. • Four new and twenty-five related known pentacyclic triterpenoids were reported. • Semiliquidacid A is a rare ursane-type triterpenoid featuring a C-25 formyl group. • Semiliquidacid D and oleanolic acid significantly inhibited the ATP-citrate lyase. • A molecular docking study was performed to provide an insight into the binding site. [ABSTRACT FROM AUTHOR]

Phytochemical investigation of the EtOAc soluble fraction from leaves of Trichilia dregeana Sond. (Meliaceae) afforded naturally rare four new pentacyclic triterpenoids (1 – 4), together with five known pentacyclic analogs (5 – 8 , and 11) and two steroids (9 and 10). Their structures were elucidated by extensive spectroscopic techniques such as 1D and 2D NMR and HRESIMS data analyses. The absolute configuration of 1 was determined by using the single-crystal X-ray diffraction analysis. The nitric oxide (NO) production inhibitory assay indicated that the EtOAc fraction as well as 4 and 7 inhibited the NO production in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophage cells with the IC 50 values of 83.53 μg/mL and 81.31 and 85.71 μM, respectively. Compounds 1 – 4 are rare 19(10 → 9) abeo -euphane-type triterpenoids bearing a 3,10-ether bridge. To the best of our knowledge, this study is the first isolation of triterpenoids with the 3,10-ether bridge in their skeleton from the genus Trichilia , providing new insights into the chemodiversity of the terpenoids in T. dregeana. [Display omitted] [ABSTRACT FROM AUTHOR]

Three Stemona alkaloids named stemotuberines A–C (1 – 3) with unique C 17 N frameworks, presumably formed by elimination of the C-11–C-15 lactone ring of the stichoneurine skeleton, were isolated from the roots of Stemona tuberosa. Their structures were elucidated by spectroscopic analysis, X-ray diffraction, and computational methods. Compounds 2 and 3 showed inhibition (IC 50 values of 37.1 and 23.2 μM, respectively) against LPS-induced nitric oxide production in RAW 264.7 cells. In addition, concern was expressed about the reported plant origin (S. sessilifolia) of the recently described alkaloids tuberostemonols O–R (4–7), which should be S. tuberosa. NMR calculations indicated structural misassignment of these compounds except for 6. Isolation of tuberostemonol P (5) from our material of S. tuberosa allowed for a close examination of the spectroscopic data leading to the revised structure 5a. Tuberostemonol R (7) was found to have identical 1H and 13C NMR data to the well-known alkaloid croomine, and therefore its structure including relative stereochemistry must be revised as 7a. [Display omitted] • Three previously undescribed Stemona alkaloids were isolated from Stemona tuberosa. • Compounds 1 – 3 possess unprecedented C 17 N skeletons. • Nitric oxide inhibitory activities of isolated compounds were evaluated. • Putative structures of tuberostemonols P and R were revised. [ABSTRACT FROM AUTHOR]

Phytochemical investigation on the extract of endophytic fungus Tolypocladium sp. SHJJ1 resulted in the identification of a pair of previously undescribed pyridoxatin atropisomers [ 1 ( M / P )] and three new indole diterpenoids (3 – 5), together with a pair of known pyridoxatin atropisomers [ 2 ( M / P )] and ten known indole diterpenoids (6 –1 5). Their structures, including their absolute configurations were elucidated by extensive spectroscopic analysis, quantum chemical calculations, and X - ray diffraction. Among the undescribed natural products, [ 1 ( M / P )] that two rapidly interconverting atropisomers are the third example to report in the pyridoxatin atropisomers. Except for compounds 1 ( M / P ) and 2 ( M / P ), all other compounds were tested for their cytotoxicity using HepG2, A549, and MCF-7 human cell lines. Compound 9 displayed moderate cytotoxicity against the HepG2, A549, and MCF-7 cell lines with IC 50 values of 32.39 ± 1.48 μM, 26.06 ± 1.14 μM, and 31.44 ± 1.94 μM, respectively, which was similar to the positive drug cisplatin (with IC 50 values of 32.55 ± 1.76 μM, 18.40 ± 1.43 μM, and 27.31 ± 1.22 μM, respectively). [Display omitted] [ABSTRACT FROM AUTHOR]

A phytochemical investigation on the buds of edible medicinal plant, Eugenia carvophyllata , led to the discovery of seven new compounds, caryophones A–G (1 – 7), along with two biogenetically-related known ones, 2-methoxy-7-methyl-1,4-naphthalenedione (8) and eugenol (9). Compounds 1 – 3 represent the first examples of C-5–C-1′ connected naphthoquinone-monoterpene adducts with a new carbon skeleton. Compounds 4 – 7 are a class of novel neolignans with unusual linkage patterns, in which the C-9 position of one phenylpropene unit coupled with the aromatic core of another phenylpropene unit. The chemical structures of the new compounds were determined based on extensive spectroscopic analysis, X-ray diffraction crystallography, and quantum-chemical calculation. Among the isolates, compounds (−)- 2 , 3 , 6 , and 9 showed significant in vitro inhibitory activities against respiratory syncytial virus (RSV)-induced nitric oxide (NO) production in RAW264.7 cells. [Display omitted] [ABSTRACT FROM AUTHOR]

Four undescribed ginkgolides, including two rare sesquiterpene ginkgolides (compounds 1 and 2) and two diterpenoid ginkgolides (compounds 3 and 4) , were isolated from Ginkgo biloba L. The structures of these four ginkgolides were identified based on extensive spectroscopic analysis, DP4+ probability analysis and X-ray diffraction. Compounds 1 and 2 exhibited excellent antiplatelet aggregation activities with IC 50 values of 1.20 ± 0.25 and 4.11 ± 0.34 μM, respectively. [Display omitted] [ABSTRACT FROM AUTHOR]

Background: Growing investigations demonstrate that graphene oxide (GO) has an undeniable impact on repairing damaged bone tissue. Moreover, it has been stated in the literatures that poly(2-hydroxyethyl methacrylate) (PHEMA) and gelatin could provide a biocompatible structure. Methods: In this research, we fabricated a scaffold using freeze-drying method comprised of PHEMA and gelatin, combined with GO. The validation of the successful fabrication of the scaffolds was performed utilizing Fourier-transform infrared spectroscopy (FTIR) and X-ray diffraction assay (XRD). The microstructure of the scaffolds was observed using scanning electron microscopy (SEM). The structural properties of the scaffolds including mechanical strength, hydrophilicity, electrical conductivity, and degradation rate were also evaluated. Human bone marrow‐derived mesenchymal stem cells (hBM-MSCs) were used to evaluate the cytotoxicity of the prepared scaffolds. The osteogenic potential of the GO-containing scaffolds was studied by measuring the alkaline phosphatase (ALP) activity after 7, 14, and 21 days cell culturing. Results: SEM assay showed a porous interconnected scaffold with approximate pore size of 50–300 μm, appropriate for bone regeneration. The increase in GO concentration from 0.25 to 0.75% w/v exhibited a significant improvement in scaffolds compressive modulus from 9.03 ± 0.36 to 42.82 ± 1.63 MPa. Conventional four-probe analysis confirmed the electrical conductivity of the scaffolds in the semiconductor range. The degradation rate of the samples appeared to be in compliance with bone healing process. The scaffolds exhibited no cytotoxicity using MTT assay against hBM-MSCs. ALP analysis indicated that the PHEMA–Gel–GO scaffolds could efficiently cause the differentiation of hBM-MSCs into osteoblasts after 21 days, even without the addition of the osteogenic differentiation medium. Conclusion: Based on the results of this research, it can be stated that the PHEMA–Gel–GO composition is a promising platform for bone tissue engineering. [ABSTRACT FROM AUTHOR]

Distraction osteogenesis (DO) is an efficient strategy that is employed for the treatment of large bone defects in craniomaxillofacial surgery. Despite its utility, however, DO is associated with a prolonged consolidation phase and a high complication rate that hinder its more widespread utilization. Panax notoginseng saponin (PNS) is a traditional Chinese medicine that is frequently administered for the treatment of a range of conditions. Herein, we explored the ability of PNS treatment to influence osteogenic differentiation using both rabbit bone marrow mesenchymal cells (BMSCs) and a model of mandibular DO. BMSC proliferation was assessed via CCK-8 assay, while osteogenic differentiation was monitored through ALP and alizarin red S staining. A PCR approach was used to evaluate the expression of genes associated with osteogenesis (ALP, Runx2, and OCN) and genes linked to the TGF pathway (TβR-II, SMAD2, SMAD3, and PPM1A). For in vivo experiments, treated BMSCs were locally injected into the DO gap, with PNS being injected into treated rabbits every other day throughout the experimental period. The quality of the regenerative process was assessed via scanning electron microscopy (SEM), energy dispersive spectroscopy (EDS), X-ray imaging, and hematoxylin and eosin (H&E) staining. These analyses revealed that PNS was able to promote BMSC osteogenesis and mandibular generation, driving the upregulation of osteogenesis-related genes at the mRNA levels through the modulation of the TGF-β1/Smad pathway. Consistently, the overexpression or silencing of TβR-II in PNS-treated BMSCs was sufficient to modulate their osteogenic potential. Analyses of in vivo mandibular DO outcomes revealed significantly augmented new bone growth in the PNS-treated group relative to control animals, with maximal osteogenesis in the group overexpressing rabbit TβR-II. Together, these results highlight the PNS as a promising and cost-effective therapeutic tool with the potential to enhance bone regeneration in clinical contexts through the modulation of the TGF-β1/Smad pathway. [ABSTRACT FROM AUTHOR]

Two novel fungal polyketides, phometides A (1) and B (2), together with four known compounds (3–6), were isolated from the endophytic fungus Phoma sp. YUD17001 obtained from Gastrodia elata Blume. The structures were elucidated based on spectroscopic analyses, X-ray crystal diffraction, and time-dependent density functional theory/electronic circular dichroism (TDDFT/ECD) calculations. Structurally, phometide A (1) represented the first example of C 12 polyketide characterized by an unusual tetrahydrobenzofuran-3(2 H)-one core with an α , β -unsaturated ketone functionality, while phometide B (2) was an unprecedented molecule containing a 2-pentylcycloheptan-1-one scaffold. In an antimicrobial activity assay, phometide A (1) exhibited significant inhibitory activity against Staphylococcus aureus with MIC value of 4 μg/mL. Phometide B (2) showed moderate antifungal activity against Candida albicans with an MIC value of 16 μg/mL. Furthermore, compounds 1 and 2 were evaluated for their acetylcholinesterase inhibitory and cytotoxic activities. [Display omitted] • Two novel fungal polyketides were identified from the endophytic fungus Phoma sp. YUD17001. • Phometide A possess an unusual tetrahydrobenzofuran-3(2 H)-one functionality. • Phometide B is a novel polyketone containing a 2-pentylcycloheptan-1-one scaffold. • Phometides A and B demonstrated antimicrobial activity against S. aureus and C. albicans , respectively. [ABSTRACT FROM AUTHOR]

A new alkaloid, Orychophragine D (1), together with three known alkaloids, were isolated from the seeds of Orychophragmus violaceus. Orychophragine D represented the first example of 2-piperazinone fused 5-azacytosine skeleton. Their structures and absolute configurations were determined by spectroscopic analyses and X-ray crystallography. Compared to Ex-RAD, compound 1 exhibited a significant radioprotective activity on cell survival of irradiated HUVEC. In vivo experiments showed that 1 not only remarkably enhanced the survival of irradiated mice in 30 days, but also significantly promoted the recovery of the blood system of irradiated mice. These results suggested that 1 was valuable for further research as promising radioprotectors. [Display omitted] [ABSTRACT FROM AUTHOR]

Ganoderpetchoids A−E and (−)-dayaolingzhiol H, six undescribed meroterpenoids, were isolated from Ganoderma petchii. Their structures including the relative configurations were identified by means of spectroscopic methods and 13C NMR calculations. Chiral separation of the new racemics was performed to afford their respective enantiomers. The absolute configurations of the new isolates were clarified by computational approaches, CD comparisons and X-ray diffraction analysis. Biological studies toward triple negative breast cancer indicated that (+)- 6 and (−)- 6 significantly inhibit the migration of MDA-MB-231 cell line. [Display omitted] [ABSTRACT FROM AUTHOR]

Seven rare noreudesmane sesquiterpenoids (dysoxydenones M-S, 1–7), including three 11,12,13-trinoreudesmanes, three 13-noreudesmanes and one spirovetivane-type sesquiterpenoid, along with two known analogues were isolated from the fruits of Dysoxylum densiflorum. The planar structures were elucidated by a combination of 1D, 2D NMR and HRESIMS analyses. Their absolute configurations were determined by combination of single-crystal X-ray diffraction, CD exciton chirality method and ECD calculation. All compounds were screened for anti-inflammatory activity on LPS-induced RAW 264.7 cells and IL-1 β inhibitory activity. [Display omitted] • Seven rare noreudesmane sesquiterpenoids were isolated from fruits of Dysoxylum densiflorum. • Compounds 1‐3 were 11,12,13-trinoreudesmanes, 4–6 were rare 13-noreudesmanes, and 7 was spirovetivane-type sesquiterpenoid. • Their absolute configurations were determined by single-crystal X-ray diffraction and CD exciton chirality method. [ABSTRACT FROM AUTHOR]

Three unprecedented indole alkaloids, wincalines A–C (1 – 3), and four known ones (4 – 7), classified into six carbon skeletal types, were isolated from the leaves of Winchia calophylla. The new isolates including their absolute configurations were elucidated based on extensive spectroscopic methods, the X-ray diffraction analyses, and electronic circular dichroism (ECD) experiments, as well as comparison with literature data. Wincaline A (1) is a rare indole alkaloid zwitterion bearing a 5,5-spirocyclic moiety. A possible biosynthetic pathway for 1 was proposed. All compounds were evaluated for their anti-inflammatory effects in terms of nitric oxide (NO) production in RAW 264.7 cells stimulated by lipopolysaccharide (LPS). Nevertheless, compound 7 showed weak activity with 43% NO production inhibition rate at 100 μM. [Display omitted] • Three new indole alkaloids were isolated from the leaves of Winchia calophylla. • Compound 1 is a rare indole alkaloid inner salt bearing a 5,5-spirocyclic moiety. • Their structures including the absolute configurations were fully assigned. • A possible biosynthetic pathway for 1 was proposed. [ABSTRACT FROM AUTHOR]

Cytospones E-J (1–6), six unreported α -pyrone derivatives, together with six known ones (7–12) were isolated from the solid culture of the endophytic fungus Cytospora rhizophorae A761, an endophytic fungus from Gynochthodes officinalis. The structures of the unreported compounds were unambiguously elucidated through spectroscopic analyses (1D, 2D NMR and HRESIMS), and their absolute configurations were assigned by single-crystal X-ray diffraction (Cu K α) analyses. Furthermore, cytospones E-J were evaluated for anti-inflammatory and α -glucosidase inhibitory activities. Cytospones E -J (1–6), six unreported α -pyrone derivatives with moderate anti-inflammatory and α -glucosidase inhibitory activities, were isolated from Cytospora rhizophorae A761. [Display omitted] • Six new α -pyrone derivatives were characterized from Cytospora rhizophorae. • The structures of novel compounds was extensively. • Compound 1 showed α -glucosidase inhibitory activity • Compounds 1 , 3 , and 6 displayed moderate anti-inflammatory activity. [ABSTRACT FROM AUTHOR]

Four new polyoxygenated cembranoids, namely sarcoboettgerol A (1), 12- epi -humilisin D (2), sarcoboettgerol B (3), and sarcoboettgerol C (4), together with one known related analogue, humilisin D (5), were isolated and characterized from the soft coral Sarcophyton boettgeri collected off Ximao island, Hainan Province, China. The structures and absolute configurations of the new compounds were determined by extensive spectroscopic data analyses, Cu k α single crystal X-ray diffraction analysis, and TDDFT-ECD calculations. A plausible biogenetic relationship of 3 and 4 was proposed. [Display omitted] [ABSTRACT FROM AUTHOR]

Four rare isotachin-derived, isotachins E -H (1 – 4), together with two known biogenetically related isotachin derivatives (5 and 6) were isolated from the solid rice fermentation of a fungus Penicillium tanzanicum ZY-5 obtained from a medicinal plant Dasymaschalon rostratum collected from the Changjiang County, Hainan Province, China. Their structures were elucidated using comprehensive spectroscopic methods. The single-crystal X-ray diffraction of compound 5 was determined. Compounds 1 – 4 have a trans-3-(methylthio)-acrylic acid fragment, which are rare in nature. The inhibitory activities of all compounds against the nitric oxide (NO) production induced by lipopolysaccharide in mouse macrophage RAW 264.7 cells in vitro were evaluated. [Display omitted] [ABSTRACT FROM AUTHOR]