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Thirteen cinnamic acid derivatives (1-13), including six formerly unreported hybrids incorporating different short-chain fatty acid esters (1-6), have been obtained and structurally elucidated from an ethnological herb Tinospora sagittata. The structures of them have been established by spectroscopic data analyses and NMR comparison with known analogs, while those of 1, 2, 4 and 6 have been further supported by total synthesis, and it is the first report of this type of metabolites from the title species. All the isolates have been assessed in an array of bioassays encompassing cytotoxic, antibacterial, anti-inflammatory, antioxidant, as well as α-glucosidase and HDAC1 inhibitory models. Compound 7 showed significant inhibitory activity against α-glucosidase, and half of the isolates also displayed moderate antiradical effect.

Chemical fractionation of the EtOH extract of the roots of a traditional Chinese herb, Morinda officinalis, afforded an array of methyl 2-naphthoate derivatives (1-9) including four pairs of enantiomers (1-4), two pimarane diterpenes and two ursane triterpenoids. Among them, eight compounds (1a/1b-3a/3b, 11 and 13) were reported in the current work for the first time. The structures of the new compounds, including their absolute configurations, were defined by spectroscopic analyses in combination with quantum chemical electronic circular dichroism (ECD) and gauge-independent atomic orbital (GIAO) NMR calculations. All the isolates were evaluated for their inhibitory effect on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in murine RAW264.7 macrophage cells, and the enantiomers 1a and 3b exhibited moderate activity with IC

Six aromatic compounds including a new (Z)-ferulic acid ester (1) and a new syringic acid ester (2), as well as four known ferulic acid esters (3–6), were isolated from a well-known edible mushroom, Pleurotus eryngii. Structures of these aromatics were unambiguously characterized via spectroscopic methods especially MS and NMR techniques. All the isolates were assessed for their antiradical effect and NO production inhibitory activity in RAW264.7 macrophages, and compounds 1 and 3 displayed mild DPPH radical removing activity, with IC50 values of 25.0 and 21.6 mM, respectively.

A pair of enantiomeric 15-nordolabellane diterpenoids, (-)- and (+)-caseadolabellols A (1a and 1b), three dolabellane diterpenoids, caseadolabellols B-D (2-4), two dolastane diterpenoids, caseadolastols A and B (5 and 6), 10 clerodane diterpenoids, caseakurzins A-J (7-16), and nine known diterpenoids (17-25) were isolated from the twigs and leaves of Casearia kurzii. The structures of the new compounds were established on the basis of extensive spectroscopic data, and those of compounds 1a, 1b, and 2 were verified by single-crystal X-ray crystallographic analysis. The enantiomers 1a and 1b were separated by chiral-phase HPLC. The absolute configurations were determined by experimental and calculated ECD data, the modified Mosher's method, or literature comparison. Compounds 1a and 5 showed significant quinone reductase-inducing activity in Hepa 1c1c7 cells, while 1b showed moderate activity. Molecular docking studies showed that 1a had greater binding affinity with Nrf2 protein (5FNQ) than 1b. The cytotoxic activity of compounds 1a, 1b, 2-12, 15, and 16 was evaluated, among which compounds 8 and 16 exhibited significant inhibitory activity against the A549 cell line. Compounds 8 and 16 induced the A549 cells to arrest at G2/M and S phases, respectively, and both compounds induced apoptosis in A549 cells.

The complete mitogenome sequence of Ochotona hyperborea was determined using long PCR. The genome was 17,063 bp in length and contained 13 protein-coding genes, two ribosomal RNA genes, 22 transfer RNA genes, one origin of L strand replication, and one control region. The overall base composition of the heavy strand is A (31.1%), C (28.7%), T (26.3%), and G (13.9%). The base compositions present clearly the A–T skew, which is most obvious in the control region and protein-coding genes. Mitochondrial genome analyses based on MP, ML, NJ, and Bayesian analyses yielded identical phylogenetic trees. This study verifies the evolutionary status of Ochotona hyperborea in Ochotonidae at the molecular level. The mitochondrial genome would be a significant supplement for the Ochotona hyperborea genetic background. The eight Ochotona species formed a monophyletic group with the high bootstrap value (100%) in all examinations.

Four new secoiridoid-iridoid heterodimers, pterocenoids E-H (1-4), together with a known analog (5), were separated from the whole plants of Pterocephalus hookeri. Their structures were characterized by detailed spectroscopic analyses and NMR comparison with reported data for known analogs. Pterocenoid E (1) represents the first bis-iridoid example incorporating a rare trans-fused monomeric unit, and the C(8) configuration in 5 was corrected to be reversed to the original assignment. Among all the isolates, compound 5 not only showed moderate inhibition against the nitric oxide production (IC

An in-fiber Michelson interferometer (MI) inclinometer, which consists of misalignment-spliced fiber with end coating, is proposed and experimentally demonstrated. The incident light divided at the misalignment-spliced joint is reflected at the end coating, and then re-coupled into the core of the fiber. Due to the phase difference between the core mode and the cladding mode, a typical Michelson interference is obtained. The fiber near the misalignment-spliced joint is inserted in two capillary quartz tubes. The inclination of the capillary quartz tube leads to a significant deformation and curvature of the misalignment-spliced joint, which causes the wavelength and amplitude of the MI spectrum to change. The experimental results indicate a good response within the angle range of 0º to 50º. Both the wavelength modulation and intensity modulation are realized, with sensitivities of 0.55 nm/deg and 0.17 dB/deg, respectively. Moreover, the sensor shows a strong orientation dependence due to the asymmetric structure in the misalignment-spliced joint.

Peritoneal metastases from invasive lobular carcinoma (ILC) of breast are uncommon and usually related to poor prognosis due to difficulty of detection in clinical practice and drug resistance. Therefore, recognizing the entities of peritoneal metastases of ILC and the potential mechanism of drug resistance is of great significance for early detection and providing accurate management. We herein report a case of a 60-year-old female who presented with nausea and vomiting as the first manifestation after treated with abemaciclib (a CDK4/6 inhibitor) plus fulvestrant for 23 months due to bone metastasis of ILC. Exploratory laparotomy found multiple nodules in the peritoneum and omentum, and immunohistochemistry confirmed that the peritoneal metastatic lesions were consistent with ILC. Palliative therapy was initiated, but the patient died two months later due to disease progression with malignant ascites. Whole exome sequencing (WES) was used to detect the tumor samples and showed the peritoneal metastatic lesions had acquired ESR1 and PI3KCA mutations, potentially explaining the mechanism of endocrine therapy resistance. We argue that early diagnosis of peritoneal metastasis from breast cancer is crucial for prompt and adequate treatment and WES might be an effective supplementary technique for detection of potential gene mutations and providing accurate treatment for metastatic breast cancer patients.

The SC200 proton therapy facility is consisting of a superconducting cyclotron, a gantry treatment room and a fixed beam room. The proton beams are transported mainly with beam transport devices, such as dipole magnets, quadrupole magnets, and corrector magnets which lie on the beam transport line layout of which is based on the beam optics design. A series of dipole, quadrupole, and corrector magnets ultimately make high-quality transmission of proton beams possible. Dipole magnets are mainly for beams deflection, quadrupole magnets are for beam focusing, and corrector magnets for orbit correction of beams. This paper shows the design of such magnets for the beam transport line. Besides, main parameters of magnets are presented and magnetic analysis work is also illustrated in this paper. The magnetic fields of dipole and quadrupole magnets are measured by hall mapping system and rotary coil measuring system. The results show that the measuring results are a little worse than the simulation results. However, both methods can meet the design requirement and the basic trend is similar to each other.

Five tigliane (

Five tigliane (1−5) and one ingenane (6) diterpenoids were isolated from the ethanol extract of Euphorbia tirucalli. The structures of these compounds were identified based on analysis of their spectroscopic data. Among them, compound 12-O-(2E,4E,6E,8E-tetradecatetraenoyl)-13-O-isobutyroyl-4β-deoxyphorbol (1) was a new tigliane. The Rho123 effluxion assay showed that tiglianes with a trans-fused 5/7 ring system such as compounds 1, 2, and 4 had potent inhibitory activity against P-glycoprotein in HepG2/ADR cells.

ObjectiveInvasive lobular carcinoma (ILC) and invasive ductal carcinoma (IDC) account for most breast cancers. However, the overall survival (OS) differences between ILC and IDC remain controversial. This study aimed to compare nonmetastatic ILC to IDC in terms of survival and prognostic factors for ILC.MethodsThis retrospective cohort study used data from the Surveillance, Epidemiology and End Results (SEER) Cancer Database (www.seer.cancer.gov). Women diagnosed with nonmetastatic ILC and IDC between 2006 and 2016 were included. A propensity score matching (PSM) method was used in our analysis to reduce baseline differences in clinicopathological characteristics and survival outcomes. Kaplan-Meier curves and log-rank test were used for survival analysis.ResultsCompared to IDC patients, ILC patients were diagnosed later in life with poorly differentiated and larger lesions, as well as increased expression of estrogen receptors (ERs) and/or progesterone receptors (PRs). A lower rate of radiation therapy and chemotherapy was observed in ILC. After PSM, ILC, and IDC patients exhibited similar OS (HR=1.017, p=0.409, 95% CI: 0.967–1.069). In subgroup analysis of HR-negative, AJCC stage III, N2/N3 stage patients, or those who received radiotherapy, ILC patients exhibited worse OS compared to IDC patients. Furthermore, multivariate analysis revealed a 47% survival benefit for IDC compared to ILC in HR-negative patients who received chemotherapy (HR=1.47, p=0.01, 95% CI: 1.09–1.97).ConclusionsOur results demonstrated that ILC and IDC patients had similar OS after PSM. However, ILC patients with high risk indicators had worse OS compared to IDC patients by subgroup analysis.

A pair of enantiomeric 15-nordolabellane diterpenoids, (-)- and (+)-caseadolabellols A (

Six new compounds including four prenylated indole alkaloids (1–4) and two lignans (5–6), along with eight known cometabolites (7–14), were isolated from the flower buds of Tussilago farfara. Structures of the new compounds were elucidated by comparison with structurally related known analogues and also by comprehensive spectroscopic analyses. Their absolute configurations were determined by a variety of means including Mosher's method, Marfey's analysis, electronic circular dichroism (ECD) exciton chirality method and ECD calculations. Our bioassays have established that compounds 1 and 2 showed potent α-glucosidase inhibitory activity with IC50 values of 105 ± 4.7 and 35.2 ± 3.2 μM, respectively, while the known 13 and 14 exerted moderate DPPH radical scavenging activity with IC50 values of 45.2 ± 2.9 and 29.2 ± 2.0 μM, respectively.

A total of 64 haplotypes were obtained from the complete Cytochrome b gene (Cyt b) of 77 Sorex isodon collected from three populations (Daxing'anling, Xiaoxing'anling, and Changbai Mountains) in Northeast China. The haplotype diversity was 0.9920 and the nucleotide diversity was 0.0105, indicating high genetic diversity. The genetic diversity of Changbai Mountains population was significantly higher than that of Daxing'anling and Xiaoxing'anling populations. The F-statistics, the number of migrants per generation and the genetic distance results showed that the genetic distances among the populations and among the sampling sites were generally consistent with geographical distance. Analysis of molecular variance showed that the differentiation among populations, among sampling sites, and within sampling site accounted for 33.4%, 10.2% and 56.4% of total variation, respectively. The analysis of population history showed that S. isodon in Northeast China experienced no population expansion. The reported complete sequence of Cyt b gene of S. isodon (GenBank) of Europe and other parts of Asia was downloaded to examine the genetic structure of S. isodon. The phylogenetic tree was divided into two large branches. One branch consisted mainly of Daxing'anling and Xiaoxing'anling samples. The other branch was departed into two sub-branches. Median-joining network analysis showed that there were three lineages: one lineage mainly consisted of haplotypes from Daxing'anling and Xiaoxing'anling, and also four haplotypes of Changbai Mountains, while the other lineage included a few haplotypes of three populations in Northeast China, and those from Baikal Lake, Russia and Finland. The last lineage was entirely composed of haplotypes from Changbai Mountains. The results of genetic diversity, phylogenetic tree and median-joining network all suggested that the Changbai Mountains was the refuge for S. isodon during last glacial.对中国东北地区3个种群(大兴安岭、小兴安岭和长白山山脉)的远东鼩鼱(77个样本)Cyt

Ten thiophene derivatives (1-10), including two previously undescribed ones (1 and 2), have been obtained and structurally characterized from the aerial parts of a traditional Chinese herb

Eight undescribed triterpenoids (pterohoonoids A-H) including four oleananes, one nor-oleanane and three nor-ursanes, along with seven known analogues, were isolated from the whole plants of Pterocephalus hookeri (Dipsacaceae). The structures with relative stereochemistries of these molecules were elucidated mainly by spectroscopic analyses, and the absolute configurations of the undescribed ones were assigned by a variety of methods, including time-dependent density functional theory (TD-DFT) based electronic circular dichroism (ECD) calculation, Rh

Nine new macrocyclic diterpenoids (1–9), jatromultones A-I, along with eight known analogues (10–17) were isolated from the trunks of Jatropha multifida. The structures of the new compounds, including their absolute configurations, were elucidated by combination of spectroscopic analysis, single crystal X-ray diffraction, Rh2(OCOCF3)4-induced CD method, and chemical correlations. All compounds were screened for the cytotoxicity against five cancer cell lines, including one drug-resistant cell line, and seven compounds exhibited significant activity with IC50 values less than 10 μM. Compound 4 with IC50 values ranging from 2.69 to 6.44 μM toward all cell lines was selected for further mechanistic study, which showed that 4 could arrest cell cycle at G2/M phase and induce apoptosis. The brief structure-activity relationships (SARs) of these macrocyclic diterpenoids were also discussed.

Twenty-seven monoterpene indole alkaloids (MIAs) including three new ones were isolated from the plant of Rhazya stricta. Their structures were elucidated by analyses of HRMS and NMR data. Secopleiocarpamine A (1) represents a novel 2,3-seco pleiocarpamine type MIA possessing a cyano group. A possible biosynthetic pathway for 1 was postulated. All compounds were evaluated for their inhibitory activities against six Candida strains, and the results showed that 2, 5, 12, 21, 23, and 27 exhibited moderate inhibitory activities with MIC values ranging from 3.125 to 50 μg/mL.

Bioassay-guided fractionation of the ethanolic extract of the roots of Euphorbia kansui led to the isolation of two new ingenane diterpenoids, euphorkans A (1) and B (2), together with 16 known analogues (3 – 18). Their structures were determined by combined spectral and chemical methods. All the isolates were evaluated for their inhibitory effects on lipopolysaccharide-induced nitric oxide production in RAW264.7 macrophage cells. Compounds 1 – 6 and 10 – 13 exhibited pronounced inhibitory activity with IC50 values in the range of 2.78 – 10.6 µM, and were more potent than the positive control, quercetin (IC50 = 15.8 µM). Compounds 1 and 5 were selected for further assays toward the key inflammation mediators TNF-α and IL-6, and showed a significant inhibition in a dose-dependent manner. The preliminary mechanistic study revealed that 1 and 5 inhibited NF-κB activity, which may exert a role in their anti-inflammatory activity.

Chemical fractionation of the EtOH extract of a medicinal macro fungus, Inonotus obliquus, afforded an array of lanostane-type triterpenoids (1-11) including two new ones (1 and 8). The structures of these compounds were determined on the basis of spectroscopic analyses, single crystal X-ray crystallography of 3-6 and biosynthetic considerations. With the confirmatory structural information provided by X-ray diffraction analysis in hand, several previously reported 21,24-cyclolanostanes, such as inonotsutriols A-C and (20R,21S,24S)-21,24-cyclopenta-3β,21,25-trihydroxylanosta-8-ene, were structurally corrected. In addition, the NMR data of other types of 21,24-cyclo triterpenoids were also re-examined and structural revisions were thus suggested. Compounds 2, 6 and 8 showed significant cytostatic effects against a panel of tumor cell lines with IC

Fifteen previously undescribed nor-clerodane diterpenoid glucosides tinosinesides C-Q (1-15), along with four known analogues (16-19), were isolated from the stems of Tinospora sinensis. The structures of the new compounds were elucidated by spectroscopic means, and their absolute configurations were established on the basis of time-dependent density functional theory (TD-DFT) based electronic circular dichroism (ECD) calculation and chemical methods. All the isolates were evaluated for their inhibitory effects on cystathionine γ-lyase (CSE), a natural enzyme responsible for the synthesis of H2S. Compounds 4 and 5 represent rare examples of natural CSE inhibitors and the possible binding mode to CSE was further probed by molecular docking experiment.

Ethnopharmacological relevance Salvia plebeia R. Brown, a traditional Chinese medicinal herb, has been used to treat inflammatory diseases such as cough, hepatitis, and diarrhea for a long history. Aim of the study The aim of the present study was to isolate and identify potential anti-inflammatory agents from the herb of S. plebeia, which may have contributed to its folk pharmacological use in the treatment of inflammatory diseases. Material and methods The aerial parts of S. plebeia were extracted with 95% ethanol and separated by silica gel, RP-C18, Sephadex LH-20, and HPLC. The structures of the isolated compounds were elucidated by extensive spectroscopic analysis (MS, NMR, and X-ray). Anti-inflammatory activities of all compounds were evaluated by the model of LPS-induced up-regulated of NO in Raw264.7 macrophages. The expression levels of cytokine (TNF-α) and proteins (iNOS and COX-2) were assessed by ELISA kit and Western blotting analysis, respectively. Furthermore, the influences of salviplenoid A (1) on NF-κB and MAPK signaling pathways were determined by Western blotting analysis and immunofluorescence assay. Results Six new (1−6, salviplenoids A–F) and ten known (7–16) sesquiterpenoids were isolated from the herb of S. plebeia. The absolute configurations of compounds 1, 2, and 7 were determined by X-ray diffraction. The new eudesmane-type sesquiterpenoid, salviplenoid A (1), significantly decreased the release of NO and TNF-α and the expression of proteins iNOS and COX-2. In addition, the biochemical mechanistic study indicated that 1 regulated the NF-κB dependent transcriptional activity through inhibiting the nuclear translocation of p50/p65 dimer and decreasing the phosphorylation of IκB and Erk1/2. Conclusions Among all sesquiterpenoids isolated from S. plebeian, the new salviplenoid A (1) exhibited the most potent anti-inflammatory activity in LPS-induced Raw264.7 cells via inhibition of NF-κB and Erk1/2 signaling pathways.

Chromatographic fractionation of the roots of Lindera aggregata has led to the isolation of three new monomers of Lindera cyclopentenedione derivatives (1–3), a pair of new enantiomers of bi-linderone derivatives (4a/4b), and six known Lindera cyclopentenediones (5–8 and 9a/9b). Their structures were determined by NMR and MS data. The absolute configurations of the new bi-linderone derivative enantiomers (4a/4b) were determined by ECD calculation. (±)-Lindepentone A (1) presents the novel skeleton of 3,5-dioxocyclopent-1-enecarboxylate. Lindoxepines A (2) and B (3) present an unprecedented oxepine-2,5-dione derivative skeleton, which may be enlightening for the in vivo biosynthesis of the monomers of Lindera cyclopentenediones. A possible biosynthetic pathway for 1 and a plausible biosynthetic pathway from stilbenes to Lindera cyclopentenediones via the key intermediates 2 and 3 were postulated. The inhibitory activity of these compounds against three microorganisms was also evaluated.

Six undescribed low-polarity compounds including three rare 14-methylergostane steroids (1-3), one euphane triterpenoid (4) and two octadecanoic acid ethyl esters (5 and 6), along with ten previously reported terpenyl cometabolites (7-16), were isolated from the stems of Tinospora sagittata. Their structures were determined by detailed spectroscopic analyses and comparison with structurally related known compounds, and all of them have been reported from T. sagittata for the first time. Compounds 4-6 and 16 showed potent in vitro inhibitory activity against the diabetes target α-glucosidase, while compounds 10 and 14 displayed promising antibacterial effect toward Staphylococcus aureus ATCC 25923.

Norhypersampsone A ( 1 ), a novel degraded polycyclic polyprenylated acylphloroglucinol (PPAP) derivative, 3-(2-hydroxy-7-methyl-3-methyleneoct-6-enyl)-5-isoprenyl-2,4,6-trihydroxybenzophenone ( 2 ), a new polyprenylated benzophenone derivative, and nine known compounds ( 3 – 11 ) were isolated from Hypericum sampsonii . Their structures were elucidated by comprehensive spectroscopic techniques. Compound 1 represents a novel cyclohexenone monocyclic-PPAP formed by losing the fragment of C-2–C-4 and the side chains at C-3 and C-5 in the phloroglucinol ring. The results of the inhibitory effects of compounds 1 – 11 on the nitric oxide (NO) production induced by lipopolysaccharide (LPS) in RAW 264.7 macrophages showed that compounds 1 , 6 – 8 , and 10 exhibited weak activities with IC 50 values in the range of 20.3–37.1 μM.

Two series of structurally related organoselenium compounds designed by fusing the anticancer agent methyl(phenyl)selane into the tubulin polymerization inhibitors isocombretastatins or phenstatins were synthesized and evaluated for antiproliferative activity. Most of these selenium containing hybrids exhibited potent cytotoxicity against a panel of cancel cell lines, with IC50 values in the submicromolar concentration range. Among them, 11a, the 3-methylseleno derivative of isocombretastatin A-4 (isoCA-4) represented the most active compound with IC50 values of 2–34 nM against 12 cancer cell lines, including two drug-resistant cell lines. Importantly, its phosphate salt, 11ab, inhibited tumor growth in xenograft mice models with inhibitory rate of 72.9% without apparent toxicity, which was better than the reference compounds isoCA-4P (inhibitory rate 52.2%) and CA-4P (inhibitory rate 47.6%). Mechanistic studies revealed that 11a is a potent tubulin polymerization inhibitor, which could arrest cell cycle ...

A finite element model of Boussinesq-type equations was set up, and a direct numerical method is proposed so that the full reflection boundary condition is exactly satisfied at a curved wall surface. The accuracy of the model was verified in tests. The present model was used to further examine cnoidal wave propagation and run-up around the cylinder. The results showed that the Ursell number is a nonlinear parameter that indicates the normalized profile of cnoidal waves and has a significant effect on the wave run-up. Cnoidal waves with the same Ursell number have the same normalized profile, but a difference in the relative wave height can still cause differences in the wave run-up between these waves. The maximum dimensionless run-up was predicted under various conditions. Cnoidal waves hold entirely distinct properties from Stokes waves under the influence of the water depth, and the nonlinearity of cnoidal waves enhances rather than weakens with increasing wavelength. Thus, the variations in the maximum run-up with the wavelength for cnoidal waves are completely different from those for Stokes waves, and there are even significant differences in the variation between different cnoidal waves.

Ten thiophene derivatives (1-10), including two previously undescribed ones (1 and 2), have been obtained and structurally characterized from the aerial parts of a traditional Chinese herb Eclipta prostrata. Six of them with one chiral center were identified to be scalemic mixtures, and the pure enantiomers of two isolates (1 and 3) were successfully separated via chemical derivatization and chiral HPLC, with the absolute configurations being established by analysis of optical rotations. All the thiophenes were subjected to a series of assays and compounds 9 and 10 exhibited mild antibacterial activity against Staphylococcus aureus.[Formula: see text].

Three new thiophene derivatives, ecliprostins A-C (1-3), have been isolated from the aerial parts of a Compositae medicinal plant Eclipta prostrata, and structures of them have been elucidated by comprehensive spectroscopic analyses. Both ecliprostins A (1) and B (2) feature an acetylenic bithiophenyl backbone and also incorporate an isovalerate moiety, while ecliprostin C (3) is a symmetrical dimer of compound 1 and represents the first example bonded via an ether bridge among the very limited natural dimers. All three compounds show antibacterial activity against Staphylococcus aureus.

Seven new diarylheptanoids, kravanhols C−I (1–7), along with two known analogues (8 and 9), were isolated from the fruits of Amomum kravanh. The structures of compounds 1–7 were elucidated by analysis of spectroscopic data, and the absolute configurations of selective ones were determined by time-dependent density functional theory (TD-DFT) based electronic circular dichroism (ECD) calculations. All compounds were evaluated for their inhibitory effects on the nitric oxide (NO) production induced by lipopolysaccharide (LPS) in murine RAW264.7 macrophage cells. Compounds 2, 5, 6 and 9 exhibited moderate inhibitory activity with IC50 values in the range of 17.4–26.5 μM, being more potent than the positive control dexamethasone (IC50 = 32.5 μM).

Seven previously undescribed polycyclic diterpenoids, euphonoids A−G, including four ent-abietanes, two ent-atisanes, and one ent-kaurene, along with 26 known analogues were isolated from the roots of Euphorbia fischeriana. The structures of the undescribed compounds were elucidated by spectroscopic analysis, ECD calculations, and single crystal X-ray diffraction. Besides, the structure of a previously reported ent-abietane diterpenoid, fischeriabietane A, was revised. All the isolates were screened for the cytotoxicities against five cancer cell lines. Euphonoid A, fischeriabietane A, 11-oxo-ebracteolatanolide B, caudicifolin, jolkinolide B, and methyl-8,11-3-dihydroxy-12-oxo-ent-abietadi-13,15(17)-ene-16-oate showed significant inhibitory activities against human prostate cancer C4-2B and C4-2B/ENZR cell lines, with IC50 values being less than 10 μM. The brief structure-activity relationships (SARs) of these diterpenoids were also discussed.

The phytochemical study of Euphorbia prolifera led to the isolation of two tiglianes (1 and 2) and 23 mysrinanes (3–25). Most of these isolates showed significant antiadipogenic activity in 3T3-L1 adipocyte without apparent cytotoxicity. Subsequent structural modification yielded 10 derivatives, among which 1a, the 5-O-acetyl derivative of 1, turned out to be the most active compound with improved triglyceride-lowering activity (EC50 for 1 and 1a: 0.61 and 0.32 μM, respectively) and reduced cytotoxicity (selectivity index for 1 and 1a: 28 and 312, respectively). The structure–activity relationship study revealed that the trans-fused 5/7/6 ring system in an angular shape was important to the activity. A mechanistic study indicated that 1 and 1a could inhibit the glucocorticoid receptor α-Dexras1 axis in adipocyte, leading to the retardation of cell differentiation at the early stage. These findings may provide a new type of lipid-lowering agents for future antiobesity drug development.