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Paederia scandens (Lour.) Merr. is a traditional Chinese medicine, which mainly has the functions of analgesia, detoxification, anti-inflammatory and anticonvulsant. Modern studies show that the main chemical constituents of this plant are iridoids and volatile oil, which have biological activities such as analgesia, anti-inflammatory, hepatoprotection, renoprotection and antibacterial. This review highlights the chemical constituents and biological activities of P. scandens based on studies published in last decades and provides the references for the further development and utilization of this medicinal plant. [ABSTRACT FROM AUTHOR]

Polycystic ovary syndrome (PCOS) is a common metabolic disorder reproductive endocrine disease in puberty and women of childbearing age. At present, metformin is mainly used in clinical to treat PCOS. From recent researches, many natural products, such as flavonoids, alkaloids, cumarins, etc, showed curing effects on PCOS. These have been attracting more and more attention. By searching the researches from database of CNKI, PubMed etc, this paper aims at providing a reference for PCOS drug research and development. [ABSTRACT FROM AUTHOR]

The property theory is a unique principle instructing traditional Chinese doctors to prescribe proper medicines against diseases. As an essential part of it, the five-flavor theory catalogs various Chinese materia medicas (CMMs) into five flavors (sweet, bitter, sour, salty, and pungent) based on their taste and medical functions. Although CMM has been successfully applied in China for thousands of years, it is still a big challenge to interpret CMM flavor via modern biomarkers, further deepening its elusiveness. Herein, to identify the correlation between gut microbiota and CMM flavor, we selected 14 CMMs with different flavors to prepare their aqueous extracts, quantified the contained major chemical components, and then performed full-length 16S rRNA sequencing to analyze the gut microbiota of C57BL/6 mice administrated with CMM extracts. We found that flavones, alkaloids, and saponins were the richest components for sweet-, bitter-, and pungent-flavored CMMs, respectively. Medicines with merged flavors (bitter-pungent and sweet-pungent) displayed mixed profiles of components. According to gut microbial analysis, modulation of CMMs belonging to the same flavor on the taxonomic classification was inconsistent to an extent, while the functional sets of gut microbiota, co-abundance gene groups (CAGs), strongly and differentially responded to distinct flavors. Moreover, these correlations were in line with their pharmacological actions. Therefore, the gut microbial functional sets (CAGs) could act as the possible indicator to reflect CMM flavor, rather than the composition of microbial community. [ABSTRACT FROM AUTHOR]

Background. Acetaminophen-related hepatic injury (ARHI) is a kind of acute hepatic injury caused by overdosing acetaminophen, which is mainly related to toxic metabolite production, oxidative stress, and mitochondrial dysfunction. The extract of Paederia scandens (Lour.) Merr. (PSM) has the abilities of anti-inflammatory, antivirus, and antioxidation. Research studies showed that PSM could improve acute or chronic hepatic injury, while the mechanism of which is still indistinct. Methods. Here, the authors applied the approach based on serum metabonomics combined with network pharmacology to study the protection of PSM on ARHI rats. Results. 10 serum potential biomarkers were found to be closely related to ARHI by metabonomics, while 3 compounds (L-ascorbyl 2,6-dipalmitate, squalene, and tributyl O-acetylcitrate) and 3 targets (NOS2, MAOB, and PDE3A) were found that might be the potential active components and active site of PSM on treating ARHI by network pharmacology analysis. Furthermore, molecular biology strategy was performed to validate whether iNOS/NF-κB signaling pathway is the potential mechanism of PSM treating ARHI. Conclusions. This study indicated that PSM could ameliorate ARHI by iNOS/NF-κB signaling pathway. During ARHI treatment by PSM, L-ascorbyl 2, 6-dipalmitate, squalene, and tributyl O-acetylcitrate might be the potential active components, while the possible active site might be NOS2, MAOB, and PDE3A. [ABSTRACT FROM AUTHOR]

Tadehaginoside, an active ingredient isolated from Tadehagi triquetrum (Linn.) Ohashi (Leguminosae), exhibited various biological activities. However, the pharmacokinetics and tissue distribution which affect tadehaginoside's therapeutic actions and application remain elusive. To clarify the metabolism of tadehaginoside in vivo. The pharmacokinetics and tissue distribution of tadehaginoside and its metabolite p-hydroxycinnamic acid (HYD) were investigated using LC-MS/MS. Pharmacokinetic parameters were determined in 10 Sprague-Dawley rats divided into two groups, the intravenous group (5 mg/kg) and the oral group (25 mg/kg). For the tissue-distribution study, 20 rats were intravenously given tadehaginoside (5 mg/kg) before the experiment (n = 4). Biological samples were collected before drug administration (control group) and after drug administration. The linearity, accuracy, precision, stability, recovery and matrix effect of the method were well-validated and the results satisfied the requirements of biological sample measurement. Treatment with tadehaginoside via intragastric and intravenous administration, the calculated Cmax in rats was 6.01 ± 2.14 ng/mL and 109.77 ± 4.29 ng/mL, and Tmax was 0.025 ± 0.08 h and 0.08 h, respectively. The results indicated that the quick absorption of tadehaginoside was observed following intravenous administration, and tadehaginoside in plasma of rats with intragastric administration showed relatively low concentration may be due to the formation of its metabolite. Tissue-distribution study indicated that kidney and spleen were the major distribution organs for tadehaginoside in rats and there was no long-term accumulation in most tissues. These results could provide clues for exploring the bioactivity of tadehaginoside based on its pharmacokinetic characteristics. [ABSTRACT FROM AUTHOR]

Laurolitsine is an aporphine alkaloid and exhibits potent antihyperglycemic and antihyperlipidemic effects in ob/ob mice. To investigate the pharmacokinetics, tissue distribution and excretion of laurolitsine. A LC-MS/MS method was established and validated to determine laurolitsine concentrations in the biological matrix of rats (plasma, tissue homogenate, urine and faeces). 10 Sprague-Dawley (SD) rats were used for plasma exposure study: 5 rats were injected with 2.0 mg/kg of laurolitsine via the tail vein, and the other 5 rats were administered laurolitsine (10.0 mg/kg) by gavage. 25 SD rats used for tissue distribution study and 5 SD rats for urine and faeces excretion study: rats administered laurolitsine (10.0 mg/kg) by gavage. After administered, serial blood, tissue, urine and faeces were collected. Analytical quantification was performed by a previous LC-MS/MS method. The pharmacokinetics, bioavailability, tissue distribution and excretion of laurolitsine were described. The pharmacokinetic parameters of oral and intravenous administration with Tmaxwere 0.47 and 0.083 h, t1/2 were 3.73 and 1.67 h, respectively. Oral bioavailability was as low as 18.17%. Laurolitsine was found at a high concentration in the gastrointestinal tract, liver, lungs and kidneys (26 015.33, 905.12, 442.32 and 214.99 ng/g at 0.5 h, respectively) and low excretion to parent laurolitsine in urine and faeces (0.03 and 1.20% in 36 h, respectively). This study established a simple, rapid and accurate LC-MS/MS method to determine laurolitsine in different rat samples and successful application in a pharmacokinetic study. [ABSTRACT FROM AUTHOR]

A new cyclolanostane triterpenoid glycoside, soulieoside O (1), together with 25-O-acetylcimigenol-3-O-β-d-xylopyranoside (2) and cimigenol-3-O-β-d-xylopyranoside (3), was isolated from the rhizomes ofSouliea vaginata. Their structures were characterized by spectroscopic analysis and chemical methods. The new compound showed moderate inhibitory activity against three human cancer cell lines with IC50values of 9.3–22.5 μM. [ABSTRACT FROM PUBLISHER]

A new sesquiterpenoid quinone, Acyl hibiscone B (1), together with five known compounds, (R)-lasiodiplodin (2), (R)-de-O-methyllasiodiplodin, (3) dibutyl phthalate (4), (R)-9-phenylnonan-2-ol (5) and hibiscone B (6), was obtained from the stem tuber of Abelmoschus sagittifolius. The structure of compound 1 was elucidated by analysing its 1H and 13C NMR, 1H–1H COSY, HSQC, HMBC, NOESY and HR-ESI-MS values. Compound 1 showed significant cytotoxicity against Hela and HepG-2 human cancer cell lines. [ABSTRACT FROM AUTHOR]

Four new phenolic acids, clerodens A–D ( 1 – 4 ) possessing an unusual bicycle [2.2.2] octane moiety were isolated from the whole plants of Clerodendranthus spicatus . Their structures were elucidated by extensive spectroscopic methods, including NMR, MS, and ECD data. All isolates were evaluated for their anti-inflammatory activities on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7, and compound 4 showed significant inhibitory activities with IC 50 value of 6.8 μM. [ABSTRACT FROM AUTHOR]

Highlights: [•] Three new and four known cassane diterpenes were isolated from the seeds of Caesalpinia sappan. [•] The structures of the new compounds were determined by spectroscopic methods, in particular 2D NMR analysis. [•] The cytotoxicity of all the isolated compounds against a panel of human cancer cell lines was evaluated. [Copyright &y& Elsevier]

A new ursane-type triterpene, cymosic acid (1) together with two known compounds, 3β,19α-dihydroxy-2-oxo-12-ursen-28-oic acid (2) and 2α,19α-dihydroxy-3-oxo-12-ursen-28-oic acid (3), were isolated from Rosa cymosa Tratt. The structure of compound 1 was elucidated by analyzing its 1H and 13C NMR, 1H–1H COSY, HSQC, HMBC, NOESY, and HR-ESI-MS values. The three compounds were found to display moderate inhibitory activities against nitric oxide production in lipopolysaccharide-activated macrophage cell lines, RAW 264.7 cells. [ABSTRACT FROM AUTHOR]

Three new cassane-type diterpenes, neocaesalpin AF ( 1), neocaesalpin AG ( 2), and neocaesalpin AH ( 3), were isolated from the seeds of Caesalpinia minax Hance. Their structures were elucidated on the basis of extensive spectroscopic analyses. The partially hydrogenated lactone unit in a tetracyclic cassane diterpene in 2 is rarely encountered in the cassane diterpenes isolated from the genus Caesalpinia. All compounds were evaluated for their in vitro cytotoxic activities against HCT-8 and MCF-7 human cancer cell lines. [ABSTRACT FROM AUTHOR]

Abstract: Four novel diterpenes possessing rare five-membered peroxide ring, aphanaperoxides E–H (1–4), were isolated from stem bark of Aphanamixis polystachya. Their structures including the absolute configuration were elucidated by spectroscopic data and CD analysis. The cytotoxicities of the isolated compounds against a panel of human cancer cell lines were evaluated. [Copyright &y& Elsevier]

A new eudesmanolide sesquiterpene, atractylenolide IV (1), together with seven known compounds were isolated from the 70% aqueous acetonic extract of the whole plant ofSarcandra glabra(Chloranthaceae). Their structures were established by spectral analysis, mainly UV, IR, HRESI-MS, 1D and 2D-NMR experiments (HSQC, HMBC and NOESY). Compounds1–4showed no remarkable cytotoxic activity against Hela, HCT-8 and MCF-7 cancer cell lines with IC50 > 50 µg mL−1. [ABSTRACT FROM PUBLISHER]

Two new ent-3,4-seco-labdane diterpenoids, methylcallicarpate (1) and callicarpic acid (2), were isolated from the leaves of Callicarpa nudiflora Hook et Arn. Their structures and relative configurations were established by analysis of spectroscopic data. Their absolute configurations were assigned by the application of the CD technique for the first time among the ent-3,4-seco-labdane-type diterpenes. [ABSTRACT FROM AUTHOR]

Two new compounds, 1,3-bis(m-carboxylphenyl)-propan-2-one (1) and 2-(m-carboxylphenyl)-3-(m-carboxylbenzyl) succinic acid (2), were isolated from the barks of Cerbera manghas, and their structures were established on the basis of spectroscopic methods. [ABSTRACT FROM AUTHOR]

Two new phenylpropionic acid derivates, cerberic acids A (1) and B (2), were isolated from the bark of Cerbera manghas. Their structures were established on the basis of spectroscopic methods including IR, ESI-FT-ICR-MS, 1D and 2D NMR. Primary bioassays showed that compound 1 possessed weak cytotoxic activity against HepG2, MCF-7, and HeLa cell lines with IC50 values of 44.7, 52.3, 48.7μg/ml, respectively. [Copyright &y& Elsevier]

A series of novel caffeoylquinic acid derivatives of chlorogenic acid have been designed and synthesized. Biological evaluation indicated that several synthesized derivatives exhibited moderate to good lipid-lowering effects on oleic acid-elicited lipid accumulation in HepG2 liver cells. Particularly, derivatives 3d, 3g, 4c and 4d exhibited more potential lipid-lowering effect than the positive control simvastatin and chlorogenic acid. Further studies on the mechanism of 3d, 3g, 4c and 4d revealed that the lipid-lowering effects were related to their regulation of TG levels and merit further investigation. [ABSTRACT FROM AUTHOR]

Three novel furanoditerpenoids, norcaesalpinin J ( 1 ) featuring an unusual 20-norcassane hydroperoxide and phangininoxys B ( 2 ) and C ( 3 ) possessing cassane hemiketal skeletons, were isolated from the seeds of Caesalpinia sappan . Their structures were elucidated by extensive spectroscopic methods. All isolates were evaluated for the cytotoxic activities on three human cancer cell lines. [ABSTRACT FROM AUTHOR]

Abstract: Two novel diterpenes, norcaesalpinin I (1) featuring an unusual ring C-contracted dinorcassane and caesalpinin U (2) possessing a highly oxygenated furanocassane skeleton were isolated from the seeds of Caesalpinia minax. Their structures were determined by different spectroscopic methods. A plausible biosynthetic pathway of 1 was proposed. The cytotoxic activity of compounds 1 and 2 against HepG2 and HeLa human tumor cell lines was evaluated. [Copyright &y& Elsevier]