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Introduction: Kaurane diterpenes, notably xylopic acid, have demonstrated important biological activities including analgesia, anti‐oxidant, antimicrobial and cytotoxicity. The fruits of Xylopia aethiopica have been reported to be a rich source of kaurane diterpenes. Objective: An analytical approach for detailed imaging and characterisation of selected kaurane diterpenes was developed using matrix‐assisted laser desorption/ionisation high‐resolution mass spectrometry (MALDI‐HRMS) imaging techniques and high‐performance liquid chromatography‐high resolution electrospray ionisation‐tandem mass spectrometry (HPLC‐HRESI‐MSn) studies, respectively. Methods: The images of the compounds were constructed based on selected ions from their HRESI–MS spectra. The matrix employed comprised a solution of α–cyano–4–hydroxycinnamic acid (HCCA) in acetonitrile–water with trifluoroacetic acid (TFA). HPLC–HRESI–MSn measurements were conducted on an LTQ–Orbitrap spectrometer equipped with a heated electrospray ionisation (HESI)–II source. Results: The analytical strategy adopted showed the spatial distribution of the compounds in the fruits of X. aethiopica based on the dominant ions at m/z 301.2163 [M + H – HOCOCH3]+ and m/z 399.1932 [M + K]+ for xylopic acid, m/z 317.2111 [M + H]+ and m/z 355.1670 [M + K]+ for 15–oxo–ent–kaur–16–en–19–oic acid and m/z 303.2319 [M + H]+ for ent–kaur–16–en–19–oic acid. The fragmentation patterns of the compounds were proposed based on the HRESI–MSn measurements. Conclusions: The study revealed the spatial variability, differential behaviours and specificity of the selected kaurane diterpenes in the fruit, seed and pericarp. The compounds under study were predominantly restricted to the pericarp of the fruit with trace amounts in the seed. The spatial distribution of selected kaurane diterpenes in the fruit, seed and pericarp of X. aethiopica was revealed using MALDI–MS imaging techniques. The compounds were predominantly restricted to the pericarp of the fruit. [ABSTRACT FROM AUTHOR]

Extracts of Chlorophora regia are frequently used in Ghana in traditional medicine. There is, however, no reported data on the chemical composition of the plant. Comprehensive phytochemical investigation of the stem bark of C. regia resulted in the isolation of three new prenylated 2-arylbenzofuran derivatives, regiafuran A–C ( 1–3 ), and one new prenylated flavonol ( 4 ), together with fifteen known compounds ( 5–19 ). Their structures were elucidated by combined spectroscopic analysis of their NMR and HRESI-MS n data. Compounds 1, 2, 5, 9 and 15 exhibited remarkable free radical scavenging properties with IC 50 values of 1.9 μg/ml, 2.4 μg/ml, 2.2 μg/ml, 2.1 μg/ml and 1.8 μg/ml, respectively, compared to the standard trolox (IC 50 1.1 μg/ml). The isolated compounds did not, however, show any anti-inflammatory potential when tested using a PGE 2 (prostaglandin E 2 ) competitive enzyme immunoassay. [ABSTRACT FROM AUTHOR]

Background: Fruit extracts of Xylopia aethiopica are used traditionally in the management of pain disorders including headache and neuralgia. An animal model of vincristine-induced sensory neuropathy was developed after repeated intraperitoneal injection in rats and used in the present work to study the effects of the ethanolic extract of X. aethiopica (XAE) and its diterpene xylopic acid (XA) in vincristine-induced neuropathic pain. Materials and Methods: Vincristine (0.1 mg kg-1 day-1) was administered during two cycles of five consecutive days to induce chemotherapy-induced neuropathic pain. Static tactile anti-allodynic, anti-hyperalgesic, and cold anti-allodynic effects of XAE (30-300 mg kg-1) and XA (10-100 mg kg-1) were assessed using Von Frey filaments of bending forces of 4, 8, and 15 g, the Randall-Selitto paw pressure test, and cold water (4.5°C), respectively. Results: Administration of vincristine caused the development of allodynia and hyperalgesia with no significant motor deficit, spontaneous pain, and foot deformity. XAE (30-300 mg kg-1) and XA (10-100 mg kg-1) exhibited anti-hyperalgesic, tactile, and cold anti-allodynic properties with XA exhibiting greater potency than XAE. Pregabalin (10-100 mg kg-1) used as control produced similar effect. Conclusion: These findings establish the anti-allodynic and anti-hyperalgesic effects of the ethanolic fruit XAE and its major diterpene XA in vincristine-induced neuropathtic pain. [ABSTRACT FROM AUTHOR]

Introduction: Kaurane diterpenes, notably xylopic acid, have demonstrated important biological activities including analgesia, anti-oxidant, antimicrobial and cytotoxicity. The fruits of Xylopia aethiopica have been reported to be a rich source of kaurane diterpenes., Objective: An analytical approach for detailed imaging and characterisation of selected kaurane diterpenes was developed using matrix-assisted laser desorption/ionisation high-resolution mass spectrometry (MALDI-HRMS) imaging techniques and high-performance liquid chromatography-high resolution electrospray ionisation-tandem mass spectrometry (HPLC-HRESI-MS n ) studies, respectively., Methods: The images of the compounds were constructed based on selected ions from their HRESI-MS spectra. The matrix employed comprised a solution of α-cyano-4-hydroxycinnamic acid (HCCA) in acetonitrile-water with trifluoroacetic acid (TFA). HPLC-HRESI-MS n measurements were conducted on an LTQ-Orbitrap spectrometer equipped with a heated electrospray ionisation (HESI)-II source., Results: The analytical strategy adopted showed the spatial distribution of the compounds in the fruits of X. aethiopica based on the dominant ions at m/z 301.2163 [M + H - HOCOCH 3 ] + and m/z 399.1932 [M + K] + for xylopic acid, m/z 317.2111 [M + H] + and m/z 355.1670 [M + K] + for 15-oxo-ent-kaur-16-en-19-oic acid and m/z 303.2319 [M + H] + for ent-kaur-16-en-19-oic acid. The fragmentation patterns of the compounds were proposed based on the HRESI-MS n measurements., Conclusions: The study revealed the spatial variability, differential behaviours and specificity of the selected kaurane diterpenes in the fruit, seed and pericarp. The compounds under study were predominantly restricted to the pericarp of the fruit with trace amounts in the seed., (© 2019 John Wiley & Sons Ltd.)

Background and Aim: Potentially life-threatening and unpleasant side effects associated with some analgesics have fueled the drive for the search for more analgesics with better side effect profiles. Geraniin, the most dominant secondary metabolite in the aqueous extract of the aerial parts of Phyllanthus muellerianus , has been shown to possess antinociceptive properties mediated partly by opioidergic mechanisms. The purpose of this study is to determine whether geraniin exhibits tolerance and if it is able to ameliorate withdrawal signs in naloxone-precipitated morphine withdrawal., Materials and Methods: After chronic treatment of mice with geraniin orally, the formalin test was used to ascertain whether tolerance will develop to its antinociceptive effects and if there is morphine-induced tolerance cross-generalization with geraniin. The effect of geraniin on naloxone-precipitated morphine withdrawal signs in morphine-dependent mice was also investigated., Results: Geraniin (3-30 mg/kg) did not produce any tolerant effects after chronic administration and there was also no cross-generalization with the tolerant effects of morphine. Geraniin did not induce withdrawal signs but significantly reduced the number of jumps in morphine-dependent mice., Conclusion: Geraniin does not produce any tolerant effects like morphine and also reduced the signs associated with naloxone-precipitated morphine withdrawal in mice., Competing Interests: Conflict of Interest: None declared.