GC-MS-based metabolomics, antibacterial and anti-inflammatory investigations to characterize the quality of essential oil obtained from dried Xylopia aethiopica fruits from Ghana and Nigeria.

OBJECTIVES: This study sought to determine the quality of essential oil from Xylopia aethiopica fruits of different geographical origins using GC-MS-based metabolomics, bacterial quorum sensing and anti-inflammation assessment. METHODS: Essential oil was obtained from eight batches of X. aethiopica fruits from Ghana and Nigeria by hydrodistillation, characterized using gas chromatography-mass spectrometry and differences therein found using metabolomics. The respective antibacterial activity of the oils was tested against four bacterial strains: two Gram-positive strains, Staphylococcus aureus (ATCC 25923) and Bacillus licheniformis (ATCC12759), and two Gram-negative strains, Escherichia coli (ATCC25922) and Klebsiella pneumoniae (ATCC 13883). Anti-inflammation was tested using RAW 264.7 macrophage cells. KEY FINDINGS: The outcome of the study revealed that the oil of the Ghana-sourced samples exhibited superior antibacterial, cytotoxic and anti-inflammatory effects than those from Nigeria. This could be attributed to the higher levels of the bioactive compounds present in those samples. This distinction between the samples from the two countries was clearly established using the metabolomics approach, and 14 differential metabolites were found to be potential chemical markers. CONCLUSIONS: The study lends credence to the traditional uses of the essential oil of X. aethiopica as an antimicrobial and anti-inflammatory agent.

Anti-inflammatory and antipyretic properties of Kang 601 heji, a traditional Chinese oral liquid dosage form.

OBJECTIVE: To evaluate the scientific basis for the use of Kang 601 heji (K-601) as an anti-inflammatory and antipyretic agent using appropriate animal models. METHODS: Carrageenan-induced rat paw and xylene-induced ear oedemas were models used to investigate anti-inflammatory actions of K-601. Lipopolysaccharide-induced pyrexia model was used to evaluate antipyretic activity in Wistar rats. The anti-inflammatory and antipyretic mechanisms were evaluated by detecting prostaglandins E2, nitric oxide, interleukin-1ß and tumour necrosis factor-α levels using appropriate reagents and ELISA kits. RESULTS: The results revealed that K-601 reduced the level of inflammations in both anti-inflammatory models in a dose-dependent manner. The same was true for the antipyretic model. The possible mechanisms of actions were through the inhibition of prostaglandins E2, interleukin-1ß, tumour necrosis factor-α and nitric oxide. CONCLUSIONS: K-601 has proven anti-inflammatory and antipyretic actions. The findings provide a scientific basis for the use of K-601 as anti-inflammatory and antipyretic agent in traditional Chinese medicinal practice.

Anti-inlfammatory and antipyretic properties of kang 601 heji, a traditional Chinese medicine oral liquid dosage form

Objective:To evaluate the scientific basis for the use of Kang 601 heji (K-601) as an anti-inflammatory and antipyretic agent using appropriate animal models. Methods:Carrageenan-induced rat paw and xylene-induced ear oedemas were models used to investigate anti-inflammatory actions of K-601. Lipopolysaccharide-induced pyrexia model was used to evaluate antipyretic activity in Wistar rats. The anti-inflammatory and antipyretic mechanisms were evaluated by detecting prostaglandins E2, nitric oxide, interleukin-1βand tumor necrosis factor-αlevels using appropriate reagents and ELISA kits. Results:The results revealed that K-601 reduced the level of inflammations in both anti-inflammatory models in a dose-dependent manner. The same was true for the antipyretic model. The possible mechanisms of actions were through the inhibition of prostaglandins E2, interleukin-1β, tumor necrosis factor-αand nitric oxide. Conclusions: K-601 has proven anti-inflammatory and antipyretic actions. The findings provide a scientific basis for the use of K-601 as anti-inflammatory and antipyretic agent in traditional Chinese medicinal practice.

Novel pH-sensitive charge-reversal cell penetrating peptide conjugated PEG-PLA micelles for docetaxel delivery: in vitro study.

In order to create a pH-sensitive charge-reversal system for cell penetrating peptides (CPP) to prevent non-specific internalization of the drug; and concomitantly enhance the physical stability and tumor targetability of poly(ethylene glycol)-poly(d,l-lactide) (PEG-PLA) micelles, two sets of novel PEG-PLA micelles were developed. Cell penetrating decapeptide arginine-glycine (RG)5 and a pH-sensitive masking decapeptide histidine-glutamic acid (HE)5 were conjugated at the PEG free end to produce pH sensitive with peptides outside micelles (PHPO), while the pH sensitive with peptides inside micelles (PHPI) are the micelles obtained with the two peptides conjugated to the free end of the PLA block. The polymers were successfully synthesized and characterized by (1)H NMR and GPC. The mixed micelles were prepared and characterized for their loading efficiency, particle size and zeta potential. The surface charge of PHPO was greatly affected by the pH of the solution and (RG)5:(HE)5 ratio at the surface. The pH value of the solution at which the surface charge of PHPO reversed could be manipulated by the feed ratio of (RG)5-PEG-PLA (RGO) and (HE)5-PEG-PLA (HEO), hence, HEO:RGO molar ratio of 45:55 was selected for tumor targeting. Docetaxel (DTX) was sufficiently solubilized by DTX-PHPO with a loading efficiency of 90.18 ± 1.65%. At pH 7.4, DTX loaded mPEG-PLA (DTX-PM) (41.2 ± 0.3 nm), DTX-PHPO (195.3 ± 1.9 nm) and DTX-PHPI (190.9 ± 4.5 nm) showed sustained DTX release of less than 55% within 48 h. However, at pH 6.8 DTX-PHPI released 87.29 ± 0.24%, while DTX-PHPO released 70.49 ± 0.39% of the initial DTX amount within 48 h. Moreover, the physical stability of DTX-PHPO was increased due to the electrostatic interaction of the two peptides. The cellular uptake of DTX-PHPO in SGC-7901 cells and the cell killing effect tested on MCF-7 cells were enhanced by 2 folds at pH 6.8 compared to pH 7.4. Hence, DTX-PHPO is highly pH-sensitive in mildly acidic pH and exhibited higher internalization, but DTX-PHPI exhibited accelerated release. Meanwhile, both formulations displayed low internalization and release at pH greater than 7. This pH sensitive charge reversal design can offer a promising safe carrier using both CPPs and PEG-PLA micelles.