Preclinical studies indicate that INFLATIV, an herbal medicine cream containing Pereskia aculeata, presents potential to be marketed as a topical anti-inflammatory agent and as adjuvant in psoriasis therapy.

OBJECTIVES: A previous study reported that the hexane fraction (HF) obtained from Pereskia aculeata leaves showed promising topical anti-inflammatory activity. Intending its future use in clinical practice, a herbal medicine cream named INFLATIV was developed. Its anti-inflammatory and antipsoriatic potential were investigated. INFLATIV was subjected to preliminary accelerated stability tests and to a degradation profile assessment. METHODS: INFLATIV was prepared at 6% and 12%. The anti-inflammatory activity was assessed by croton oil single and multiple application challenge in mice. Mouse tail test was used for antipsoriatic potential investigation. Cutaneous atrophy test was performed. Preliminary accelerated stability tests were performed together with a degradation profile by GC-MS analysis. KEY FINDINGS: The anti-inflammatory activity shown by INFLATIV was comparable to dexamethasone. However, the skin atrophy caused by that drug was not observed. INFLATIV modified skin parakeratotic differentiation into orthokeratosis, which revealed its antipsoriatic potential. The ingredients used were suitable to carry the bioactives as they were well permeated by the skin. The preliminary accelerated stability tests indicated that INFLATIV 6% is more stable than 12%. CONCLUSIONS: The results demonstrated the relevant therapeutic and marketing potentials of INFLATIV, which is likely to be further evaluated in clinical trials for drug registration process with regulatory agencies.

Kalanchoe brasiliensis Cambess., a Promising Natural Source of Antioxidant and Antibiotic Agents against Multidrug-Resistant Pathogens for the Treatment of Salmonella Gastroenteritis.

Kalanchoe brasiliensis Cambess. is a native Brazilian plant popularly known as "saião", and the juice of its fresh leaves is traditionally used to treat several disorders, including inflammatory and infectious processes such as dysentery. The goals of this study were to characterize the phytochemical composition and investigate the antioxidant activity, the antibiotic effect, and the mode of action against Salmonella of the hydroethanolic extracts from K. brasiliensis leaves collected in the summer and spring Brazilian seasons. These extracts had their chemical composition established by high-performance liquid chromatography with diode-array detection. Total phenolic and flavonoid contents were spectrophotometrically determined. 2,2-Diphenyl-1-picryl-hydrazyl radical scavenging, phosphomolybdenum reducing power and ß-carotene bleaching assays were carried out to evaluate the antioxidant capacity. Antibiotic potential was assessed by minimal inhibitory concentration against 8 bacterial ATCC® and 5 methicillin-resistant Staphylococcus aureus and 5 Salmonella clinical strains. The mode of action was investigated by time-kill, bacterial cell viability, and leakage of compounds absorbing at 280 nm assays against Salmonella. Chromatographic profile and UV spectrum analyses suggested the significant presence of flavonoid type patuletin and eupafolin derivatives, and no difference between both periods of collection was noted. Significant amounts of total phenolic and flavonoid contents and a promising antioxidant capacity were observed. Hydroethanolic extracts (70%, summer and spring) were the most active against the tested Gram-positive and Gram-negative bacterial strains, showing the bacteriostatic action of 5000 µg/mL. Time-kill data demonstrated that these extracts were able to reduce the Salmonella growth rate. Cell number was reduced with release of the bacterial content. Together, these results suggest that K. brasiliensis is a natural source of antioxidant and antibacterial agents that can be applied in the research and development of new antibiotics for the treatment of Salmonella gastroenteritis because they are able to interfere in the Salmonella growth, probably due to cell membrane damage.

A promising antibiotic, synergistic and antibiofilm effects of Vernonia condensata Baker (Asteraceae) on Staphylococcus aureus.

Vernonia condensata Baker is traditionally used to treat several inflammatory and infectious processes. So, this study evaluated the antibiotic, synergistic and antibiofilm effects, and the mode of action of ethyl acetate fraction from V. condensata leaves (Vc-EAF) against Staphylococcus aureus. Five S. aureus ATCC® and five methicillin-resistant S. aureus (MRSA) routine strains were used to determine Minimal Inhibitory Concentration (MIC) and Minimal Bactericidal Concentration. The combinatory effect was evaluated by checkerboard and time kill methods; the mode of action through the bacterial cell viability and leakage of compounds absorbing at 280 nm; and the antibiofilm action by quantifying the percentage of adhesion inhibition. Vc-EAF was active against S. aureus (ATCC® 6538™), (ATCC® 25923™), (ATCC® 29213™), (ATCC® 33591™), (ATCC® 33592™), MRSA 1485279, 1605677, 1664534, 1688441 and 1830466, with MIC of 625 µg/mL for ATCC®, and 1250, 1250, >2500, 2500 and 2500 µg/mL for MRSA, in this order, with bacteriostatic effect for both ATCC® and MRSA strains. Vc-EAF plus ampicillin revealed a total synergic effect on MRSA 1485279, and Vc-EAF combined with chloramphenicol, a partial synergic action against S. aureus (ATCC® 29213™) and (ATCC® 25923™). The time kill data agreed with checkerboard results, and the treated cells number was reduced with release of bacterial content. An expressive bacterial adhesion inhibition for S. aureus (ATCC® 25923™) and MRSA 1485279 was detected. These results showed that V. condensata is a promising natural source of active substances against S. aureus, including multiresistant strains, interfering with their antibacterial growth and hampering their adhesion to surfaces.

Vernonia condensata Baker (Asteraceae): a promising source of antioxidants.

The present study evaluated the antioxidant potential of Vernonia condensata Baker (Asteraceae). Dried and powdered leaves were exhaustively extracted with ethanol by static maceration followed by partition to obtain the hexane, dichloromethane, ethyl acetate, and butanol fractions. Total phenols and flavonoids contents were determined through spectrophotometry and flavonoids were identified by HPLC-DAD system. The antioxidant activity was assessed by DPPH radical scavenging activity, TLC-bioautography, reducing power of Fe(+3), phosphomolybdenum, and TBA assays. The total phenolic content and total flavonoids ranged from 0.19 to 23.11 g/100 g and from 0.13 to 4.10 g/100 g, respectively. The flavonoids apigenin and luteolin were identified in the ethyl acetate fraction. The IC50 of DPPH assay varied from 4.28 to 75.10 µg/mL and TLC-bioautography detected the antioxidant compounds. The reducing power of Fe(+3) was 19.98 to 336.48 µg/mL, while the reaction with phosphomolybdenum ranged from 13.54% to 32.63% and 56.02% to 135.00% considering ascorbic acid and rutin as reference, respectively. At 30 mg/mL, the ethanolic extract and fractions revealed significant effect against lipid peroxidation. All these data sustain that V. condensata is an important and promising source of bioactive substances with antioxidant activity.

Antinociceptive and anti-inflammatory effects of ethanol extract from Vernonia polyanthes leaves in Rodents.

The ethanol extract from Vernonia polyanthes leaves (EEVP) was investigated for antinociceptive and anti-inflammatory effects at the doses (p.o.) of 100, 200 and 400 mg/kg in animal models. The extract reduced the number of abdominal contortions by 16.75% and 31.44% at a dose of 200 and 400 mg/kg, respectively. The results obtained showed that EEVP exerted a significant antinociceptive effect in the two phases of formalin. The EEVP increased the reaction time on a hot plate at the doses of 100, 200 and 400 mg/kg after 90 min of treatment. The paw edema was reduced by EEVP at the doses of 100, 200 and 400 mg/kg after 4 h of application of carrageenan. Doses of 200 and 400 mg/kg, administered 4 h before the carrageenan injection, significantly reduced the exudate volume (29.25 and 45.74%, respectively) and leukocyte migration (18.19 and 27.95%, respectively). These results suggest that V. polyanthes can be an active source of substances with antinociceptive and anti-inflammatory activities.

New approaches to clarify antinociceptive and anti-inflammatory effects of the ethanol extract from Vernonia condensata leaves.

The present study was aimed at evaluating the antinociceptive and anti-inflammatory effects of the ethanol extract from Vernonia condensata leaves in animal models, in order to afford a better understanding of these properties. The extract reduced the number of abdominal contortions at doses of 100 (51.00 ± 3.00), 200 (42.00 ± 2.98) and 400 mg/kg (39.00 ± 4.00). In formalin tests, a significant reduction in the licking time (p < 0.01) was observed in the first phase by 25.14 (200 mg/kg = 51.50 ± 4.44) and 31.15% (400 mg/kg = 48.00 ± 4.37). The doses of 100 (43.37 ± 5.15), 200 (34.62 ± 4.16) and 400 mg/kg (28.37 ± 3.98) inhibited (p < 0.001) the second phase. After 60 and 90 min of treatment, a dose of 400 mg/kg (10.13 ± 0.39 and 11.14 ± 1.33, respectively) increased the latency time. Doses of 200 and 400 mg/kg potentiated the sleeping time induced by diazepam, pentobarbital and meprobamate. The extracts (100, 200 and 400 mg/kg) showed anti-inflammatory effects by a decrease in paw edema. The extracts also reduced the exudate volume at the doses of 200 and 400 mg/kg. The leukocyte migration had significant effect (p < 0.001) at doses of 100, 200 and 400 mg/kg. The completion of additional experiments in the investigation of the antinociceptive and anti-inflammatory activities of V. condensata allowed a better understanding of the central and peripheral mechanisms involved.