A Standardized Composition Comprised of Extracts from Rosmarinus officinalis, Annona squamosa and Zanthoxylum clava-herculis for Cellulite - PubMed (original) (raw)

A Standardized Composition Comprised of Extracts from Rosmarinus officinalis, Annona squamosa and Zanthoxylum clava-herculis for Cellulite

Mesfin Yimam et al. Pharmacognosy Res. 2017 Oct-Dec.

Abstract

Background: Cellulite, characterized by changes in the skin morphology presented as dimpled or puckered skin appearance, is highly prevalent among postadolescent women. Cellulite management ranges from topical cream applications to invasive procedures. While some interventions showed improvements in physical appearances of affected areas, so far, none have reversed the condition to a full recovery. These unsuccessful measures signify the intricate nature of cellulite etiology highlighting its complexity leading to the possibility for a combination treatment approach to target multiple mechanisms.

Materials and methods: We screened our plant library for extracts that reduce cellular lipid accumulation, improve microcirculation, possess high total antioxidant capacity, significant anti-platelet aggregation, and anti-inflammatory activities using lipid accumulation assay in 3T3-L1 cells, Croton oil-induced hemorrhoid test in rats as a model for microcirculation, anti-platelet aggregation assay, nitric oxide (NO) inhibition assay, and 1,1-diphenyl-2-picrylhydrazyl assay.

Results: Three known botanicals such as Rosemary officinalis, Annona squamosa and Zanthoxylum clava-herculis were identified as lead extracts in these tests. Treatment of 3T3 cell with A. squamosa at 1 μg/ml resulted in 68.8% reduction in lipid accumulation. In croton oil-induced hemorrhoid study, Z. clava-herculis reduced the recto-anus coefficient by 79.6% at 6 mg/kg indicating improvement in microcirculations. Similarly, R. officinalis caused inhibition of 82%, 71.8%, and 91.8% in platelet aggregation, NO production and free radical generation at 31.25 μg/ml, 6.2 μg/ml, and 40 μg/ml concentrations suggesting its anti-oxidant, and anti-inflammatory activities.

Conclusions: Data depicted here suggest that formulation of these well-known botanicals at a specific ratio perhaps may yield a composition with a much wider spectrum of mechanisms of actions to impact the multiple pathways involved in cellulite onset, continuation, or exacerbations.

Summary: Cellulite represents one of the main esthetic concerns of women with a likely cause of psychological insecurities. Its pathophysiology involves multiple pathways that include vascular, adipose tissues, inflammation, structural and physiological.Treatment strategies for cellulite comprises increasing microcirculation flow, reducing lipogenesis, promoting lipolysis, free radicals scavenging or formation reduction, anti-inflammation and other invasive procedures.We screened our plant library for extracts that reduces cellular lipid accumulation, improves microcirculation, possesses high total antioxidant capacity, inhibits platelet aggregation, and moderates inflammation.Botanical extracts from Rosmarinus officinalis, Annona squamosa and Zanthoxylum clava-herculis were identified as leads and formulated to yield a standardized composition designated as UP1307 and suggested its usage for cellulite. Abbreviations Used: GMP: Good Manufacturing Practice; CA: Carnosic acid; NF-kB: nuclear factor-kB; HPLC: high-performance liquid chromatography; EtOH: Ethanol; DMEM: Dulbecco's modified Eagle's medium; FBS: fetal bovine serum; SD: Sprague Dawley; RAC: recto-anus coefficient; LPS: Lipopolysaccharide; DPPH: 1,1-diphenyl-2-picryl-hydrazyl; TNF-α: tumor necrosis factor; NO: Nitric oxide.

Keywords: Annona squamosa; Rosemary officinalis; Zanthoxylum clava-herculis; cellulite.

PubMed Disclaimer

Conflict of interest statement

There are no conflicts of interest.

Figures

Figure 1

Figure 1

Effect of Annona squamosa extract (RM606) on lipid accumulation. 3T3 L1 cells were treated with RM606 at 0.0625 μg/ml, 0.125 μg/ml, 0.25 μg/ml, 0.35 μg/ml, 0.5 μg/ml, and 1 μg/ml concentrations. Lipid droplets on cells were stained with Oil Red-O and measured at 510 nm on day 8. Data are expressed as percent inhibition of lipid accumulation

Figure 2

Figure 2

Effect of Zanthoxylum clava-herculis (UP342-C) on microcirculation improvement. Croton oil-induced hemorrhoid in rats was used as a disease model. Rats were administered with UP342-C suspended in Saline at oral doses of 0.67 mg/kg, 2.0 mg/kg, and 6.0 mg/kg 24 h after hemorrhoid induction. Control group is for the vehicle control (Saline). The recto-anus coefficient was determined 24 h posttreatment. Recto-anus coefficient was calculated using the formula: Weight of recto-anus (mg)/body weight (g)

Figure 3

Figure 3

Anti-platelet aggregation effects of Rosmarinus officinalis (RM504-C). Platelets were pre-incubated at 37°C for 2 min with RM504-C or vehicle (<0.1%) and then stimulated with collagen. The reaction mixture was incubated for 5 min. with stirring at 170 ×g. Aggregation was monitored by measuring light transmission in an aggregometer. Data are expressed as percent inhibition of aggregation

Figure 4

Figure 4

Nitric oxide inhibition effects of rosemary extract (RM504-C). Lipopolysaccharide (0.1 μg/ml) stimulated RAW264.7 cells were used to determine the over production of nitric oxide. Controls are unstimulated cells expected to have minimal to no production of nitric oxide. Cells were treated with RM504-C at 6.25–100 μg/ml concentrations. Data expressed as mean ą standard deviation of triplicates

Figure 5

Figure 5

Anti-oxidant effect of rosemary extract (RM504-C) in 1,1-diphenyl-2-picrylhydrazyl assay. The extract was tested at concentrations of 1, 5, 10, 20 and 40 μg/ml. The anti-oxidant activity is expressed as a percent inhibition

Similar articles

Cited by

References

    1. Hexsel D, Orlandi C, Zechmeister do Prado D. Botanical extracts used in the treatment of cellulite. Dermatol Surg. 2005;31:866–72. - PubMed
    1. Piérard GE. Commentary on cellulite: Skin mechanobiology and the waist-to-hip ratio. J Cosmet Dermatol. 2005;4:151–2. - PubMed
    1. Curri SB, Ryan TJ. Panniculopathy and fibrosclerosis of the female breast and thigh. Clin Dermatol. 1989;7:107–19. - PubMed
    1. Rossi AB, Vergnanini AL. Cellulite: A review. J Eur Acad Dermatol Venereol. 2000;14:251–62. - PubMed
    1. Goldman MP. Cellulite: A review of current treatments. Cosmet Dermatol. 2002;15:17–20.

LinkOut - more resources