HPLC-PDA-MS and NMR characterization of a hydroalcoholic extract of Citrus aurantium L. var. amara peel with antiedematogenic activity.

The phytochemical profile of a hydroalcoholic extract of Citrus aurantium var. amara L. peel, used as herbal medicine, was characterized by HPLC-PDA-MS. Two di-C-glycosyl flavones (vincenin II and diosmetin 6,8-di-C-glucoside), a series of flavones (luteolin 7-O-neohesperidoside, rhoifolin, and neodiosmin), and flavanone (neoeriocitrin, naringin, and neohesperidin) 7-O-neohesperidosides and two methoxyflavones (nobiletin and tangeretin), commonly present in Citrus, were identified. Furthermore, brutieridin and melitidin, two 3-hydroxy-3-methylglutaryl flavanone glycosides, were also characterized along with rhoifolin 4'-glucoside and three coumarins (8,3'-ß-D-glucopyranosyloxy-2'-hydroxy-3'-methylbutyl-7-methoxycoumarin, merazin hydrate, and isomerazin). A preparative isolation procedure followed by NMR spectroscopy confirmed the proposed structures of the major flavonoids and identified the coumarins. The phenolic content was found to be 14.8 mg mL(-1), and naringin and neohesperidin were the compounds present in the highest concentration (3.6 and 2.6 mg mL(-1)). The extract of C. aurantium peel inhibited significantly (p < 0.05) both histamine- and dextran-induced edema in rats in a concentration-dependent manner (IC(50) = 119.6 and 118.3 mg kg(-1), respectively), providing evidence for the therapeutic use of C. aurantium var. amara peel.

Inhibition of human platelet aggregation in vitro by standardized extract of Wendtia calycina

Wendtia calycina (Griseb.) Griseb., Vivianiaceae, is a Paraguayan herbaceous plant commonly known as burrito. Our previous study indicated that burrito leaves are a very good source of phenylpropanoid glycosides, principally verbascoside. From W. calycina leaves, a standardized, water-soluble extract rich in phenylpropanoid glycosides (WSE) has been developed on an industrial scale to be used as a food supplement, cosmetic, phytomedicine, and ingredient of different formulations. In this study, we investigated the effect of the WSE on human platelet aggregation in vitro induced by adenosine diphosphate (ADP), epinephrine (EPN), collagen (COL) or arachidonic acid (AA). WSE, concentration-dependently, inhibited ADP and EP-induced human platelet aggregation (IC50 were 0.82±0.15 mg/mL and 0.41±0.02 mg/mL, respectively). It did not inhibit collagen-induced platelet aggregation, thus suggesting a selectivity for the ADP-induced platelet activation pathways.

De Marco Formula effectiveness as an adjunctive therapy to prevent infected ischemic diabetic foot amputation and reduce plasma fibrinogen.

BACKGROUND: De Marco Formula (DMF) is a new procaine chemical combination of Procaine HCl and polyvinylpyrrolidone. A prospective randomized controlled clinical trial demonstrated that infected ischemic diabetic foot treatment with DMF for 52 days as an adjuvant with conventional therapy reduced major amputations. OBJECTIVE: To evaluate the possible association of clinical effectiveness and plasma fibrinogen reduction with DMF therapy. METHODS: Adult patients, 24 male/23 female, suffering from infected ischemic diabetic foot ulcers were randomly assigned to receive conventional therapy alone (group A, N=24) or combined with DMF (receiving 0, 15 ml/kg day i.m.) for ten days and then twice a week until lesion healing or completion of 52 days (group B, N=23). Fibrinogen concentrations were determined before and after a ten-day treatment period. Treatment clinical responses were considered favorable if major amputations were not needed. Pre and post-treatment fibrinogen values were compared within each group and between groups. Differences were considered statistically significant for p<0, 05. RESULTS: Fifty percent of group A patients (12/24) and 21.7% of the Group B (5/23) showed unfavorable responses (a 56.6% reduction for group B). There were not statistical differences between pre and post-treatment fibrinogen within Group A (406.7±49.08 vs. 354.6±62.5, p=0,11). However, post-treatment values were significantly lower within Group B (298.9±15.24 vs. 487.1±49.08, p=0, 0016). Patients who showed favorable responses had statistically lower fibrinogen concentrations than those with unfavorable responses (280±5.1 vs. 310±7,1, p=0.002) within group B. CONCLUSION: DMF combined with conventional therapy for infected ischemic diabetic foot was associated with plasma fibrinogen decrease.

Clinical evaluation of De Marco formula as an adjunctive therapy for infected ischemic diabetic foot: a prospective randomized controlled trial.

BACKGROUND: De Marco Formula (DMF) is a novel formulation of procaine and PVP. OBJECTIVE: To assess the efficacy and safety of DMF as an adjunctive therapy for infected ischemic diabetic foot in a prospective randomized controlled clinical trial. METHODS: Adult patients, 39 male/ 79 female, were randomly assigned (59 patients/treatment group) to the conventional therapy alone (A) or plus DMF (0, 15 ml/kg .day i.m.) during ten days and them twice a week until healing of the lesions or completion of 52 days (B).The response to the treatment was considered favorable when an amputation was not needed even though a decrease of the wound area or complete healing was not shown. It was considered unfavorable when a major amputation was necessary because of worsening of the lesion (wound spreading to any magnitude greater than the initial one) or the appearance of new wounds in the same leg. RESULTS: Both groups were comparable with regard to age, sex, level of arterial occlusion, type of lesion, anatomic localization of lesions and previous surgical procedures. The cumulative percentage of unfavorable results was significantly lower after treatment B with respect to treatment A (25.4% vs. 45.8%; p= 0.02), for a reduction of 44.5%. Four slight adverse reactions were associated with DMF: vertigo and nausea at the 7th treatment administration (one patient), and headache and tachycardia at the 12th dose (another patient). Blood hemoglobin and leukocyte counts and serum alanine transaminase were not affected. CONCLUSION: The treatment with DMF for 52 days as an adjuvant for the conventional therapy was associated with a lower need for major amputations. It was also well tolerated and safe.