Phytotherapeutic Extracts Research Articles

Reduction of the in vitro toxicity of elevated concentrations of SPIONLA by its administration through PHBV/curcumin composite microspheres

Superparamagnetic iron oxide nanoparticles have been developed for various biomedical applications for decades. In this work, lauric acid-coated SPION (SPIONLA) were incorporated into poly (3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) at different ratios to produce composite microspheres, which were evaluated for their properties, including potential cytotoxicity. Additionally, a phytotherapeutic extract, curcumin, was loaded into the resulting microspheres to develop magnetic drug delivery capsules. The results show a significant improvement in the cytocompatibility after 7 days of SPIONLA administrated in cells through the composite microspheres compared to pristine SPIONLA. The composite also exhibited prolonged cumulative release of curcumin in a simulated body fluid environment. The results confirmed the efficacy of the mixture of PHBV and curcumin in attenuating potential side effects due to direct administration of high initial amounts of SPIONLA while maintaining magnetic properties in the resulting composite. The results add evidence to the potential of these composite devices for targeted drug delivery applications.

Preliminary data on the effect of a phytotherapeutic extract in small animal periodontitis

Preliminary data on the effect of a phytotherapeutic extract in small animal periodontitis

Determination of the potency of a novel saw palmetto supercritical CO2 extract (SPSE) for 5α-reductase isoform II inhibition using a cell-free in vitro test system.

BackgroundThe nicotinamide adenine dinucleotide phosphate-dependent membrane protein 5α-reductase catalyses the conversion of testosterone to the most potent androgen – 5α-dihydrotestosterone. Two 5α-reductase isoenzymes are expressed in humans: type I and type II. The latter is found primarily in prostate tissue. Saw palmetto extract (SPE) has been used extensively in the treatment of lower urinary tract symptoms secondary to benign prostatic hyperplasia (BPH). The pharmacological effects of SPE include the inhibition of 5α-reductase, as well as anti-inflammatory and antiproliferative effects. Clinical studies of SPE have been inconclusive – some have shown significant results, and others have not – possibly the result of varying bioactivities of the SPEs used in the studies.PurposeTo determine the in vitro potency in a cell-free test system of a novel SP supercritical CO2 extract (SPSE), an inhibitor of the 5α-reductase isoenzyme type II.Materials and methodsThe inhibitory potency of SPSE was compared to that of finasteride, an approved 5α-reductase inhibitor, on the basis of the enzymatic conversion of the substrate androstenedione to the 5α-reduced product 5α-androstanedione.ResultsBy concentration-dependent inhibition of 5α-reductase type II in vitro (half-maximal inhibitory concentration 3.58±0.05 μg/mL), SPSE demonstrated competitive binding toward the active site of the enzyme. Finasteride, the approved 5α-reductase inhibitor tested as positive control, led to 63%–75% inhibition of 5α-reductase type II.ConclusionSPSE effectively inhibits the enzyme that has been linked to BPH, and the amount of extract required for activity is comparatively low. It can be confirmed from the results of this study that SPSE has bioactivity that promotes prostate health at a level that is superior to that of many other phytotherapeutic extracts. The bioactivity of SPSE corresponds favorably to that reported for the hexane extract used in a large number of positive BPH clinical trials, as well as to finasteride, the established standard of therapy among prescription drugs. Future in vitro and clinical trials involving SPEs would be useful for elucidating their comparative differences, as well as appropriate patient selection for their use.

Phytotherapeutic interventions in the management of biochemically recurrent prostate cancer: a systematic review of randomised trials.

To evaluate the evidence from randomised trials for the efficacy and safety of phytotherapeutic interventions in the management of biochemically recurrent (BCR) prostate cancer, indicated by prostate-specific antigen (PSA) progression, numbers progressing to/time to initiation of androgen-deprivation therapy or salvage therapy. MEDLINE (Ovid), EMBASE (Ovid), AMED (Ovid), CINAHL (EBSCO) and the Cochrane Library databases were searched. Clinical trials investigating phytotherapeutic interventions as dietary supplements or dietary components, including multi-component herbal formulations, in men with BCR prostate cancer were located. Eight of nine authors contacted for further information responded. Methodological quality was assessed using the Cochrane Collaboration's risk of bias assessment tool. The Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) statement for reporting systematic reviews was followed. Of 23 full-text articles assessed for eligibility, five met the criteria for inclusion. Two studies were placebo controlled; two were active control trials; and one a high-/low-dose trial. The interventions were administered as isolated phytochemicals (sulphoraphane), phytotherapeutic extracts [Pomi-T (pomegranate, turmeric, green tea and broccoli sprout extract), soy, lycopene, and POMx (pomegranate extract)], or plant-derived dietary items (soy and lycopene). All studies found serum PSA levels to stabilise, decrease or rise more slowly in a significant number of men, and three studies reported stabilising or lengthening of PSA-doubling time. Studies were generally of good quality, but sample sizes were predominantly small, and durations short. High-quality studies in this area are lacking. Sulphoraphane, lycopene, soy isoflavones, POMx, and Pomi-T are safe and well tolerated. There is limited evidence that they can affect PSA dynamics. No recommendation can be made for the use of these agents in managing prostate cancer morbidity and mortality until high-quality, fully powered studies are available. Recommendations are made for improving reproducibility and translation of findings with regard to study population, study endpoints, design, and the reporting of phytotherapeutic interventions.

Research on the evolution of blood biochemical parameters in calves treated with phyto-therapeutic extracts

Research on the evolution of blood biochemical parameters in calves treated with phyto-therapeutic extracts

Oral bioavailability of silymarin phytocomplex formulated as self-emulsifying pellets

The objective of this study was to develop new solid self-emulsifying pellets to deliver milk thistle extract (silymarin). These pellets were prepared via extrusion/spheronisation procedure, using a self-emulsifying system or SES (Akoline MCM®, Miglyol®, Tween 80®, soy lecithin and propylene glycol), microcrystalline cellulose and lactose monohydrate. To select the most suitable formulations for extrusion and spheronisation, an experimental design of experiences was adopted. The screening amongst formulations (13 different blends) was performed preparing pellets and evaluating extrusion profiles and quality of the spheronised extrudates. The pellets were characterised for size and shape, density, force required to crush them. Although more than one type of pellets demonstrated adequate morphological and technological characteristics, pellets prepared from formulation 7 revealed the best properties and were selected for further biopharmaceutical investigations, including in vitro dissolution and in vivo trials on rats to study serum and lymph levels after oral administration of the pellets. These preliminary technological and pharmacokinetic data demonstrated that extrusion/spheronisation is a viable technology to produce self-emulsifying pellets of good quality and able to improve in vivo oral bioavailability of main components of a phytotherapeutic extract of more than 100 times by enhancing the lymphatic route of absorption.

Non-estrogenic approaches for the treatment of climacteric symptoms

Non-estrogenic alternatives for the treatment of climacteric symptoms have their origin lost in history. Recent clinical trial data have shown that lifestyle and diet adjustment have some effect in improving both hot flushes and mood.Over-the-counter phytotherapeutic extracts are very popular and women often try a variety of products before resorting to traditional medicine. Preparations containing isoflavones in variable doses, such as soy extract and red clover, or extracts from evening primrose, Cimifuga racemosa, ginseng and black cohosh are often used for treating the climacteric syndrome. The scientific support for their efficacy certainly does not equal their popularity.The most tested pharmacological alternatives to estrogens are serotonin reuptake inhibitors (SSRIs). All available SSRIs have undergone trials for the relief of hot flushes. In spite of the difference between the compounds in both half-life and engagement of serotonin receptors, they appear to have very similar effectiveness in reducing hot flushes. At their best, SSRIs reduce hot flushes by 50–60%, compared with 80% for estrogen, and their effect appears only in the short term. SSRIs have mood-improving effects that appear to be independent of the effect on hot flushes. When used for the treatment of the climacteric syndrome, SSRIs do not adversely affect libido. Dependence is a major concern in women when offered this type of treatment, but does not appear to be a problem with this class of drugs. Withdrawal symptoms have never been reported in trials for hot flushes but are known to occur when SSRIs are used in the long term. In order to avoid these symptoms, the dose should be tapered slowly. Gabapentin, a drug used for the treatment of neuropathic pain and epilepsy, has shown that, in high doses, it has an efficacy similar to that of estrogen; however, this needs further confirmation.

A phytotherapeutic extract of Equisetum myriochaetum is not genotoxic either in the in vivo wing somatic test of Drosophila or in the in vitro human micronucleus test

Equisetum myriochaetum is a Mexican plant used in folk medicine to treat kidney diseases and type 2 diabetes mellitus. The main constituents of the phytoextract are flavonol glycosides (kaempferol), phytoesterols and carbohydrates. In this study, phytotherapeutic extracts from Equisetum myriochaetum were investigated for genotoxicity in the in vivo wing spot test in Drosophila melanogaster and in the in vitro human micronucleus test. No acute toxicity of the phytoextract could be determined in Drosophila or in human lymphocytes in culture, ranging from 0.78 μg/ml to 3700 μg/ml for the wing assay and between 12.5 μg/ml and 500 μg/ml for the micronucleus test. The Drosophila wing somatic mutation and recombination test (SMART) was applied in the standard version with basal biotransformation activity as well as in a variant version with increased cytochrome P450-dependent bioactivation capacity. The ranges of exposure concentrations for these genotoxicity experiments were between 0.78 μg/ml and 500 μg/ml. The human micronucleus test in vitro was performed with cultured lymphocytes obtained from four healthy donors. The concentrations assayed for these experiments ranged from 12.5 μg/ml to 500 μg/ml. No statistically significant increase was observed between treated series when compared with a concurrent negative (water solvent) control series in either assay. The results demonstrate clearly that the phytotherapeutic extract from Equisetum myriochaetum, under the experimental conditions tested, is not genotoxic in the in vivo experiments or in the in vitro studies.

A Review of Non-Hormonal Options for the Relief of Menopausal Symptoms

The climacteric syndrome involves a variety of symptoms such as profuse sweating, insomnia, memory loss, decreased sexual drives, joint aches, and anxiety. However, amongst these symptoms, hot flashes and sweats are generally considered the hallmark and result in the majority of the medical consultations for this condition. Hot flashes are known to respond readily to placebo, which alone decreases their frequency by 20-40%. In the ideal setting of clinical trials, with optimal patient selection and compliance, estrogen therapy reduces hot flashes by about 70-80%; this is twice as effective as placebo. However, estrogen is unable to be universally used, either because of contraindications or because of an unwillingness of women to take it. Furthermore, hot flashes may persist in spite of adequate estrogen replacement, and physicians are often faced with the dilemma of finding something to administer in place of, or in addition to, estrogen to improve symptoms. The most commonly used non-hormonal alternatives for climacteric symptoms are neurotransmitter modulators such as serotonin reuptake inhibitors and gabapentin. These are, at best, approximately half as effective as estrogen for the relief of menopausal symptoms, and are only marginally better than placebo.Complementary treatment, particularly over-the-counter phytotherapeutic extracts, are very popular and women often try a variety of such products before resorting to conventional medicine. Preparations containing isoflavones, such as soy extract and red clover or extracts from evening primrose or cimicifuga (black cohosh, Actaea racemosa, syn. Cimicifuga racemosa), in variable doses are very popular for the treatment of hot flashes. The scientific support for their efficacy certainly does not equal their popularity.Non-hormonal treatments for menopause are not as effective as estrogens in relieving hot flashes, but may have a role in therapy for women who have contraindications to gonadal steroid use.

Pharmacological therapy of benign prostatic hyperplasia/lower urinary tract symptoms: an overview for the practising clinician.

Less than 10 years ago surgery and watchful-waiting were the only widely accepted management options for lower urinary tract symptoms (LUTS) suggestive of benign prostatic hyperplasia (BPH) and benign prostatic obstruction (BPO). There has been an enormous decline in the popularity of surgery and it is now apparent that medication is the most frequently used treatment for BPH/LUTS; this has arguably therefore been the most major change in urological clinical practice in the last decade. Currently alpha(1)-adrenoceptor antagonists are the commonest medical therapy, and are thought to act by relaxing prostatic smooth muscle, the neural or so-called 'dynamic' component of BPO. 5alpha-reductase inhibitors (finasteride, dutasteride) are another option for BPH/LUTS, which reduce prostatic mass and therefore the mechanical or 'static' component of BPO. In the last 10 years there have been four direct comparative studies between alpha(1)-adrenoceptor antagonists and finasteride, including their combination, the results of which, and their implications for therapy, are discussed. Another group of agents are the phytotherapeutic extracts, which act via various mechanisms, many as yet poorly defined. This review critically assesses existing publications relating to the medical management of BPH/LUTS.

Absence of genotoxicity of a phytotherapeutic extract from Stryphnodendron adstringens (Mart.) Coville in somatic and germ cells of Drosophila melanogaster.

Stryphnodendron adstringens (Mart.) Coville, a medicinal plant that grows in the "cerrados" (a savanna ecosystem) of Brazil, popularly known as "Barbatimão," is an important source of tannins (polyphenols). In Brazil, it is used in industry (mainly as vegetable tanning) and also in traditional medicine for the treatment of various diseases. In the present study, a phytotherapeutic extract from S. adstringens stem bark was evaluated for mutagenic and recombinagenic effects using the wing spot test of Drosophila melanogaster (somatic mutation and recombination test, SMART), and for chromosome damage in germ cells using the Drosophila sex-chromosome loss test (ring-X loss). For SMART, the standard as well as the high bioactivation fly crosses were used; the latter cross is characterized by a high sensitivity to promutagens and procarcinogens. Third-instar larvae from these two crosses were treated for 48 hr with different concentrations (66%, 75%, and 100%) of the phytotherapeutic extract. The wings of the emerging adults were analyzed for the occurrence of different types of mutant spots. No statistically significant differences in spot frequencies between controls and treated series were observed. For the ring-X loss test, adult males were fed with the same concentrations of the extract as in the wing spot test. No statistically significant increases in ring-X losses were observed. The results of our experiments suggest that the phytotherapeutic extract from S. adstringens stem bark is not genotoxic in somatic and germ cells of D. melanogaster.

High-performance liquid chromatographic determination of the biologically active principle hypericin in phytotherapeutic vegetable extracts and alcoholic beverages.

Hypericin was determined using an RP C18 (3 microns) column 8.3 x 0.4 cm I.D.), thermostated at 50 degrees C. The separation was achieved with programmed elution using phosphate buffer (pH 7)-methanol (3:7) and watermethanol (3:7) as eluents. Fluorimetric detection was carried out with excitation at 470 nm and emission at 590 nm. The analytical sample was prepared by simple dilution in methanol of the phytotherapeutic extract or of the alcoholic beverage. Hypericin can be rapidly and accurately determined at concentrations down to 0.1 mg/kg without any interferences.