Prospective randomized double-blind comparative study of topical acetyl zingerone with tetrahexyldecyl ascorbate versus tetrahexyldecyl ascorbate alone on facial photoaging.

BACKGROUND: Tetrahexydecyl ascorbate (THDA) is a lipophilic precursor to ascorbic acid that may be stabilized by acetyl zingerone (AZ). Studies have shown that the topical application of THDA may have photoprotective effects. Similarly, AZ has been shown to mitigate oxidative and inflammatory stress, thereby improving the appearance of photoaging. AIMS: To examine the effects of THDA and AZ (THDA-AZ) on skin photoaging compared to THDA alone. PATIENTS/METHODS: In this double-blind, randomized controlled trial, healthy individuals aged 30 to 65 were included and 44 participants were randomized to receive either THDA-AZ (THDA 5% + AZ 1%) or THDA only (THDA 5%) for 8 weeks. Facial photographs were taken at 0, 4, and 8 weeks to analyze wrinkle severity, pigment intensity, and redness intensity. A skin colorimeter was used to assess infraorbital pigmentation and erythema. Self-perception of skin and tolerability were assessed through questionnaires. RESULTS: Average wrinkle severity was significantly decreased in the THDA-AZ group at Weeks 4 and 8 by 0.75% (p = 0.023) and 3.72% (p = 0.048), respectively, compared to the THDA group where wrinkle severity at Weeks 4 and 8 was increased by 7.88% and 4.48%, respectively. Facial pigment intensity was significantly decreased in the THDA-AZ group by 4.10% (p = 0.0002) at Week 8 compared to a 0.69% decrease in the THDA group. Facial redness intensity was decreased in the THDA-AZ group at Weeks 4 and 8 by 3.73% (p = 0.0162) and 14.25% (p = 0.045), respectively, compared to the THDA group where at Weeks 4 and 8 erythema increased by 27.5% and 8.34%, respectively. There were no significant differences in either group for infraorbital pigmentation or erythema. CONCLUSIONS: Daily use of combined THDA and AZ may improve facial wrinkle severity, pigment intensity, and erythema to a greater extent than THDA. While THDA alone increases facial wrinkle severity and erythema, the addition of AZ reduces both.

Combination of zingerone and dihydroartemisinin presented synergistic antimalarial activity against Plasmodium berghei infection in BALB/c mice as in vivo model.

Malaria is a global health problem leading to the death of 435,000 cases in tropical and sub-tropical zones. Spread and emergence of increasing resistance to the antimalarial drugs are the major challenges in the control of malaria. Therefore, searching for alternative antimalarial drugs is urgently needed, and combination treatment preferred as an approach to address this. This study aimed to evaluate in vivo antimalarial activity of zingerone (ZN), and its combination with dihydroartemisinin (DHA) against Plasmodium berghei infected mice. ZN was prepared and tested for acute oral toxicity according to the OECD guideline. In vivo antimalarial activity of different doses of ZN and combination with DHA were determined using the 4-day suppression test. The results showed that ZN was found to be safe and no mortality within the observation period, and the lethal dose might be greater than the limited dose of 1000 mg/kg. For in vivo antimalarial test, ZN exhibited significant (p < .05) parasitemia inhibition of 30.65% and 45.75% at the doses of 50 mg/kg and 100 mg/kg, respectively. Moreover, effective dose 50 (ED50) of ZN was 29.76 mg/kg. The combination treatment of ZN and DHA at the doses of ED50 values at the fixed ratio 1:1 was found to present significant (p < .001) antimalarial activity as compared to ZN and DHA treated alone with markedly prolonged mean survival time. Additionally, the combination index (0.83384) revealed the synergistic antimalarial effect. It can be concluded that ZN exerted potent antimalarial activity with no toxicity, and combination treatment with DHA produced the synergistic antimalarial effect.

A biochemical and 2, 3, 5-triphenyl tetrazolium chloride staining study on the preventive effects of zingerone (vanillyl acetone) in experimentally induced myocardial infarcted rats.

Myocardial infarction continues to be a major public health problem, not only in western countries but also increasingly in developing countries and makes significant contribution to the mortality statistics. Reduction in mortality rate and prevention of myocardial infarction are of utmost importance. Tachycardia, left ventricular hypertrophy (LVH), altered adenosine triphosphatases (ATPases), and shifts in electrolyte balance play a vital role in the pathogenesis of myocardial infarction. This study was designed to evaluate the preventive effects of zingerone (vanillyl acetone) on tachycardia, LVH, altered electrocardiogram (ECG), altered activities of membrane bound ATPases, electrolyte imbalance and myocardial infarct size in isoproterenol induced myocardial infarcted rats. Rats were pretreated with zingerone (vanillyl acetone) 6 mg/kg body weight daily for a period of 14 days and were then induced myocardial infarction with isoproterenol (100 mg/kg body weight) on 15th and 16th day. Isoproterenol induced myocardial infarcted rats showed tachycardia, LVH, altered ECG, serum cardiac troponin-T, plasma myoglobin, heart ATPases, heart sodium ion, calcium ion, potassium ion, and increased myocardial infarct size. Pretreatment with zingerone (vanillyl acetone) revealed preventive effects on tachycardia, LVH, ECG, and all the above mentioned biochemical parameters evaluated in isoproterenol induced myocardial infarcted rats. The 2, 3, 5-triphenyl tetrazolium chloride staining on myocardial infarct size confirmed the prevention of myocardial infarction. Further, the in vitro study revealed a very convincing free radical scavenging of zingerone (vanillyl acetone). Thus, the observed effects of zingerone (vanillyl acetone) are due to its antioxidant and free radical scavenging activities in isoproterenol induced myocardial infarcted rats.

Complexação de guaiacol com ß-ciclodextrina para tratamento de alveolite seca: avaliação in vitro e in vivo / ß-cyclodextrin complexation of guaiacol for the treatment of dry socket: in vitro and in vivo evaluation

A alveolite seca (AS) é uma das complicações pós-operatórias mais comuns e sintomáticas na odontologia, porém, até o momento não há um protocolo de tratamento definido. O composto fenólico guaiacol (Gu) é um dos materiais utilizados para revestimento intra-alveolar devido às suas propriedades analgésicas, antioxidantes e antimicrobianas. Contudo, sua desvantagem é a dificuldade de manipulação decorrente da sua baixa estabilidade, alta volatilidade e sensibilidade à oxidação. Para melhorar suas propriedades e aumentar sua aplicabilidade clínica, um complexo de inclusão de Gu com ß-ciclodextrina (ßcd) foi desenvolvido. A formação do complexo supramolecular de Gu:ßcd foi caracterizada mediante a ressonância magnética nuclear (RMN), nos experimentos de 1H e 2D ROESY. A atividade antibacteriana do Gu e Gu:ßcd frente a Escherichia coli, Staphylococcus aureus, Streptococcus mitis, Streptococcus mutans, Streptococcus sanguis e Aggregatibacter actinomycetemcomitans foi analisada pelo método da microdiluição e sua citotoxicidade em osteoblastos de calvária de rato, foi estudado com o ensaio do MTT. O processo de reparo alveolar induzido pelo Gu:ßcd foi avaliado histologicamente após tratamento de alveolite seca em molares inferiores de ratos. A RMN mostrou correlações espaciais entre os hidrogênios internos (H3 e H5) da ßcd e os hidrogênios aromáticos, H(a) e H(b) do Gu, confirmando a formação do complexo. A complexação do Gu na ßcd potencializou seu efeito antibacteriano e reduziu sua citotoxicidade em osteoblastos. O estudo in vivo evidenciou a ocorrência de ossificação no ápice alveolar dos ratos tratados com Gu:ßcd, no 7o dia. No 14o dia, as trabéculas ósseas ocuparam também o terço médio do alvéolo e no 21o dia, todo o alvéolo se encontrava preenchido por osso neoformado. Estes resultados foram similares ao controle negativo e superiores ao controle positivo (Alvogyl®). Os benefícios obtidos pela inclusão do Gu na ßcd foram demonstrados pela melhora das...

Dry socket is one of the most common and symptomatic complications in dentistry, however, there is still not a settled treatment for this condition. The phenolic compound guaiacol (Gu) is one of several alveolar dressings used in dry socket because it has analgesic, antioxidant and antimicrobial properties. Nevertheless, its disadvantage is the difficulty of manipulation due to its low stability, high volatility and sensitivity to oxidation. To improve its properties and increase its clinical applicability, an inclusion complex of Gu with ß-cyclodextrin (ßcd) was developed. The Gu:ßcd supramolecular complex was characterized by Nuclear Magnetic Ressonance (NMR), in the 1H and 2D ROESY experiments. The antibacterial activity of Gu and Gu:ßcd over Escherichia coli, Staphylococcus aureus, Streptococcus mitis, Streptococcus mutans, Streptococcus sanguis and Aggregatibacter actinomycetemcomitans was analyzed using the microdilution method and its cytotoxicity in rat calvaria-derived osteoblast was evaluated with the MTT assay. The alveolus repair process induced by Gu:ßcd was histologically studied after the treatment of dry socket in rat mandibular molars. The NMR showed spatial correlations between internal hydrogens (H3 and H5) of ßcd and aromatic hydrogens, H(a) and H(b), of Gu confirming the inclusion complex formation. Gu:ßcd complex potentiated Gu antibacterial effect and reduced its cytotoxicity in osteoblasts. The in vivo study revealed that ossification occurred in the alveolar apex of rats treated with Gu:ßcd, by day 7. In the 14th day, the trabecular bone occupied the apical and middle thirds of the socket and on the 21st day, the entire alveolus was filled by newly formed bone. These results were similar to the negative control and superior to the positive control (AlvogylTM). Benefits gained from inclusion of Gu in cyclodextrin have been particularly demonstrated by the improvement in Gu biological properties in vitro and the appropriate alveolus...

Prenatal and early sucking influences on dietary preference in newborn, weaning, and young adult cats.

Early experiences are of potential importance in shaping long-term behavior. This study examined the relative influence of prenatal and/or early postnatal experience of chemosensory stimuli on subsequent olfactory and dietary preferences of cats as newborns, at 9-10 weeks, and at 6 months. Cats were exposed to vanillin or 4-ethylguaiacol via their mother's diet either prenatally, postnatally, perinatally (prenatal and postnatal), or experienced no exposure to the stimuli (control). Newborns were given a two-choice olfactory test between the familiar "odor" and no odor; 9-10 week olds were tested for their preference between two food treats, one flavored with the familiar stimulus and the other unflavored; at 6 months, cats were given a choice of two bowls of food, one flavored with the familiar stimulus and the other unflavored. At all ages, cats preferred the familiar, and avoided the unfamiliar, stimulus. Perinatal exposure exerted the strongest influence on preference. Prenatal exposure influenced preference at all ages and postnatal exposure exerted a stronger effect as the cat aged. We conclude that long-term chemosensory and dietary preferences of cats are influenced by prenatal and early (nursing) postnatal experience, supporting a natural and biologically relevant mechanism for the safe transmission of diet from mother to young.

Effects of zingerone [4-(4-hydroxy-3-methoxyphenyl)-2-butanone] and eugenol [2-methoxy-4-(2-propenyl)phenol] on the pathological progress in the 6-hydroxydopamine-induced Parkinson's disease mouse model.

Parkinson's disease (PD) is characterized by progressive degeneration of dopaminergic neurons in the nigrostriatal system and dopamine (DA) depletion in the striatum. The most popular therapeutic medicine for treating PD, 3-(3,4-Dihydroxyphenyl)-L-alanine (L-DOPA), has adverse effects, such as dyskinesia and disease acceleration. As superoxide (·O(2)(-)) and hydroxyl radical (·OH) have been implicated in the pathogenesis of PD, free radical scavenging and antioxidants have attracted attention as agents to prevent disease progression. Rodents injected with 6-hydroxydopamine (6-OHDA) intracerebroventricularly are considered to be a good animal model of PD. Zingerone and eugenol, essential oils extracted from ginger and cloves, are known to have free radical scavenging and antioxidant effects. Therefore, we examined the effects of zingerone and eugenol on the behavioral problems in mouse model and on the DA concentration and antioxidant activities in the striatum after 6-OHDA administration and L-DOPA treatment. Daily oral administration of eugenol/zingerone and injection of L-DOPA intraperitoneally for 4 weeks following a single 6-OHDA injection did not improve abnormal behaviors induced by L-DOPA treatment. 6-OHDA reduced the DA level in the striatum; surprisingly, zingerone and eugenol enhanced the reduction of striatal DA and its metabolites. Zingerone decreased catalase activity, and increased glutathione peroxidase activity and the oxidized L-ascorbate level in the striatum. We previously reported that pre-treatment with zingerone or eugenol prevents 6-OHDA-induced DA depression by preventing lipid peroxidation. However, the present study shows that post-treatment with these substances enhanced the DA decrease. These substances had adverse effects dependent on the time of administration relative to model PD onset. These results suggest that we should be wary of ingesting these spice elements after the onset of PD symptoms.

A case of toxic epidermal necrolysis-type drug eruption induced by oral lysozyme chloride.

We report a case of toxic epidermal necrolysis-type drug eruption. A 23-year-old man took an oral over-the-counter preparation for the common cold. A few days later, generalized erythema developed with systemic malaise and pain. A multiple blister formation followed, and Nikolsky's sign was noted on each blister. A lymphocyte stimulation test (LST) with the patient's peripheral lymphocytes strongly suggested that the eruption was attributable to lysozyme chloride which was included in the preparation taken. Following an intravenous drip of betamethasone for two weeks, the eruptions improved favorably.

[The clinico-pathological studies on the influence of immediate root canal filling after formalin guaiacol was applied on the extirpated pulp surface].

The method of immediate root canal filling following vital pulp extirpation involves many problems to be solved clinically. Therefore, the present study was performed to increase the clinical usefulness by applying formalin medicine in the root canal before immediate root canal filling after vital pulp extirpation. Group 1 (the group of applying formalin tricresol or formalin guaiacol on the intentionally exposed pulp tissue) Group 2 (pulp extirpation). This study is based upon 95 human permanent teeth with noninfected pulps in patients ranging in age from 16 to 43 years. Under local anesthesia the experimental teeth were isolated with cotton rolls. The pulp was intentionally exposed during the preparation of the Ingle's cavity with diamond instruments mounted on a high speed air turbine. The cavity and exposed pulp surface were cleaned with Neo-cleaner (10% Hypochlorite) and oxydol, and then dried using an absorbent material. One of the experimental medicines, which had been saturated into phi 2mm cotton pellet, was applied on the exposed pulp tissue. The cavity was filled with gutta-percha and amalgam. Under local anesthesia, the pulp was intentionally exposed in the same way as mentioned above. After removal of pulp tissue, root canals were cleaned with oxydol. Root canals were filled with Calvital (CV) in 15 cases. Following insertion of sterilized paper point soaked in the solution of formalin guaiacol (FG) or formalin tricresol (FC) for 5 minutes, root canal filling with Calvital was carried out in 20 cases. The experimental teeth were clinically observed at various intervals, and then extracted. After fixation in 10% formalin solution, the teeth were decalcified using nitric acid and embedded in celloidin. The serial sections were stained with hematoxylin and eosin and observed histopathologically. Group 1. 1. Kinds of clinical discomfort observed in this investigation were as follows. FG: Spontaneous pain (25.0%), Percussion discomfort (5.0%). FC: Spontaneous pain (35.0%), Percussion discomfort (35.0%). 2. Clinical results were as follows. FG: 14 cases (70.0%) out of 20 were evaluated as good, 6 cases (30.0%) as fairly good, and none as bad. FC: 11 cases (55.0%) out of 20 were evaluated as good, 9 cases (45.0%) as fairly good, and none as bad. 3. Histopathological changes observed in this investigation were as follows. 1) Hyperemia, 2) Hemorrhage, 3) Round cell infiltration, 4) Suppurative inflammation, 5) Coagulation necrosis, 6) Atrophy, 7) Cicatrization. Group 2. 1. Kinds of clinical discomfort observed in this investigation were as follows. CV: Spontaneous pain (20.0%), Percussion discomfort (20.0%). FG: Spontaneous pain (30.0%), Percussion discomfort (15.0%). FC: Spontaneous pain (30.0%), Percussion discomfort (30.0%). 2. Clinical results were as follows.

Contact dermatitis from antioxidants.

In a search for contact sensitivity to antioxidants we patch tested consecutive patients referred with eczematous dermatitis. Six cases of allergic contact sensitivity to nordihydroguairetic acid (NDGA) were observed. Three had been sensitized by one brand of cream containing 0.1% NDGA, in three patients the source of sensitization could not be traced. In four patients we found positive patch tests to butylated hydroxyanisole and/or to butylated hydroxytoluene. In two cases the positive patch tests were relevant, since both patients remained asymptomatic when antioxidants were avoided in food. They both had acute flares of vesicular eczema on the fingers after oral administration of small amounts. Gallate esters and Vitamin E (d,l-alpha-tocopherol) each gave one unexplained positive patch test. The present data suggest that further search for hidden sensitizers in topical medicaments and cosmetics is warranted. A declaration of all ingredients in industrial products should be placed on the label.