Repeated 28-Day Oral Toxicological Study and Gastroprotective Effects of Nigella sativa L. Oil (Shuhada) against Ethanol-Induced Gastric Mucosal Injury in Rats.

Nigella sativa L. and black seeds are traditionally used for cooking and medicinal purposes in Arab and other countries. Although N. sativa seed extract has many known biological effects, the biological effects of cold-pressed N. sativa oil are poorly understood. Therefore, the objective of this study was to investigate the gastroprotective effects and subacute oral toxicity of black seed oil (BSO) in an animal model. The gastroprotective effects of oral BSO (50% and 100%; 1 mg/kg) were tested using acute experimental models of ethanol-induced gastric ulcers. Gross and histological gastric lesions, ulcerated gastric areas, ulcer index score, percentage of inhibition rate, gastric juice pH, and gastric wall mucus were all evaluated. The subacute toxicity of BSO and its thymoquinone (TQ) content were also examined. The results indicated that the administration of BSO exerted gastroprotective effects by increasing the gastric wall mucus and decreasing gastric juice acidity. In the subacute toxicity test, the animals behaved normally, and their weight and water and food intake did not show significant variations. High-performance liquid chromatography detected 7.3 mg/mL TQ in BSO. These findings suggest that BSO may be a safe therapeutic drug for preventing gastric ulcers.

Alpha-glucosidase inhibitory activities of astilbin contained in Bauhinia strychnifolia Craib. stems: an investigation by in silico and in vitro studies.

INTRODUCTION: Bioactive compounds from traditional medicines are good alternatives to standard diabetes therapies and may lead to new therapeutic discoveries. The stems of Bauhinia strychnifolia Craib. (BC) have a possible antihyperglycemic effect; However, the extraction of astilbin from BC has never been recorded in alpha-glucosidase inhibitory activities. METHODS: Using liquid chromatography-mass spectrometry (LC-MS/MS), 32 compounds were detected in the BC extract. The screening was based on peak area. Seven compounds found. PASS recognized all seven compounds as potential alpha-glucosidase (AG) inhibitors. Astilbin and quercetin 3-rhamnoside were the most likely inhibitors of AG. Arguslab, AutoDock, and AutoDock Vina investigated the binding of the two compounds and AG. The binding stability was confirmed by molecular dynamics (MD). In addition, the optimum solvent extraction was studied via CosmoQuick, and extracts were examined with 1H-NMR prior to testing with AG. RESULTS: All three software programs demonstrated that both compounds inhibit AG more effectively than acarbose. According to the sigma profile, THF is recommended for astilbin extraction. The BC extract with THF showed outstanding AG inhibitory action with an IC50 of 158 ± 1.30 µg mL-1, which was much lower than that of the positive control acarbose (IC50 = 190 ± 6.97 µg mL-1). In addition, astilbin from BC was found to inhibit AG strongly, IC50 = 22.51 ± 0.70 µg mL-1 through the extraction method of large-scale astilbin with THF has the best extraction capacity compared to other solvents, hence the initial stage of extraction employs THF to extract and precipitate them with ethyl acetate and water. CONCLUSION: In silico and in vitro studies reveal that astilbin inhibits AG and is superior to acarbose, validating its promise as an AG inhibitor. Overall, astilbin was the most bioactive component of BC for antidiabetic action.

A Thai Traditional Triple-Fruit Formulation "Phikud Tri-Phon" May Provide Fat Loss and Nutritional Benefits.

Obesity and overweight have serious health outcomes. "Phikud Tri-Phon" (PTP) is a traditional Thai medicine comprising three dried fruits from Aegle marmelos L., Morinda citrifolia L., and Coriandrum sativum L. Whether this medicine impacts on metabolic disease is unclear. This study aimed to investigate the phenolic and flavonoid contents of PTP and each of its herbal components, and further assess their antioxidant and anti-adipogenetic activities. Oil-red O staining was measured for lipid accumulation in 3T3-L1 adipocytes. The chemical profiles of PTP and each herbal extract were determined by LC-ESI-QTOF-MS/MS. Our results show that the total phenolic and flavonoid contents of PTP water extract were 22.35-108.42 mg of gallic acid equivalents and PTP ethanolic extract was 1.19-0.93 mg of quercetin equivalents and the DPPH scavenging capacity assay of PTP ethanolic extract (1 mg/mL) was 92.45 ± 6.58 (Trolox equivalent)/g. The PTP extracts and individual herbs had inhibitory adipogenesis activity, which reduced lipid accumulation by approximately 31% in PTP water extract and 22% in PTP ethanolic extract compared with control cells. These results provided insights into the traditional preparation method of using boiling water as a vehicle for PTP. In conclusion, PTP has antioxidant and anti-adipogenesis potential, indicating it is a promising ingredient in functional food and herbal health products.

Inhibition of α-Glucosidase and Pancreatic Lipase Properties of Mitragyna speciosa (Korth.) Havil. (Kratom) Leaves.

Kratom (Mitragyna speciosa (Korth.) Havil.) has been used to reduce blood sugar and lipid profiles in traditional medicine, and mitragynine is a major constituent in kratom leaves. Previous data on the blood sugar and lipid-altering effects of kratom are limited. In this study, phytochemical analyses of mitragynine, 7-hydroxymitragynine, quercetin, and rutin were performed in kratom extracts. The effects on α-glucosidase and pancreatic lipase activities were investigated in kratom extracts and mitragynine. The LC-MS/MS analysis showed that the mitragynine, quercetin, and rutin contents from kratom extracts were different. The ethanol extract exhibited the highest total phenolic content (TPC), total flavonoid content (TFC), and total alkaloid content (TAC). Additionally, compared to methanol and aqueous extracts, the ethanol extract showed the strongest inhibition activity against α-glucosidase and pancreatic lipase. Compared with the anti-diabetic agent acarbose, mitragynine showed the most potent α-glucosidase inhibition, with less potent activity of pancreatic lipase inhibition. Analysis of α-glucosidase and pancreatic lipase kinetics revealed that mitragynine inhibited noncompetitive and competitive effects, respectively. Combining mitragynine with acarbose resulted in a synergistic interaction with α-glucosidase inhibition. These results have established the potential of mitragynine from kratom as a herbal supplement for the treatment and prevention of diabetes mellitus.

Development, Characterization, and Stability Evaluation of the Anti-Cellulite Emgel Containing Herbal Extracts and Essential Oils.

Recently, the herbal compress was successfully developed and applied for cellulite treatment. The aim of this study was to formulate a more convenient dosage form of herbal application from the original formula. In addition, we aimed to characterize and evaluate the stability of the developed dosage form. A gelled emulsion, or an "emgel," incorporated with 0.1 wt% tea and coffee extracts (1:1 ratio) plus 5 wt% essential oils (mixed oil) was prepared. The caffeine content in the finished product obtained from tea and coffee extracts analyzed by HPLC was 48.1 ± 2.3 µg/g. The bio-active marker monoterpenes of mixed oil characterized by headspace GCMS were camphene 50.8 ± 1.8 µg/mg, camphor 251.0 ± 3.2 µg/mg, 3-carene 46.7 ± 1.8 µg/mg, α-citral 75.0 ± 2.1 µg/mg, ß-citral 65.6 ± 1.3 µg/mg, limonene 36.8 ± 6.7 µg/mg, myrcene 53.3 ± 4.5 µg/mg, α-pinene 85.2 ± 0.6 µg/mg, ß-pinene 88.4 ± 1.1 µg/mg, and terpinene-4-ol 104.3 ± 2.6 µg/mg. The stability study was carried out over a period of 3 months at 4, 25, and 50 °C. The caffeine content showed no significant changes and passed the acceptance criteria of ≥80% at all tested temperatures. However, monoterpenes showed their stability for only 2 months at 50 °C. Therefore, the shelf-life of the emgel was, consequently, calculated to be 31 months using the Q10 method. Thus, the anti-cellulite emgel was successfully formulated. The characterization methods and stability evaluation for caffeine and monoterpenes in an emgel matrix were also successfully developed and validated.

Efficacy of an Anti-Cellulite Herbal Emgel: A Randomized Clinical Trial.

Cellulite describes unsightly skin overlying subcutaneous fat around thighs and buttocks of post-pubescent females. A herbal 'emgel' containing volatile oils and extracts of A traditional Thai herbal compress was tested in a double-blind, placebo-controlled trial with 18 women aged 20-50 year with severe cellulite. Appearance of cellulite (primary outcome), thigh circumferences, skin firmness, and cutaneous blood flow (secondary outcomes) were assessed at baseline, 2, 4, 8 and 12 weeks with a 2-week follow-up. Herbal emgel applied onto the thigh skin twice daily reduced cellulite severity scores in every time point. The score was reduced from 13.4 ± 0.3 (baseline) to 12.1 ± 0.3 (week 2) and 9.9 ± 0.6 (week 12). All secondary outcomes improved with both placebo and herbal emgels suggesting that ingredients in the base-formulation might be responsible. Querying of participants, analysis of their diaries, and physical monthly inspections found no adverse events. The herbal emgel safely improved the appearance of cellulite, while the base emgel may play a role for other endpoints. Further studies on the active constituents and their mechanism of action are needed to further explore these factors.

Effects of Essential Oils and Some Constituents from Ingredients of Anti-Cellulite Herbal Compress on 3T3-L1 Adipocytes and Rat Aortae.

Cellulite is associated with a complex array of adipocytes under the skin and vascular system. A herbal compress that was previously developed was proven to have an anti-cellulite effect in healthy volunteers within 2 weeks of treatment. However, its mechanism and ingredients responsible for reducing cellulite were not known. The purpose of this study was to investigate the activity of eight essential oils in, and two water extracts from, the ingredients of the herbal compress together with nine monoterpenoid constituents on the 3T3-L1 adipocytes. The vasodilatory effect on rat aortae was also studied. The adipocytes were induced by dexamethasone, 3-isobutyl-1-methylxanthine and insulin. At all concentrations tested, all essential oils, water extracts and their monoterpenoid constituents significantly inhibited lipid accumulation activity (p < 0.05) and decreased the amount of triglycerides when compared to untreated cells (p < 0.01). In addition, our results showed that the mixed oil distilled from the herbal compress mixed ingredients could relax the isolated rat aorta (EC50 = 14.74 ± 2.65 µg/mL). In conclusion, all essential oils, extracts and chemical constituents tested showed effects on adipogenesis inhibition and lipolysis induction on the cultured adipocytes with the mixed oil demonstrating vasorelaxation activity, all of which might be the mechanisms of the anti-cellulite effects of the herbal compress.

Cellulite Reduction by Modified Thai Herbal Compresses; A Randomized Double-Blind Trial.

Cellulite remains an obstinate clinical and cosmetic problem. In this study, we adapted the Thai traditional noninvasive treatment formulated with 5 additional herbals to improve blood flow, edema, and lipolysis, thereby augmenting cellulite treatment. This was a double-blind, randomized placebo-controlled paired trial. Twenty-one women (20-55 years) having cellulite (grade ≥2) were treated with steamed placebo or herbal compresses randomly assigned to one or other thigh twice weekly for 8 weeks with 2 weeks washout. Cellulite reduction was assessed from standardized photographs by 3 blinded evaluators at baseline and every 2 weeks; also assessed were thigh circumferences and cutaneous skin-fold thicknesses, trial diaries, and participant feedback. After 8 weeks, herbal compress treatment reduced Nürnberger-Müller cellulite scores from 12.6 ± 2.0 to 9.9 ± 2.4 compared with 12.5 ± 2.1 to 12.1 ± 2.0 (means ± SEM) for contralateral placebo-treated thighs ( P < .0001; effect size [ES] = 1.16, confidence interval [CI] = 0.48-1.83). Thigh circumferences diminished by 2.2 ± 0.9 cm (herbal) and 1.4 ± 0.7 cm (placebo) (ES = 0.96, CI = 0.30-1.61) and correspondingly skin-folds by 5.6 ± 2.2 and 2.4 ± 1.3 mm (ES = 1.72, CI = 0.99-2.45). No adverse actions were reported, and there were no dropouts, no missing data, and 100% adherence. Herbal compresses were efficacious against cellulite and thigh sizes. The herbal formula might be adapted to other delivery options, and rationally added herbals may increase effectiveness of traditional therapies and more sustainable actions.