Search Results (11)

The objective of this study is to determine the physiological and metabolic effects of administration of dietary fiber formulations to male Wistar rats. The study population was divided into five groups to which food and water were orally administered ad libitum (control), alongside Psyllium plantago, sennosides A and B, cactus pear peel powder, and cactus pear peel tablet powder for 28 days. Body weight, biochemical parameters, fecal moisture, and intestinal transit were determined. The administration of the fiber formulations did not cause differences between the groups and they maintained a healthy weight; however, the consumption of the cactus pear peel tablet powder decreased serum glucose (127.85 ± 5.37 to 68.30 ± 12.48 mg/dL) in rats in a similar form to Psyllium plantago (127.85 ± 5.37 to 96.96 ± 3.26 mg/dL) in comparison with commercial products for rats, and the cactus pear peel powder had lower triglyceride levels (49.52 to 74.44 mg/dL) than commercial products at the end of the treatment. The samples maintained normal HDL levels with the exception of Psyllium plantago that had a decrease in treatment after 28 days. The administration of formulations of dietary fiber of cactus pear peel had physiological and metabolic effects similar to those of commercial products without change in the growth of the animals. Therefore, it could be used in the pharmaceutical or food industry. Full article

Hydroxyanthracene derivatives (HADs) are plant substances produced by a variety of plant species, including different Aloe, Rheum, and Rhamnus species and Cassia senna. These plants are often used in food supplements to improve bowel function. However, recently, the European Commission prohibited a number of HADs due to toxicological concerns. These HADs included aloin (aloin A and aloin B), aloe-emodin, emodin, and danthron. Most of the currently available analytical methods are restricted to the analysis of only these compounds and do not include other HADs. In this view, a multi-analyte method could be useful for both regulatory analysis and dietary intake studies. To this end, such a method, employing liquid chromatography–tandem mass spectrometry and targeting 16 different HADs, was developed and validated in this study. Limits of quantification were in the range from 0.025 mg kg⁻¹ to 1 mg kg⁻¹. The recovery of the method was within the acceptable range of 80% to 120%, with the exception of physcion. Repeatability varied from 0.5% to 11.6%, and the range for within-laboratory reproducibility was from 3.4% to 16.3%. The expanded measurement uncertainty was below 50% for all HADs. Subsequently, 24 commercial samples of food supplements and herbal infusions sourced in Belgium were analyzed. The results indicated that although the industry put a great effort into minimizing the amount of aloin and danthron present in food supplements, more than half of the products still exceeded the maximum tolerated levels suggested for aloe-emodin and emodin. Full article

Rhubarb is a significant medicinal herb in China. Its adulteration or fabrication is common in the market. Consequently, it is necessary to establish a comprehensive identification method to accurately identify genuine rhubarb and its adulterants. In this study, the sequences of chloroplast genes rps3-rpl22 and rpl16 from three genuine rhubarbs (Rheum tanguticum, Rh. palmatum and Rh. officinale) and their adulterants (Rumex japonicus and Rumex spp.) were amplified, sequenced and subjected to genetic analyses. The genetic distances for rps3-rpl22 and rpl16 between genuine rhubarbs and their adulterants showed that there was an evident barcoding gap, which allowed the adulterants to be distinguished from the genuine rhubarbs, as demonstrated by a neighbor joining tree. Additionally, Rh. officinale could be distinguished from the other two genuine rhubarbs. The anthraquinone, sennoside, polysaccharide and protein contents were analyzed in seven rhubarbs using high-performance liquid chromatography and ultraviolet spectrophotometry. Cluster and principal component analyses results showed that Rh. tanguticum and Rh. palmatum could be effectively distinguished. The study suggests that DNA barcoding based on rps3-rpl22 and rpl16 sequences coupled with multiple-indicator quantification can be successfully applied to identify rhubarb species and distinguish among the three genuine rhubarbs, and this can provide a scientific foundation for rhubarb quality assurance. Full article

Senna Mill. (Fabaceae) is an important medicinal plant distributed worldwide. Senna alexandrina (S. alexandrina), the officinal species of the genus, is one of the most well-known herbal medicines traditionally used to treat constipation and digestive diseases. Senna italica (S. italica), another species of the genus, is native to an area ranging from Africa to the Indian subcontinent, including Iran. In Iran, this plant has been used traditionally as a laxative. However, very little phytochemical information and pharmacological reports investigating its safety of use are available. In the current study, we compared LC-ESIMS metabolite profiles of the methanol extract of S. italica with that of S. alexandrina and measured the content of sennosides A and B as the biomarkers in this genus. By this, we were able to examine the feasibility of using S. italica as a laxative agent like S. alexandrina. In addition, the hepatotoxicity of both species was evaluated against HepG2 cancer cell lines using HPLC-based activity profiling to localize the hepatotoxic components and evaluate their safety of use. Interestingly, the results showed that the phytochemical profiles of the plants were similar but with some differences, particularly in their relative contents. Glycosylated flavonoids, anthraquinones, dianthrones, benzochromenones, and benzophenones constituted the main components in both species. Nevertheless, some differences, particularly in the relative amount of some compounds, were observed. According to the LC-MS results, the amounts of sennoside A in S. alexandrina and S. italica were 1.85 ± 0.095% and 1.00 ± 0.38%, respectively. Moreover, the amounts of sennoside B in S. alexandrina and S. italica were 0.41 ± 0.12 % and 0.32 ± 0.17%, respectively. Furthermore, although both extracts showed significant hepatotoxicity at concentrations of 50 and 100 µg/mL, they were almost non-toxic at lower concentrations. Taken together, according to the results, the metabolite profiles of S. italica and S. alexandrina showed many compounds in common. However, further phytochemical, pharmacological, and clinical studies are necessary to examine the efficacy and safety of S. italica as a laxative agent. Full article

In the present work, a two-dimensional qNMR method for the determination of sennosides was established. Using band-selective HSQC and the cross correlations of the characteristic 10–10’ bonds, we quantified the total amount of the value-determining dianthranoids in five minutes, thus, rendering the method not only fast, but also specific and stability indicating. The validation of the method revealed excellent accuracy (recovery rates of 98.5 to 103%), precision (RSD values of 3.1%), and repeatability (2.2%) and demonstrated the potential of 2D qNMR in the quality control of medicinal plants. In a second method, the use of 2D qNMR for the single analysis of sennosides A, B, and A₁ was evaluated with acceptable measurement times (31 min), accuracy (93.8%), and repeatability (5.4% and 5.6%) for the two major purgatives sennoside A and B. However, the precision for sennoside B and A₁ was not satisfactory, mainly due to the low resolution of the HSQC signals of the two compounds. Full article

In this study, ultrasound-assisted extraction conditions were optimized to maximize the yields of sennoside A, sennoside B, aloe-emodin, emodin, and chrysophanol from S. alexandrina (aerial parts). The three UAE factors, extraction temperature (S₁), extraction time (S₂), and liquid to solid ratio (S₃), were optimized using response surface methodology (RSM). A Box–Behnken design was used for experimental design and phytoconstituent analysis was performed using high-performance liquid chromatography-UV. The optimal extraction conditions were found to be a 64.2 °C extraction temperature, 52.1 min extraction time, and 25.2 mL/g liquid to solid ratio. The experimental values of sennoside A, sennoside B, aloe-emodin, emodin, and chrysophanol (2.237, 12.792, 2.457, 0.261, and 1.529%, respectively) agreed with those predicted (2.152, 12.031, 2.331, 0.214, and 1.411%, respectively) by RSM models, thus demonstrating the appropriateness of the model used and the accomplishment of RSM in optimizing the extraction conditions. Excellent antioxidant properties were exhibited by S. alexandrina methanol extract obtained using the optimized extraction conditions with a DPPH assay (IC50 = 59.7 ± 1.93, µg/mL) and ABTS method (47.2 ± 1.40, µg/mL) compared to standard ascorbic acid. Full article

Natural products (NPs) have played a significant role in drug discovery for diverse diseases, and numerous attempts have been made to discover promising NP inhibitors of tumor necrosis factor α (TNF-α), a major therapeutic target in autoimmune diseases. However, NP inhibitors of TNF-α, which have the potential to be developed as new drugs, have not been reported for over a decade. To facilitate the search for new promising inhibitors of TNF-α, we developed an efficient competitive binding screening assay based on analytical size exclusion chromatography coupled with liquid chromatography-tandem mass spectrometry. Application of this screening method to the NP library led to the discovery of a potent inhibitor of TNF-α, sennoside B, with an IC₅₀ value of 0.32 µM in TNF-α induced HeLa cell toxicity assays. Surprisingly, the potency of sennoside B was 5.7-fold higher than that of the synthetic TNF-α inhibitor SPD304. Molecular docking was performed to determine the binding mode of sennoside B to TNF-α. In conclusion, we successfully developed a novel competition binding screening method to discover small molecule TNF-α inhibitors and identified the natural compound sennoside B as having exceptional potency. Full article

Senna and rhubarb are often used as routine laxatives, but there are differences in mechanism of action and potential side effects. Here, we studied metabolites of senna anthraquinones (SAQ), rhubarb anthraquinones (RAQ) and their chemical marker, sennoside A (SA), in a rat diarrhea model. In in vitro biotransformation experiments, SAQ, RAQ and SA were incubated with rat fecal flora solution and the metabolites produced were analyzed using HPLC. In in vivo studies, the same compounds were investigated for purgation induction, with measurement of histopathology and Aqps gene expression in six organs. The results indicated that SAQ and RAQ had similar principal constituents but could be degraded into different metabolites. A similar profile of Aqps down-regulation for all compounds was seen in the colon, suggesting a similar mechanism of action for purgation. However, in the kidneys and livers of the diarrhea-rats, down-regulation of Aqps was found in the RAQ-rats whereas up-regulation of Aqps was seen in the SAQ-rats. Furthermore, the RAQ-rats showed lower Aqp2 protein expression in the kidneys, whilst the SA-rats and SAQ-rats had higher Aqp2 protein expression in the kidneys. This may have implications for side effects of SAQ or RAQ in patients with chronic kidney or liver diseases. Full article

The emergence of the SARS-CoV-2 pandemic has prompted scientists to search for an efficient antiviral medicine to overcome the rapid spread and the marked increase in the number of patients worldwide. In this regard natural products could be a potential source of substances active against coronavirus infections. A systematic computer-aided virtual screening approach was carried out using commercially available natural products found on the Zinc Database in addition to an in-house compound library to identify potential natural product inhibitors of SARS-CoV-2 main protease (M^PRO). The top eighteen hits from the screening were selected for in vitro evaluation on the viral protease (SARS-CoV-2 M^PRO). Five compounds (naringenin, 2,3′,4,5′,6-pentahydroxybenzophenone, apigenin-7-O-glucoside, sennoside B, and acetoside) displayed high activity against the viral protein. Acteoside showed similar activity to the positive control GC376. The most potent compounds were tested in vitro on SARS-CoV-2 Egyptian strain where only naringenin showed moderate anti-SARS-CoV-2 activity at non-cytotoxic micromolar concentrations in vitro with a significant selectivity index (CC₅₀/IC₅₀ = 178.748/28.347 = 6.3). Moreover; a common feature pharmacophore model was generated to explain the requirements for enzyme inhibition by this diverse group of active ligands. These results pave a path for future repurposing and development of natural products to aid in the battle against COVID-19. Full article

Symbiotic arbuscular mycorrhizal fungi (AMF) play a major role in plant development, growth, and relationships with the environment through a change in the accumulation of secondary metabolites; hence, we planned to investigate AMF’s influence on sennoside A and B accumulation in Senna alexandrina (SA) and Senna italica (SI). Seeds of SA (S. alexandrina free of mycorrhizae) and SI (S. italica free of mycorrhizae) were planted in two types of soils: +mycorrhiza and—mycorrhiza. The plant leaves of SA, SI, S. alexandrina with mycorrhizae (SAM) and S. italica with mycorrhizae (SIM) were collected and extracted (with 85% methanol), and sennoside A and B content was evaluated by the HPLC–UV method. The antioxidant activity of SA, SI, SAM and SIM was evaluated by using 2, 2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) methods, while antimicrobial properties were evaluated by the minimum inhibitory concentration method (MIC). The AMF colonization was 85.66% and 85%, respectively, in the roots of SA and SI. The HPLC analysis showed a significant increase in (%) the content of sennoside A/sennoside B by 71.11/88.21, respectively, in SAM and 6.76/36.37 in SIM, which clearly indicated positive AMF effects. The DPPH/ABTS [The half maximal inhibitory concentration (IC₅₀): 235.9/321.5 µg/mL] scavenging activity of SAM was comparatively higher and it also exhibited strong antibacterial action (MIC: 156.25 µg/mL), which supported the increase in sennoside content. This finding may be useful for further investigations of the symbiotic relation of mycorrhizal fungi with other plant species. Full article

Senna and its main components sennosides are well-known effective laxative drugs and are used in the treatment of intestinal constipation in the world. Their potential side effects have attracted more attention in clinics but have little scientific justification. In this study, senna extract (SE), sennosides (SS), and sennoside A (SA) were prepared and used to generate diarrhea rats. The diarrhea rats were investigated with behaviors, clinical signs, organ index, pathological examination, and gene expression on multiple aquaporins (Aqps) including Aqp1, Aqp2, Aqp3, Aqp4, Aqp5, Aqp6, Aqp7, Aqp8, Aqp9, and Aqp11. Using qRT-PCR, the Aqp expression profiles were constructed for six organs including colon, kidney, liver, spleen, lung, and stomach. The Aqp alteration profiles were characterized and was performed with Principle Component Analysis (PCA). The SE treatments on the rats resulted in a significant body weight loss (p < 0.001), significant increases (p < 0.001) on the kidney index (27.72%) and liver index (42.55%), and distinguished changes with up-regulation on Aqps expressions in the kidneys and livers. The SS treatments showed prominent laxative actions and down regulation on Aqps expression in the colons. The study results indicated that the SE had more influence/toxicity on the kidneys and livers. The SS showed more powerful actions on the colons. We suggest that the caution should be particularly exercised in the patients with kidney and liver diseases when chronic using senna-based products. Full article