Coix lacryma-jobi L., Poaceae, is traditionally used for the treatment of gastrointestinal disorders, yet its gastroprotective and ulcer-healing properties remain poorly explored. This study, integrating network pharmacology, in vivo assays, and molecular docking, demonstrates that the hydroalcoholic extract of C. lacryma jobi exerts its effects through convergent antioxidant, anti-inflammatory, and cytoprotective pathways. In ethanol-induced acute gastric injury, extract of C. lacryma jobi (100 mg/kg) prevented the depletion of reduced glutathione levels and decreased myeloperoxidase activity. Histological and histochemical analyses confirmed preservation of gastric mucosal structure. In addition, the reversal of extract of C. lacryma jobi protective effects by pretreatment with N-ethylmaleimide, indomethacin, and Nω-nitro-l-arginine methyl ester (l-NAME) indicates the involvement of sulfhydryl groups, prostaglandins, and nitric oxide pathways in its gastroprotective mechanism. In chronic acetic acid–induced ulcer, extract of C. lacryma jobi not only reduced the ulcerated area but also produced clear histological improvement, characterized by re‑epithelialization, reorganization of mucosal layers, and partial restoration of glandular architecture. These activities are likely related to decreased levels of reduced glutathione, lipid hydroperoxides, and diminished myeloperoxidase activity. Network pharmacology analyses indicated that the bioactive constituents of extract of C. lacryma jobi primarily exert their effects by modulating inflammatory signaling pathways. Mass spectrometry identified polyphenols, among which quercetin and kaempferol exhibited the highest binding affinity to myeloperoxidase and to IL-1β in docking simulations. Furthermore, no evidence of toxicity was observed in vivo and in silico assays for extract of C. lacryma jobi and its bioactive compounds. Collectively, these findings demonstrate that extract of C. lacryma jobi exerts multi-target gastroprotective and healing effects, supporting its potential as a natural antiulcer agent.
Boswellia serrata is a medicinal plant traditionally used to treat inflammatory conditions and this study aimed to evaluate the efficacy of B. serrata dry extract (BSDE) in treating gastric ulcers and ulcerative colitis. Chronic gastric ulcers were induced using 80
Fridericia chica (Bonpl.) L.G.Lohmann, Bignoniaceae, is popularly used to treat gastrointestinal disorders. This study aimed to evaluate the antiulcer activities of a hydroalcoholic extract of F. chica and to advance the understanding of the pharmacological mechanisms through in silico, in vivo, and ex vivo studies. For the gastric healing evaluation, rats were induced with acetic acid (80
ETHNOPHARMACOLOGICAL IMPORTANCE:Aloysia polystachya (Griseb.) Moldenke is a medicinal plant that has long been used in South American medicine to treat a variety of diseases, most notably gastrointestinal issues. Despite its well-known ethnobotanical usage, this plant's putative anti-gastric ulcer action has yet to be investigated. AIM OF THE STUDY:To evaluate the gastroprotective and gastric healing effects of the hydroalcoholic extract from Aloysia polystachya (HEAp) and its bioactive compound, carvone, through both in vivo and in silico approaches. Additionally, it seeks to elucidate the pharmacological mechanisms underlying these biological effects. MATERIALS AND METHODS:First, phytochemical tests were performed with HEAp. Next, to demonstrate the gastroprotective activities, rats were orally treated with HEAp (30, 100, or 300 mg/kg) or carvone (3 mg/kg) before induction with ulcerative agents (ethanol or piroxicam). Furthermore, the role of prostaglandins, α-2 adrenergic receptors, nitric oxide, and sulfhydryl compounds were investigated. Additionally, the antisecretory activity of HEAp was investigated using a pylorus ligation model. For gastric healing analysis, acetic acid-induced chronic ulcer was used, in which rats were treated with HEAp at 100 mg/kg. Biochemical evaluations included measurements of myeloperoxidase (MPO), superoxide dismutase (SOD), glutathione S-transferase (GST), glutathione reduced (GSH) levels, and lipid peroxides (LPO) in ulcerated tissues. Finally, computational studies, including network pharmacology and molecular docking analyses, were conducted to explore the potential pharmacological targets of HEAp phytoconstituents. RESULTS:Mass spectrometry analysis (ESI-MS) identified four compounds: caffeic, p-coumaric, gallic acids, and epigallocatechin, which, along with carvone, were used in the in-silico analyses. Oral administration of HEAp (100 or 300 mg/kg) and carvone (3 mg/kg) significantly prevented ethanol- and piroxicam-induced gastric ulcers, as corroborated by histopathological assessments. Furthermore, pretreatment with N-ethylmaleimide (NEM) abolished the gastroprotective effects of both agents, implicating the involvement of sulfhydryl compounds in their modes of action. In the pylorus ligation assay, carvone (3 mg/kg) notably increased gastric pH and reduced acidity and peptic activity, mirroring the effects of omeprazole. Additionally, HEAp (100 mg/kg) and carvone (3 mg/kg) accelerated acetic acid-induced gastric ulcer healing by 75.06 % and 76.18 %, respectively, as supported by histological and histochemical analyses. Moreover, the healing effects of HEAp and carvone diminished MPO activity and LPO, along with elevated GSH levels and enhanced GST and SOD activities. In silico, carvone presented a binding mode similar to the co-crystallized substrate vonoprazan and effective interactions with the protein MPO, which highlights the compound's potential as a natural therapeutic agent for the treatment of gastric ulcers. CONCLUSION:The findings of this study demonstrate that the hydroalcoholic extract of A. polystachya (HEAp) and its bioactive compound carvone possess significant gastroprotective and gastric healing properties. These effects are likely mediated through the modulation of sulfhydryl compounds, anti-inflammatory and antioxidant defenses, and antisecretory mechanisms. The identification of phenolic constituents, combined with in silico analyses, further supports the potential therapeutic relevance of HEAp and carvone. Collectively, these results highlight that the phytoconstituents from A. polystachya corroborate the traditional use of the plant and are promising candidates for the investigation of anti-ulcer gastric agents.
The biosynthesis of melanin, the main protein involved in skin pigmentation, involves tyrosine, the enzyme tyrosinase, and ultraviolet radiation. However, an imbalance in this process can promote cutaneous hypermelanosis (CH), which causes spots on the skin. The CH treatment involves techniques and products with high adverse reactions. In this context, research has been increased into natural products. However, investigations using computational tools combined with evaluations of enzyme inhibition (in vitro) and toxicity tests are scarce. In this study, we evaluated thirteen bioactive compounds using virtual screening (SwissADME and SwissTarget Prediction software), and the most promising molecules were tested for tyrosinase inhibitory effects and cytotoxicity assays (MTT). Kaempferol, apigenin, and quercetin revealed better in silico bioavailability and tyrosinase inhibition parameters (94.8, 91.9, and 88.4%, respectively). Additionally, these molecules demonstrated different cytotoxicity profiles at 24 and 48 hours of exposure. Our evidence indicates that the flavonoids tested are promising agents in inhibiting tyrosinase.
Ethnopharmacological importance: Uncaria tomentosa Willd. DC., is used in the Amazonian region of South America, wherein ethnic groups use the plant to treat diseases, including gastric disorders. However, despite its widespread popular use, this species has yet to be assessed for its anti-ulcer effects. Aim of the study: In this study, we aimed to evaluate the in vivo gastroprotective and gastric healing activities of an aqueous extract of the bark of Uncaria tomentosa (AEUt) and sought to gain an understanding of the pharmacological mechanisms underlying these biological effects. Materials and methods: To verify the gastroprotective properties rats were treated with AEUt (30, 60, or 120 mg/ kg) prior to inducing gastric ulceration with ethanol or piroxicam. Additionally, the involvement of nitric oxide, non-protein sulfhydryl compounds (NP-SH), alpha-2 adrenergic receptors, and prostaglandins was investigated. Furthermore, a pylorus ligature model was employed to investigate the antisecretory activity of AEUt. The gastric healing effects of AEUt (60 mg/kg) were examined in rats in which ulceration had been induced with 80% acetic acid, whereas the quality of healing was evaluated in mice with interleukin-induced recurrent ulcers. We also evaluated the in vivo thickness of the gastric wall using ultrasonography. Moreover, the levels of reduced glutathione (GSH) and malondialdehyde (MDA) were evaluated in ulcerated mucosa, and we determined the activities of the enzymes myeloperoxidase (MPO), N-acetyl-8-D-glycosaminidase, superoxide dismutase, catalase, and glutathione S-transferase. In addition, we assessed the effects of AEUt on cell viability and subjected the AEUt to phytochemical analyses. Results: Administration of the AEUt (60 or 120 mg/kg) prevented ethanol- and piroxicam-induced ulceration, which was also confirmed histologically. Moreover, we observed that pre-treatment with NEM and indomethacin abolished the gastroprotective effects of AEUt, thereby indicating the involvement of NP-SH and prostaglandins in these protective effects. In addition, we found that the administration of AEUt had no appreciable effects on the volume, acidity, or peptic activity of gastric juice. Furthermore, the AEUt (60 mg/kg) accelerated the gastric healing of acetic acid-induced ulcers by 46.2% and ultrasonographic findings revealed a reduction in the gastric wall thickness in this group. The gastric healing effect of AEUt was also accompanied by a reduction in MPO activity. The AEUt (60 mg/kg) also minimized ulcer recurrence in mice exposed to IL-18 and was associated with the maintenance of GSH levels and a reduction in MDA contents. We deduce that the biological effects of AEUt could be associated with the activities of polyphenols and the alkaloids isomitraphylline and mitraphylline, identified as predominant constituents of the AEUt. Furthermore, we found no evidence to indicate that AEUt would have any cytotoxic effects. Conclusion: Collectively, our findings provide compelling evidence indicating the therapeutic efficacy of U. tomentosa. Our data indicate that compounds in AEUt confer gastroprotection and that this preventive effect of AEUt was accompanied by gastric healing and a reduction in gastric ulcer recurrence. Moreover, we provide evidence to indicate that the gastroprotective and gastric healing effects involve the antioxidant system and anti-inflammatory responses that contribute to preserving the gastric mucosa.
Tanacetum parthenium is popularly used to treat gastric disorders. However, the gastroprotective activity has not yet been tested. This study evaluated the anti-ulcer gastric effects of hydroalcoholic extract from T. parthenium (HETp) and parthenolide (PTL), its bioactive compound. Our findings revealed a significant reduction in HETp (10, 30, or 100 mg/Kg) and PTL (5 and 50 mg/Kg) in ethanol and piroxicam-induced ulcers, and this evidence was corroborated histologically. In addition, we explored the acid antisecretory activity by the pylorus ligation. Moreover, in mice pre-treated with the inhibitors indomethacin, L-NAME, and yohimbine, the antiulcerogenic effects of HETp and PTL were abolished, suggesting the involvement of nitric oxide, adrenergic receptors and prostaglandins in gastroprotective effects. Additionally, HETp and PTL prevented the depletion of SOD and CAT and decreased the activity of MPO and the levels of GSH and LPO. The results suggest that gastroprotection of HETp and PTL involves different pharmacological pathways.
Fridericia chica is an Amazonian plant used to treat stomach disorders. However, the pharmacological activity of flavonoids in the extract has yet to be investigated. Therefore, we considered that a flavonoid-rich F. chica subfraction (FRS) has gastroprotective functions. For this, before the induction of gastric ulcers with ethanol or piroxicam, the rats received vehicle (water), omeprazole (30 mg/kg), or FRS (30 mg/kg), and the ulcer area was measured macro and microscopically, and the antisecretory action was investigated in pylorus-ligated rats. In addition, the roles of nitric oxide (NO) and nonprotein sulfhydryl compounds (NP–SH) in the gastroprotective effects of FRS were studied. FRS reduced ethanol- and piroxicam-induced ulcerations by 81
Fridericia chica is widely distributed in Brazil, where it is commonly known as crajiru or pariri in several regions. Despite its popular use for treating inflammations and as an insect repellent, there has been limited assessment of its chemical and biological properties, including its bioinsecticide activities. In this study, we conducted phytochemical analyses and investigated the larvicidal and repellent effects of F. chica against the mosquito Aedes aegypti. The F. chica (HEFc) hydroalcoholic extract was partitioned using column chromatography, and subfractions were analyzed using chromatographic and spectroscopic analyses (ESI-IT-MSn and NMR). In addition, HEFc was evaluated for its larvicidal and repellent activities. Phytochemical analyses revealed the presence of 17 constituents, including 2,4-dihydroxybenzoic and p-coumaric acids, along with umbelliferone, acetovanilone, myricetin-3-O-glucuronide, and cis-isorhapontigenin, which are reported for the first time in this species. Although no larvicidal effect was observed at the doses tested, the HEFc exhibited promising repellent effects against A. aegypti, which aligns with its ethnopharmacological potential. In addition, molecular docking studies demonstrated that the compounds of HEFc interacted efficiently with insect odorant binding proteins (OBPs), providing repellent effects. Consistent with the chemical profile and in silico studies, preparations of F. chica have considerable repellent potential.
Sonchus oleraceus L. is an edible and medicinal plant used to treat stomachache and gastric ailments around the world. Thus, this study aimed to determine the gastroprotective mode of action of hydroalcoholic extract of S. oleraceus (HES). Mice were treated with HES before induction of gastric ulceration by ethanol/HCl. The area and histological appearance of ulcers were quantified, and mucus was measured histochemically. The effects of HES on inflammatory and oxidative markers were assessed in the ulcerated tissue. In addition, we investigated the gastric acid antisecretory activity of HES in pylorus-ligated rats. Chemical analyses of HES and its antioxidant activity were also performed in vitro. The HES (30 or 300 mg/kg) reduced the ulceration by 71.5 and 76.2%, respectively, compared with vehicle (p < 0.001), and the histological analysis confirmed the macroscopic results with elevation in mucin levels by 361.4 and 477.5%, respectively, compared with vehicle (p < 0.001). Moreover, the gastroprotection was accompanied by increases in GSH levels and in SOD, CAT, and GST activities; in parallel to a reduction in MPO activity and TNF levels. Furthermore, HES reduced the total acidity, and pepsin activity of the gastric juice of rats by 61 and 63%, respectively, compared to the vehicle. Phytochemical analysis indicated that luteolin-7-O-β-D-glucoside is the main active compound annotated in HES. Was also found that HES scavenged the DPPH radical with an IC50 of 15.41 μg/mL. In conclusion, the gastroprotective effects of HES involve reductions in oxidative stress and inflammatory injury, in conjunction with an increase in mucus layer and inhibition of gastric secretion. This study advances in elucidating the modes of the antiulcer potential of S. oleraceus and contributes to the prospection of new gastroprotective molecules.
Aloysia citriodora Palau is popularly used to treat nervous disorders. Experimental evidence has indicated that verbascoside (VBS) isolated from A. citriodora has pharmacological potential. In this study, we evaluated the antidepressant-like effects of a hydroalcoholic extract of A. citriodora (HEAc) and VBS against lipopolysaccharide- (LPS-) induced depressive-like behavior in mice. In the pretreatment protocol (performed to evaluate the preventive potential), mice were pretreated with HEAc (3, 30, or 300 mg/kg) or VBS (30 mg/kg) before the administration of LPS. In the posttreatment protocol (performed to evaluate the therapeutic potential), mice were initially administered LPS and were subsequently given HEAc (3, 30, or 300 mg/kg) or VBS (30 mg/kg). In both treatments, the mice were submitted to an open-field test and tail suspension test (TST) at 6 and 24 h after LPS administration. The posttreatment evaluation revealed that HEAc (30 or 300 mg/kg) and VBS produced an antidepressant-like effect, as indicated by a reduction in the time spent with no movement in the TST. Moreover, HEAc (30 or 300 mg/kg) was found to reduce interleukin-6 (IL-6) levels and N-acetyl-glycosaminidase activity in the hippocampus, increase glutathione (GSH) levels in the hippocampus and cortex, and enhance IL-10 in the cortex and, at a dose of 300 mg/kg, reduced myeloperoxidase activity in the cortex. Contrastingly, no comparable effects were detected in mice subjected to the pretreatment protocol. Administration of VBS similarly reduced the levels of IL-6 in the hippocampus and increased GSH levels in the cortex. Our observations indicate that both HEAc and VBS show promising antidepressant-like potential, which could be attributed to their beneficial effects in reducing neuroinflammatory processes and antioxidant effects in the central nervous system.
Taraxacum officinale F.H. Wigg. belonging to the family Asteraceae is an edible medicinal plant distributed worldwide. This study aimed to determine the gastroprotective effects of aqueous extract of T. officinale (AETo) in rats using ultrasound, histological, and biochemical analyses. In this study, gastric ulceration was induced by ethanol or piroxicam. Rats were then treated with AETo (3, 30, or 300 mg/kg). The area and histological appearance of gastric ulcers were quantified, and histochemical analysis was performed. The activity of AETo on inflammatory and oxidative stress markers was assessed in the ulcerated tissue. In addition, we investigated the thickness of the gastric wall using the ultrasound technique. Moreover, chemical analyses of AETo were performed. In rats with ethanol- or piroxicam-induced ulcers, AETo reduced the ulceration area, elevated mucin level, and the gastroprotective effect was confirmed by histological analysis. The gastroprotective effect was accompanied by increased activities of SOD, CAT, and GST, as well as an increase in GSH level and reduction in MPO activity. Furthermore, AETo reduced the thickness of the gastric wall in rats. Phytochemical analysis of AETo indicated phenolic acids and flavonoids as the main active compounds. In conclusion, the gastroprotective effect of AETo involves reduction in oxidative stress and inflammatory injury and increase in mucin content. This study advances in the elucidation of mechanisms of gastric protection of T. officinale, contributes to the prospection of new molecules gastroprotective, and proposes the ultrasonographic analyses as a new gastroprotective assessment tool in preclinical studies.
The gastroprotective effects of Jacaranda puberula Cham., Bignoniaceae, a tree native to the Brazilian Atlantic Forest, were evaluated using two models of acute ulceration in mice: acidified ethanol- and non-steroidal anti-inflammatory-induced ulceration. The mice were divided into five groups and treated orally with vehicle, carbenoxolone, or hydroalcoholic extract obtained from the tested plant (3, 30, or 300 mg/kg). Results showed that the doses of 300 mg/kg decreased both acidified ethanol- and indomethacin-induced ulceration by 89% and 33%, respectively, compared to the vehicle (p < 0.001). These results were similarly to those obtained for the carbenoxolone-treated group. Gastroprotection was confirmed by histological analysis. The gastroprotective mechanisms involve reductions in inflammatory and oxidative stress markers, including a reduction in myeloperoxidase activity, along with increases in glutathione levels and superoxide dismutase activity. Jacaranone and verbascoside were identified as the active components.
The Aedes aegypti is the main vector of the transmission of diseases such as dengue, yellow fever, Chikungunya, and Zika. The agents used for the control of mosquito involve the use of synthetic compounds, which may cause toxicity and contamination environmental. Aiming to test the effectiveness of natural products, the aim of this study was to evaluate the larvicidal and repellent activity of extracts of Ateleia glazioveana Baill. (timbó) and essential oil of Ocimum basilicum L. (manjericão), against A. aegypti. The activities of hydroalcoholic (HEA) and dichloromethane (DEA) extracts from A. glazioveana against A. aegypti larvae were assessed after exposure for 24, 48, and 72 h, using water and Bacillus thuringiensis israelensis as negative and positive controls, respectively. For repellent evaluation, we investigated the sting attempts of A. aegypti in response to the application of HEA- and DEA-based body creams (5%), as well as an alcoholic spray based on the essential oil from O. basilicum. The repellency of these preparations was compared with negative (vehicle) and positive (DEET) controls. Although HEA showed no apparent larvicidal activity, DEA at concentrations of 150 to 500 mg/ml showed high larvicidal potential after 24 h, compared to the negative control group (p < 0.001). Moreover, the DEA-based cream and the alcoholic spray of O. basilicum based essential oil showed higher repellency compared with the vehicle (84.5% and 70.5%, respectively). Accordingly, it is possible to infer that extracts and preparations of A. glazioveana and O. basilicum exhibit larvicidal and repellent activity against A. aegypti.
Natural products and especially medicinal plants, have been extensively studied and have exhibited antiproliferative effects. The species Eugenia uniflora L. (Myrtaceae) is native to Brazil and distributed throughout Australia, East Asia, and the Americas. The leaves are commonly used for the treatment of diarrhea, fever, and hypertension. However, the chemical properties and antiproliferative potential of the extracts remain to be elucidated. In this work, the antiproliferative effects of hydroethanolic (HEE) and dichloromethane (DEE) extracts of leaves from E. uniflora against a panel of human tumor cell lines in vitro were evaluated. Quercetin was identified using an HPLC, and the chemical component β-sitosterol was isolated. The HEE was an inactive extract, whereas the DEE extract showed antiproliferative activity against OVCAR-3 ovarian cells. In a bioassay-guided process, more pronounced antiproliferative effects were found for β-sitosterol isolated from DEE, which demonstrated potent antiproliferative effects against glioblastoma (U-251 cells) and leukemia (K-562 cells). This study contributes to the knowledge of E. uniflora and suggests that β-sitosterol is a potential chemotherapeutic compound.
BACKGROUND:Considering the pharmacological potential of solidagenone from Solidago chilensis, the present investigation was carried out to evaluate its antidepressant-like effect in mice with bacterial lipopolysaccharide (LPS)-induced depressive like behavior and its mode of action through the measurement of neuroinflammatory and oxidative markers.MATERIALS AND METHODS:In the prophylactic test, the mice were pretreated with solidagenone (1, 10 or 100 mg/kg, p.o) and after one hour received LPS. In therapeutic test, the mice received LPS and after 5 h were treated with solidagenone (1, 10 or 100 mg/kg, p.o). In both experimental approaches, the animals were submitted to OFT and to the TST after 6 and 24 h of the LPS administration, respectively. One hour after the TST the animals were euthanized, the blood was collected, the cortex was removed and biochemical analyzes were performed for measurement of the inflammatory and oxidative stress markers.RESULTS:The LPS induced sickness- and depressive-like behaviors and increased the cortical activity of myeloperoxidase (MPO), as well as the IL-6 and TNF amount. Interestingly, the pretreatment with solidagenone at 100 mg/kg avoided the behavioral alterations in OFT. In the mice post treated with solidagenone, all tested doses of resulted in an antidepressant-like effect evidenced by the decrease in immobility time in the TST. This effect was accompanied by a decrease in the MPO activity and in the IL-6 and TNF levels in the cortex in parallel to the increase in catalase activity.CONCLUSIONS:The solidagenone has a promissor antidepressant-like potential, which can result of its beneficial action in the neuroinflammation process and due its antioxidant capability at the central nervous system.
Natural products, especially phytochemicals, have been extensively studies and have exhibited important antiproliferative effects. The American native species Urera baccifera (L.) Gaudich. ex Wedd. (Urticaceae) is widely distributed in Brazil, where it is known as urtiga-vermelha or urtigao. The leaves are popularly used as anti-inflammatory, antirheumatic and in the treatment of gastric disorders. However, the antiproliferative potential of this plant against human tumor cells remain to be elucidated. In this study, we evaluated the antiproliferative effects of U. baccifera leaves extracts and fractions against a panel of human tumor cell lines in vitro besides a chemical evaluation of the most active sample by mass spectrometry (ESI-IT-MSn). The hydroalcoholic extract was inactive while dichloromethane extract showed moderate cytostatic activity against ovarian carcinoma cell line (OVCAR-3, GI(50) = 1.5 mu g/mL). More, the ethyl acetate and n-butanol fractions did not show important activity against tumour cell while the dichloromethane and hexane fractions showed moderate cytostatic activity against ovarian tumor cell line (OVCAR-3, GI(50) = 12.7 and 9.4 mu g/mL, respectively). Finally, the chemical profile evaluated by mass spectrometry (ESI-IT-MSn) allowed the detection of flavonoids in the HEU and hydroxylated fatty acid in DEU that can explain partially the biological effects observed. This is the first report of the antiproliferative effects of U. baccifera, and DEU has shown potential as a promising source of bioactive compounds.
Natural products have been reported as a main source of anticancer molecules. The species Celtis iguanaea (Jacq.) Sarg., (Cannabaceae) is widely distributed in Brazil where it is known as “esporão-de-galo or taleira”. The leaves are popularly used as anti-inflammatory, in the treatment of body pain and urinary infections. However, the antiproliferative potential against human cancer cells remain to be elucidated. In this study, extracts and different fractions from the leaves of C. iguanaea were tested in vitro, against a panel tumor cell lines. The hydroalcoholic extract was inactive, while dichloromethane extract showed promisor antiproliferative effects. In turn, the dichloromethane fraction showed potent cytostatic activity against ovarian cell line (OVCAR-3, GI50 = 4.65 mg/ml). However, the stronger antiproliferative effects with high selectivity were observed for the hexane fraction that exhibited activity against ovarian (GI50 = 3.99 mg/ml) and colon (HT-29, GI50 = 3.16 mg/ml). The antiproliferative effects observed are probably related to the presence of 3,7,11,15-tetramethyl-2-hexadecen-1-ol and gamma-sitosterol present in the hexane fraction and detected by GC/MS. This is the first report of antiproliferative activity of C. iguanaea and the results suggested that the molecules of fraction hexane are promising chemotherapeutic compounds, especially against tumor cell of ovarian and colon.
Plants are considered among the main sources of biologically active chemicals. The species Solidago chilensis Meyen, Asteraceae, is native to the southern parts of South America, where the aerial parts of the plant are commonly used for the treatment of inflammatory conditions. However, the effects of S. chilensis on human cancer cells remain to be elucidated. In this study, we evaluated the antiproliferative effects of the hydroalcoholic and dichloromethane extracts of S. chilensis, as well as their chemical constituents quercitrin and solidagenone against the five human tumor cell lines in vitro. The dichloromethane extract showed a promisor antiproliferative effects in vitro, especially against glioma cell line. Besides, the hydroalcoholic extract and quercitrin were inactive. The diterpene solidagenone showed highly potent antiproliferative effects against breast (MCF-7), kidney (786-0), and prostate cancer (PC-3) cells (total growth inhibition: TGI<6.25μg/ml). Solidagenone meets the theoretical physico-chemical criteria for bioavailability of drugs, according to the “Rule of Five” and, by theorical studies, the observed biological effects were probably related to the interaction of the molecule with nuclear receptors and as an enzymatic inhibitor. This study contributes to chemical study and to the identification of antiproliferative molecules in S. chilensis.