Trollioside, a new compound from the flowers of Trollius chinensis

A new compound, named trollioside, together with nine known compounds, proglobeflowery acid, isoswertisin, isoswertiajaponin, cirsimaritin, veratric acid, vitexin, orientin, β-sitosterol and daucosterol, were isolated from the ethanol extract of the dried flowers of Trollius chinensis Bunge. The isolation and structural determination of these compounds are discussed.     

Hepatic,gastric, and intestinal first-pass effects of vitexin in rats

Context: Recent research has demonstrated that vitexin exhibits a prominent first-pass effect. In this light, it is necessary to investigate the causes of this distinct first-pass effect.

Objective: The aim of this study was to evaluate hepatic, gastric, and intestinal first-pass effects of vitexin in rats and, furthermore, to investigate the role of P-glycoprotein (P-gp) and cytochrome P450 3A (CYP3A) in the absorption and secretion of vitexin in the duodenum.

Materials and methods: Vitexin was infused into rats intravenously, intraportally, intraduodenally, and intragastrically (30?mg/kg). In addition, verapamil (50?mg/kg), a common substrate/inhibitor of P-gp and CYP3A, was also instilled with vitexin into the duodenum to investigate the regulatory action of P-gp and CYP3A. The plasma concentrations of vitexin were measured by the HPLC method using hesperidin as an internal standard.

Results: The hepatic, gastric, and intestinal first-pass effects of vitexin in rats were 5.2%, 31.3%, and 94.1%, respectively. In addition, the total area under the plasma concentration–time curve from zero to infinity (AUC) of the vitexin plus verapamil group and of the normal saline group was 44.9 and 39.8?μg??min/mL, respectively.

Discussion and conclusion: The intestinal first-pass effect of vitexin was considerable, and gastric and hepatic first-pass effects also contribute to the low absolute oral bioavailability of vitexin. The AUC of the vitexin plus verapamil group was slightly higher than that of the vitexin plus normal saline group (by approximately 1.13-fold), suggesting that verapamil does not play an important role in the absorption and secretion of vitexin.     

Flavone C-glycosides from the flowers of Trollius chinensis and their anti-complementary activity

Phytochemical investigation of ethanol extract from the flowers of Trollius chinensis Bunge resulted in the isolation of two new flavone C-glycosides (1–2), along with 10 known compounds (3–12). The structures of the new compounds were established as 6?-(3-hydroxy-3-methylglutaroyl)-2″-O-β-d-galactopyranosyl orientin (1) and 6?-(3-hydroxy-3-methylglutaroyl)-2″-O-β-d-galactopyranosyl vitexin (2) on the basis of various spectroscopic analysis (including different 1D and 2D NMR spectroscopies, high-resolution electrospray ionization mass spectrometry) and chemical evidences. Bioassay showed that eight flavonoids inhibited complement activation on the classic pathway in vitro, with their IC₅₀ values ranging from 0.88 to 4.02 mM, which may contribute to the applications of the herb in treatment of acute respiratory distress syndrome, etc.     

Quantitative HPLC estimation of flavonoids in showy tick trefoil herbs

Quantitative and qualitative analysis of flavonoids in showy tick trefoil [Desmodium canadense (L.) DC., Fabaceae] herbs collected in various vegetative phases at the Department of Medicinal Herbs of the Kaunas Botanical Garden (Vytautas Magnus University) was performed using HPLC techniques. A total of 15 flavonoids were identified as aglycons and glycosides including apigenin, apigenin-7-O-glycoside, luteolin, rutin, vicenin-2, vitexin, isovitexin, vitexin rhamnoside, orientin, homoorientin, quercitrin, quercetin, hyperoside, astragalin, and kaempferol. The maximum amount of identified flavonoids (13573.83 μg/g) was observed at the budding stage. Among these flavonoids, orientin and homoorientin (6236.24 μg/g), vicenin-2 (2040.25 μg/g), vitexin (1717.12 μg/g), isovitexin (1767.82 μg/g), and rutin (925.72 μg/g) predominated.     

Assessment of bioactive metabolites and hypolipidemic effect of polyphenolic-rich red cabbage extract

Context: Cardiovascular disease is the leading cause of death worldwide and the consumption of red cabbage (Brassica oleracea var. capitata f. rubra DC. – Brassicaceae) has been linked with the reduction risk of chronic diseases.

Objective: The present study assesses the bioactive metabolites and hypolipidemic effect of red cabbage on rats.

Materials and methods: The content of total phenols, flavonoids, anthocyanins, carotenoids, ascorbic acid and antioxidant capacity were assessed, while individual phenolic acids and flavonoids were detected using reverse phase-high performance liquid chromatography (HPLC) analysis. Acute hypolipidemic activity of aqueous extract of red cabbage (RC – 125, 250 and 500?mg/kg) was investigated using a Triton WR-1339 (400?mg/kg) induced hyperlipidemic Wistar rats compared to fenofibrate (65?mg/kg).

Results: The HPLC analysis of extracts revealed eight phenolic acids, gallic, protocatechuic, p-hydroxybenzoic, m-coumaric, syringic, caffeic, cinnamic, dicaffeoylquinic and three flavonoids, epicatechin, epigallocatechin, gallocatechin. Furthermore, the aqueous extract showed higher amounts of total phenolics (116.00?mg/g), flavonoids (161.32?μg/g) and, antioxidant activity (87.19%) than the hydromethanolic (89.33?mg/g, 123.34?μg/g and 75.07%), respectively. The RC significantly (p < 0.001) ameliorated the levels of cholesterol, triglycerides and lipoproteins alterations in hyperlipidemic rats without toxicity.

Discussion and conclusion: Herein, the RC presented the higher amounts of phenolics and flavonoids comparing with the hydromethanolic extract. Additionally, the RC showed as the majority compounds, dicaffeoylquinic and cinnamic acids, and the flavonoids epicatechin and gallocatechin. Furthermore, the RC demonstrated a beneficial effect against hypercholesterolemia and hypertriglyceridemia, demonstrating its potential therapeutic effect on these risk factors of cardiovascular diseases.     

Quantitative hplc estimation of flavonoids in showy tick trefoil (<Emphasis Type="Italic">Desmodium canadense</Emphasis>) herbs

Quantitative and qualitative analyses of flavonoids in showy tick trefoil (Desmodium canadense L., Fabaceae) herbs during various vegetative phases were performed using HPLC techniques at the Department of Medicinal Herbs of the Kaunas Botanical Garden (Vytautas Magnus University). A total of 15 flavonoids of aglycone and glycoside nature was determined including apigenin, apigenin-7-O-glycoside, luteolin, rutin, 2-vicenin, vitexin, isovitexin, vitexin rhamnoside, orientin, homoorientin, quercitrin, quercetin, hyperoside, astragalin, and kaempferol. The maximum amount of identified flavonoids was observed during the flowering phase and was 2.45% in the second vegetative year and 1.28% in the sixth vegetative year, i.e., it decreased constantly during the plant perennial vegetation process. Of these, orientin and homoorientin varied from 45.9 to 38.9% of the total flavonoids; 2-vicenin, from 16.3 to 12.8; vitexin, from 12.7 to 8.6; isovitexin, from 13.0 to 7.7; rutin, from 11.6 to 6.9. The optimum collection time of showy tick trefoil herbs as plant raw material was the flowering and budding phases of herbs regrowing after mowing. The recommended optimal exploitation time of a plantation is up to six years.     

Chemical composition and biological activities of Helicteres vegae and Heliopsis sinaloensis

Context: Helicteres vegae Cristóbal (Sterculiaceae) (Hv) and Heliopsis sinaloensis B.L. Turner (Asteraceae) (Hs) are endangered and poorly studied plant species; related plants have been used against chronic-degenerative and infectious diseases. Therefore, Hv and Hs could be sources of bioactive compounds against these illnesses.

Objective: To determine the chemical composition and biological activities (antioxidant, antimutagenic and antimicrobial) of Hv and Hs leaves (L) and stems (S).

Materials and methods: Methanol extracts (ME) of each plant/tissue were evaluated for their phytochemicals; phenolics (HPLC-DAD-ESI-MS); antioxidant activity (AA) (0.125–4?mg/mL) (DPPH, ABTS, ORAC and β-carotene discoloration); antimutagenicity (0.5 and 1?mg/plate) (Ames assay, tester strain Salmonella enterica serovar Typhimurium YG1024, 1-nitropyrene as mutagen); activity against human pathogens (1?mg/mL); and toxicity (0.01–2?mg/mL) (Artemia salina assay).

Results: All ME showed flavonoids and triterpenes/steroids. The ME-SHv had the highest content of total phenolics (TP) (2245.82?±?21.45?mg GAE/100?g d.w.) and condensed tannins (603.71?±?1.115?mg CE/100?g d.w.). The compounds identified were flavonoids (kaempferol 7-O-coumaroylhexoside, and two kaempferol 7-O-rhamnosylhexosides) and phenolics [rosmarinic acid, and 3′-O-(8″-Z-caffeoyl) rosmarinic acid]. The ME-LHs showed the highest content of flavonoids (357.88?mg RE/g d.w.) and phenolic acids (238.58?mg CAE/g d.w.) by HPLC. The ME-SHv showed the highest AA. All ME were strong antimutagens (63.3-85.7%). Only the Hs extracts were toxic (ME-LHs, LC₅₀?=?94.9?±?1.7?μg/mL; ME-SHs, LC₅₀?=?89.03?±?4.42?μg/mL).

Discussion and conclusions: Both Hv and Hs are potential sources of preventive and therapeutic agents against chronic-degenerative diseases.     

Phytochemical analysis and antioxidant activity of Lycium barbarum (Goji) cultivated in Greece

Context: The fruit of Lycium barbarum L. (Solanaceae), known as goji berry, has been exploited for a long time in traditional Chinese medicine. In recent decades, it has received much attention as one of the trendiest functional foods with a wide array of pharmacological activities in Western diets.

Objective: In this study the phenolic profile and potential antioxidant capacity of Lycium barbarum cultivated in Crete (Greece) were investigated.

Materials and methods: The berries were defatted with hexane and then extracted with dichloromethane and methanol using a Soxhlet apparatus. Furthermore, the methanol extract was fractionated with ethyl acetate and butanol. All fractions/extracts were tested for their antioxidant activity (DPPH, FRAP, chemiluminescence). Folin–Ciocalteu and LC-DAD-MS analyses were utilized for the identification of the phenolic compounds.

Results: The total phenolic content ranged from 14.13?±?0.40 (water fraction) to 109.72?±?4.09 (ethyl acetate fraction) mg gallic acid equivalent/g dry extract. Ethyl acetate extract exhibited the highest scavenging activities determined as EC₅₀ (4.73?±?0.20?mg/mL) and IC₅₀ (0.47?±?0.001?mg/mL) using DPPH and chemiluminescence assays. Seventeen phenolic compounds, including cinnamoylquinic acids and derivatives, hydrocinnamic acids and flavonoid derivatives, were tentatively identified. To the best of our knowledge, quercetin 3-O-hexose coumaric ester and quercetin 3-O-hexose-O-hexose-O-rhamnose are reported for the first time in goji berry fruits.

Discussion and conclusion: The results of this study suggest that consumption of goji berry fruits could serve as a potential source of natural antioxidant compounds and that goji berry phenolic extracts could be exploited for nutritional pharmaceutical purposes.     

Insights into the intestinal bacterial metabolism of flavonoids and the bioactivities of their microbe-derived ring cleavage metabolites

Abstract

Flavonoids are a group of phytochemicals widely distributed in plants, fruits, and vegetables that possess numerous bioactivities. After oral administration, flavonoids can be metabolized by the intestinal bacteria into a wide range of low-molecular-weight phenolic acids. In this review, the intestinal bacterial metabolic pathways of different flavonoids (flavones, isoflavones, flavonols, flavanones, and chalcones) and the bioactivities of their microbe-derived ring cleavage metabolites are summarized. Flavonoids undergo different intestinal bacterial metabolic reactions, depending on the characteristics of their structure. Free hydroxyl groups, especially 5 and 4’ free hydroxyl groups play significant roles in fission metabolism. Microbe-derived ring cleavage metabolites such as 3,4-dihydroxyphenylacetic acid (3,4-DHPAA) and 3,4-dihydroxytoluene (3,4-DHT) possess various bioactivities including antioxidant, anti-inflammatory, antidiabetic, neuroprotective, and anti-colon cancer effects. Also, the intestinal bacteria associated with the bacterial metabolism of flavonoids are covered in this review.     

Role of glucose transporters in the intestinal absorption of gastrodin,a highly water-soluble drug with good oral bioavailability

Abstract

Gastrodin, a sedative drug, is a highly water-soluble phenolic glucoside with poor liposolubility but exhibits good oral bioavailability. The current study aims to investigate whether glucose transporters (GLTs) are involved in the intestinal absorption of gastrodin. The intestinal absorption kinetics of gastrodin was determined using the rat everted gut sac model, the Caco-2 cell culture model and the perfused rat intestinal model. In vivo pharmacokinetic studies using diabetic rats with high GLT expression were performed. Saturable intestinal absorption of gastrodin was observed in rat everted gut sacs. The apparent permeability (Papp) of gastrodin from the apical (A) to basolateral (B) side in Caco-2 cells was two-fold higher than that from B to A. Glucose or phlorizin, a sodium-dependent GLT (SGLT) inhibitor, reduced the absorption rates of gastrodin from perfused rat intestines. In vivo pharmacokinetic studies showed that the time of maximum plasma gastrodin concentration (T_max) was prolonged from 28 to 72?min when orally co-administered with four times higher dose of glucose. However, the T_max of gastrodin in diabetic rats was significantly lowered to 20?min because of the high intestinal SGLT1 level. In conclusion, our findings indicate that SGLT1 can facilitate the intestinal absorption of gastrodin.     

Antioxidant and urease inhibitory C-glycosylflavonoids from Celtis africana

Two new C-glycosylflavonoids celtisides A (1) and B (2) have been isolated from n-butanol-soluble fraction of Celtis africana, along with five known C-glycosylflavonoids vitexin (3), orientin (4), isoswertiajaponin (5), isoswertisin (6), and 2″-O-rhamnosyl vitexin (7) reported for the first time from this species. Their structures were assigned from 1D and 2D NMR spectra. These compounds were investigated for biological activities and showed significant antioxidant and urease inhibitory activities.     

Gastroprotective activity of the resin from Virola oleifera

Context: The resin from the trunk wood of Virola oleifera (Schott) A. C. Smith (Myristicaceae) is used in folk medicine to hasten wound repair and to treat pain and inflammatory conditions, and our previous report indicated the anti-oxidative properties in other oxidative stress model.

Objective: To investigate the protective effects of resin from V. oleifera in two experimental models of gastric ulcer oxidative-stress dependent.

Materials and methods: Plant material was collected and the resin was subjected to partitioning with organic solvents. The buthanol fraction was subjected to chromatographic and spectrometric methods for isolation and structural elucidation. The resin was quantified for polyphenols and flavonoids by colorimetric methods. Furthermore, the antioxidant activity of resin was determined by three different methods. The ulcers were induced acutely in Swiss male mice with ethanol/HCl and indomethacin using single-doses of 10 and 100?mg/kg. The gastroprotection of the experimental groups was comparable to reference control lansoprazole (3?mg/kg).

Results: The high content of polyphenols (～82%) and the presence of epicatechin and eriodictyol were determined. The LD₅₀ was estimated at 2500?mg/kg. At minimum (10?mg/kg) and maximum (100?mg/kg) dosage of resin, both in ethanol/HCl as indomethacin ulcer induction models demonstrate reduction of lesions (minimum: ～97% and ～66%; maximum: ～95% and ～59%).

Discussion: The gastroprotection might be related to tannins, phenolic acids and flavonoids present in the resin by antioxidant properties.

Conclusions: The results indicate that this resin has gastroprotective activity probably associated with the presence of phenolic antioxidant substances.     

金莲花汤中葛根素、牡荆素、迷迭香酸和咖啡酸的肠吸收研究

目的 考察金莲花汤中葛根素、牡荆素、迷迭香酸和咖啡酸的肠吸收特性,确定金莲花汤中活性成分。方法 采用HPLC法测定肠吸收样品中咖啡酸、葛根素、牡荆素、迷迭香酸,以大鼠肠外翻吸收实验和Caco-2细胞模型转运实验计算各成分的累积吸收量、吸收速率常数和表观渗透系数。结果 随着金莲花汤的质量浓度增加,咖啡酸、葛根素、牡荆素、迷迭香酸的吸收速率常数呈线性关系增加,符合零级吸收速率,且吸收率均小于1.4%,在肠道中吸收效果普遍较差,其中咖啡酸的吸收较为明显。各成分的表观渗透系数值大小为迷迭香酸>咖啡酸>葛根素>牡荆素。结论 金莲花汤中葛根素、牡荆素、迷迭香酸和咖啡酸均可在肠道中被吸收,吸收方式为被动扩散,咖啡酸和迷迭香酸可能是金莲花汤中发挥药效的活性物质,葛根素和牡荆素可能是前药。     

Antioxidant properties of Ferulago angulata and its hepatoprotective effect against N-nitrosodimethylamine-induced oxidative stress in rats

Context: Ferulago angulata (Schlecht.) Boiss. (Apiaceae) (FASB) is used to treat liver diseases and has been used both as food and therapeutics by many cultures for thousands of years because of the natural antioxidant compounds.

Objective: This study determines antioxidant properties of FASB flowers, the levels of minerals and vitamins, and also, evaluates the hepatoprotective effect of flowers against N-nitrosodimethylamine (NDMA) induced on liver tissue by assessing antioxidant enzymes and histopathological parameters in Wistar albino rats.

Materials and methods: In the study, the rats were divided into six groups of ten. Control, untreated animals were given 0.9% NaCl. Rats were intraperitoneally given NDMA (10?mg/kg) for the first 7 days. FASB methanol extract (150 and 300?mg/kg) was administered orally for 21 days.

Results: α-Tocopherol, retinol, ascorbic acid, total antioxidant activity, phenolic and flavonoid contents of FASB were 0.70?±?0.13, 0.29?±?0.03?μg/g, 139.32?±?7.06?μg/100?g, 171.61?±?6.05?mM ascorbic acid/g, 90.47?±?4.11?mg GA/g and 37.39?±?2.85?mg QE/g. DPPH and hydroxyl radical scavenging activity was obtained IC₅₀ 67.34?±?4.14 and 64.87?±?4.68?μg/mL, respectively.

Discussion and conclusion: The results of the study indicated that FASB flowers contain high levels of vitamins, minerals, total antioxidant activity, phenolics and flavonoids. Due to the positive effect on significant changes in antioxidant enzymes of liver tissue and histopathological examination, it is thought that the plant could be used as a hepatoprotective.     

Anti-inflammatory and anticancer effects of flavonol glycosides from Diplotaxis harra through GSK3β regulation in intestinal cells

Context and objective: Diplotaxis harra (Forssk.) Boiss. (Brassicaceae) is traditionally used as an antidiabetic, anti-inflammatory or anticancer agent. In these pathologies, the glycogen synthase kinase 3 β (GSK3β) is overactivated and represents an interesting therapeutic target. Several flavonoids can inhibit GSK3β and the purpose of this study was to search for the compounds in Diplotaxis harra which are able to modulate GSK3β.

Materials and methods: Methanol extracts from D. harra flowers were prepared and the bio-guided fractionation of their active compounds was performed using inflammatory [protease-activated receptor 2 (PAR₂)-stimulated IEC6 cells] and cancer (human Caco-2 cell line) intestinal cells. 50–100?μg/mL of fractions or compounds purified by HPLC were incubated with cells whose inhibited form of GSK3β (Pser9 GSK3β) and survival were analyzed by Western blot at 1?h and colorimetric assay at 24?h, respectively. LC-UV-MS profiles and MS-MS spectra were used for the characterization of extracts and flavonoids-enriched fractions, and the identification of pure flavonoids was achieved by MS and NMR analysis.

Results: The methanol extract from D. harra flowers and its flavonoid-enriched fraction inhibit GSK3β in PAR₂-stimulated IEC6 cells. GSK3β inhibition by the flavonoid-enriched D. harra fraction was dependent on PKC activation. The flavonoid-enriched D. harra fraction and its purified compound isorhamnetin-3,7-di-O-glucoside induced a 20% decrease of PAR₂-stimulated IEC6 and Caco-2 cell survival. Importantly, normal cells (non-stimulated IEC6 cells) were spared by these treatments.

Conclusion: This work indicates that flavonoids from D. harra display cytotoxic activity against inflammatory and cancer intestinal cells which could depend on GSK3β inhibition.     

Constituents of Cynara syriaca. Leaves

Abstract

Six flavonoids (apigenin, chrysoeriol, luteolin, apigenin 7-O.-glucoside, chrysoeriol 7-O.-glucoside, luteolin 7-O.-glucoside), four phenolic acids (caffeic acid, chlorogenic acid, 1,5-dicaffeoylquinic acid, cynarin), and three sesquiterpene lactones (11,13-dihydroxy-8-desoxygrosheimin, 11,13-dihydrodeacylcynaropicrin, solstitialin) were isolated from the leaves of Cynara syriaca. Boiss (Asteraceae). Three of these compounds, chrysoeriol, chrysoeriol 7-O.-glucoside, and 11,13-dihydrodeacylcynaropicrin, were isolated for the first time from Cynara. species. 11,13-Dihydroxy-8-desoxygrosheimin was isolated for the second time from a plant.     

Geographic origin influences the phenolic composition and antioxidant potential of wild Crataegus monogyna from Spain

Context: Crataegus monogyna Jacq L. (Lind.) (Rosaceae) is used in folk medicine as a sedative, aerial parts being rich in polyphenols with antioxidant ability.

Objectives: To study the variation in polyphenolic composition and antioxidant ability of spontaneous samples of C. monogyna in order to assess the relationship among these variables.

Materials and methods: Aerial parts of C. monogyna were collected from nine different locations in central Spain and extracted with methanol after drying. Total polyphenols were determined by the Folin-Ciocalteu method using gallic acid (GA) as standard. Sixteen polyphenolic compounds (11 flavonoids and 5 phenolic acids) were identified and quantified by reversed-phase HPLC in one single analysis. The antioxidant ability was evaluated by the oxygen radical absorbance capacity (ORAC) and the free radical scavenging activity (DPPH) methods. Linear correlation analysis was used to explore the relationships between the studied variables.

Results: Total polyphenol content ranged between 117.729?±?0.011 and 204.286?±?0.015?mg GAE/g extract, depending on the geographic origin. No relationship was found between total polyphenols and antioxidant ability by the ORAC or DPPH methods. Chromatographic analysis yielded lower amounts of polyphenols (23.3–143.26?mg/kg), as only flavonoids and phenolic acids were quantified. All the samples exhibited antioxidant activity between 1.32?±?0.08 and 2.76?±?0.007?μmol Trolox equivalents/mg and IC₅₀ from 0.82?±?0.10 to 3.76?±?0.67?μg/mL.

Conclusion: A statistically significant relationship between flavonoids and phenolic acids content and the antioxidant potential obtained by the ORAC method for C. monogyna samples was proven.     

Quantitative estimation of flavonoids in the vegetative and reproductive organs of showy tick trefoil (<Emphasis Type="Italic">Desmodium canadense</Emphasis>)

Qualitative and quantitative analysis of flavonoids in the vegetative and reproductive organs of showy tick trefoil [Desmodium canadense (L) DC., Fabaceae] herbs (stems, leaves, buds, inflorescences, legumes, and seeds) collected at various stages of vegetation at the Department of Medicinal Herbs of the Kaunas Botanical Garden (Vytautas Magnus University) was performed using HPLC techniques. A total of 15 flavonoids of aglycon and glycoside nature including apigenin, apigenin-7-O-glycoside, luteolin, rutin, vicenin-2, vitexin, isovitexin, vitexin rhamnoside, orientin, homoorientin, quercitrin, quercetin, hyperoside, astragalin, and kaempferol were identified. Among the vegetative organs, the maximum amount of flvaonoids was found in leaves, where the total content of flavonoids was 23,952.2 mg/g in the budding phase and reached a maximum of 25,472.71 mg/g (2.55%) at the ripening phase (1.88 times greater than in herbs at the beginning of flowering). In stems, the maximum amount of flavonoids (2,318.0 mg/g) was accumulated in the budding phase while the minimum (1,910.77 mg/g) was found at the beginning of seed ripening phase. the maximum amount of flavonoids in the reproductive organs was found in inflorescences, where the total content of flavonoids was 8,164.1 mg/g at the budding phase, reached a maximum of 15,226.39 mg/g in the full flowering phase, and then gradually decreased. Legumes at the beginning of ripening contained 8,892.3 mg/g flavonoids while seeds in the fully ripened phase contained only 4,270.1 mg/g (0.43%) flavonoids. Among the individual flavonoids, orientin and homoorientin predominated in all cases. Thus, not only the inflorescences of showy tick trefoil but also leaves can be used as medicinal raw material. The optimum time for collecting leaves for the raw material is from the budding phase until the beginning of fruit ripening.     

Nephroprotective and curative effects of Ficus religiosa latex extract against cisplatin-induced acute renal failure

Abstract

Context. Ficus religiosa L. (Moraceae) is widely planted in the tropics. Its chemical constituents include tannin, saponin gluanol acetate, β-sitosterol, leucoanthocyanidin and leucoanthocyanin which are used for the treatment of pain, inflammation, impotence, menstrual disturbances, uterine tonic and urine related problems.

Objective: To determine the possible nephroprotective and curative effects of F. religiosa latex methanol extract against cisplatin induced acute renal failure.

Materials and methods: Methanol extract was obtained by maceration process. Rats were divided in five groups. Group 1 was administered acacia (2% w/v) of 5?ml/kg throughout the experiment; group 2 was treated with single dose of cisplatin (5?mg/kg i.p.) on the 1st day; group 3 (200?mg/kg p.o.) of extract control for the 1st to 10th day, group 4 (200?mg/kg p.o.) of extract from the 1st to 10th day and a single dose of cisplatin (5?mg/kg, i.p.) on 11th day while group 5 received the same dose of cisplatin on day 1 and extract (200?mg/kg p.o.) from the 7th to 16th day.

Results: Phytochemical screening of the extract revealed the presence of glycoside, alkaloids, tannins (phenolic compounds), flavonoids and amino acids. The half maximal inhibitory concentration (IC₅₀) values of the extract were 31.75?±?0.12 and 18.35?±?0.48?µg/ml, respectively. The cisplatin-treated group 2 showed significant changes; renal functions, biochemical parameters and histopathology were significantly (**p?<?0.01) recovered by 200?mg/kg curative and protective groups.

Discussion and conclusion: These findings demonstrated that F. religiosa latex and constituents have excellent nephroprotective and curative activities and thus have great potential as a source for natural health products.     

Curcumin-loaded solid lipid nanoparticles with Brij78 and TPGS improved in vivo oral bioavailability and in situ intestinal absorption of curcumin

Abstract

Purpose: The present study was to formulate curcumin solid lipid nanoparticles (Cur-SLNs) with P-gp modulator excipients, TPGS and Brij78, to enhance the solubility and bioavailability of curcumin.

Methods: The formulation was optimized by Plackett–Burman screening design and Box–Behnken experiment design. Then physiochemical properties, entrapment efficiency and in vitro release of Cur-SLNs were characterized. In vivo pharmacokinetics study and in situ single-pass intestinal perfusion were performed to investigate the effects of Cur-SLNs on the bioavailability and intestinal absorption of curcumin.

Results: The optimized formulations showed an average size of 135.3?±?1.5?nm with a zeta potential value of ?24.7?±?2.1?mV and 91.09%?±?1.23% drug entrapment efficiency, meanwhile displayed a sustained release profile. In vivo pharmacokinetic study showed AUC_0→t for Cur-SLNs was 12.27-folds greater than curcumin suspension and the relative bioavailability of Cur-SLNs was 942.53%. Meanwhile, T_max and t_1/2 of curcumin for Cur-SLNs were both delayed comparing to the suspensions (p?<?0.01). The in situ intestinal absorption study revealed that the effective permeability (P_eff) value of curcumin for SLNs was significantly improved (p?<?0.01) comparing to curcumin solution.

Conclusion: Cur-SLNs with TPGS and Brij78 could improve the oral bioavailability and intestinal absorption of curcumin effectively.