Systematical Ingredient Investigations of Ficus tikoua Bur. Fruit and Immunoregulatory and Antioxidant Effects of Different Fractions.

Although the fruit of Ficus tikoua Bur. has been consumed by montanic people in China for centuries, its chemical and biological composition was still unclear. A series of comprehensive investigations on its chemical constituents and bioactivities were carried out for the first time. As a result, six compounds were isolated and identified as the main components in this fruit. GC-MS analysis of the lipid components demonstrated that Ficus tikoua Bur. fruit contains some wholesome constituents such as fatty acids, vitamins, triterpenoids, and phytosterols. The fatty acids are mainly composed of linolenic acid (61.27%) and linoleic acid (22.79%). Furthermore, this fruit contains a relative high content of crude protein (9.41 ± 0.03%), total amino acids (9.28%), and total polyphenols (0.86 ± 0.01 g/100 g). The analysis of monosaccharide composition showed that the total polysaccharide mainly consists of glucose, glucuronic acid, xylose, arabinose, mannose, galactose, galacturonic acid, and rhamnose. The polysaccharide, polyphenol, water, ethanol, and flavonoid extracts exhibited prominent antioxidant activity determined by ABTS, DPPH, and FRAPS methods. Meanwhile, the total polysaccharide exhibited significant immunomodulatory effect by enhancing the release of cytokines and expression of iNOS and COX-2 in RAW264.7 cells, significantly decreasing the expression of c-Jun and p65 proteins in the cytoplasm; increasing the translocation of c-Jun and p65 to the nucleus; and regulating the phosphorylation level of Akt, PI3K, and PDK1 in the PI3K/AKT signaling pathway. This study proved that the fruit of F. tikoua is a reliable source of functional food.

Effect of carbon nanoparticles on the growth and photosynthetic property of Ficus tikoua Bur. plant.

The application of nanomaterials in different plants exerts varying effects, both positive and negative. This study aimed to investigate the influence of carbon nanoparticles (CNPs) on the growth and development of Ficus tikoua Bur. plant. The morphological characteristics, photosynthetic parameters, and chlorophyll content of F. tikoua Bur. plants were evaluated under four different concentrations of CNPs. Results indicated a decreasing trend in several agronomic traits, such as leaf area, branching number, and green leaf number and most photosynthetic parameters with increasing CNPs concentration. Total chlorophyll and chlorophyll b contents were also significantly reduced in CNPs-exposed plants compared to the control. Notably, variations in plant tolerance to CNPs were observed based on morphological and physiological parameters. A critical concentration of 50 g/kg was identified as potentially inducing plant toxicity, warranting further investigation into the effects of lower CNPs concentrations to determine optimal application levels.

A new hemiacetal chromone racemate and α-glucosidase inhibitors from Ficus tikoua Bur.

From the petroleum ether and ethyl acetate portions of the 95% ethanol extract of Ficus tikoua Bur., a new hemiacetal chromone racemate, named (±)-ficunomone (1), together with twenty-two known flavonoids (2-23) were isolated. The new structure was elucidated by NMR, HRESIMS, and X-ray single-crystal diffraction analysis, and the known structures were determined by comparison of spectroscopic data with those reported from literatures. All the compounds were assayed for their inhibitory activities against yeast α-glucosidase, seven flavonoids could inhibit α-glucosidase, among which compounds 22 and 23 exhibited the highest inhibitory activity, with IC50 values at 5.12 ± 0.10 and 3.43 ± 0.15 µM respectively. Preliminary structure and relationship activity of all the compounds was analysed. Kinetic analysis of compounds 22 and 23 indicated that they are both uncompetitive inhibitors. Molecular docking studies revealed that they bound to amino acid residues of the α-glucosidase activity pocket.

New antifungal pyranoisoflavone from Ficus tikoua Bur.

Considering the undesirable attributes of synthetic fungicides and the availability of Ficus species in China, the stem of Ficus tikoua Bur. was investigated. One new antifungal pyranoisoflavone, 5,3',4'-trihydroxy-2″,2″-dimethylpyrano (5″,6″:7,8) isoflavone (1), together with two known isoflavones, wighteone (2) and lupiwighteone (3) (with previously reported antifungal activities), were isolated from ethyl acetate extract by bioassay-guided fractionation. Their structures were determined by spectroscopic analysis, such as NMR ((1)H-(1)H COSY, HMQC, HMBC and NOESY), IR, UV and HRMS, as well as ESI-MS(n) analyses. The antifungal activities of 1-3 against Phytophthora infestans were evaluated by direct spore germination assay, and the IC(50) values were 262.442, 198.153 and 90.365 µg·mL(-1), respectively.

Efficacy of Ficus tikoua Bur. extract in ethylene glycol-induced urolithiasis model in SD rats.

The development of new herbal preparations for the treatment of urolithiasis is an urgent task of medical science. Ficus have attracted the attention of pharmacologists due to a wide range of biological properties, including antioxidant, anti-inflammatory, antibacterial and antifungal activity. We studied the effectiveness of Ficus tikoua Bur. in SD rats in which urolithiasis was induced by 6 weeks of oral administration of ethylene glycol 0.5% ad libitum instead of drinking water. Administration of the extract of Ficus tikoua Bur., as well as comparative drug Cystone® after modeling of urolithiasis lead to the restoration of diuresis and the concentration of inorganic phosphates starting from the 6th week of the experiment. The use of the Ficus tikoua Bur. extract for 6 weeks, both during the modeling of urolithiasis and during the recovery period, led to the restoration of the percentage of lymphocytes in the blood, content of sodium, chlorine and inorganic phosphates in the blood to the control level. Thus, the extract of Ficus tikoua Bur. seems to be a promising drug for effective treatment of the initial stages of the development of urolithiasis.

In Vitro and In Vivo Evaluation of Antidiabetic Properties and Mechanisms of Ficus tikoua Bur.

In folk medicine, Ficus tikoua (F. tikoua) has been used to treat diabetes for a long time, but there is a rare modern pharmacological investigation for its antidiabetic effect and mechanisms. Our study aimed to evaluate its hypoglycemic effect using in vitro and in vivo experimental models and then explore the possible mechanisms. In the ethanol extracts and fractions of F. tikoua, n-butanol fraction (NBF) exhibited the most potent effect on inhibiting α-glucosidase activity (IC50 = 0.89 ± 0.04 µg/mL) and promoting glucose uptake in 3T3-L1 adipocytes. Further animal experiments showed that NBF could play an antidiabetic role by ameliorating random blood glucose, fasting blood glucose, oral glucose tolerance, HbA1c level, and islets damage in diabetic mice. Then, the activities of the five subfractions of NBF (NBF1-NBF5) were further evaluated; NBF2 showed stronger α-glucosidase inhibition activities (IC50 = 0.32 ± 0.05 µg/mL) than NBF. Moreover, NBF2 also possessed the ability to promote glucose uptake, which was mediated via P13K/AKT and AMPK pathways. This study demonstrated that F. tikoua possesses antidiabetic efficacy in vitro and in vivo and provided a scientific basis for its folk medicinal use. NBF2 might be potential natural candidate drugs to treat diabetes mellitus. It is the first time the antidiabetic activity and the potential mechanisms of NBF2 were reported.

A new benzofuran glucoside from Ficus tikoua Bur.

From the water-soluble portion of the methanol extract of stems of Ficus tikoua Bur., a new benzofuran glucoside, named 6-carboxyethyl-5-hydroxybenzofuran 5-O-ß-d-glucopyranoside (1), together with one known benzofuran glucoside (2) were isolated. Their structures were elucidated by 1D and 2D ((1)H-(1)H COSY, HMQC, and HMBC) NMR spectroscopy and HRMS techniques. The antioxidant activities of the isolated compounds were assayed based on the scavenging activities of DPPH free radical. Compounds 1 and 2 exhibited moderate antioxidant activities, and the IC(50) values were 242.8 µg·mL(-1) and 324.9 µg·mL(-1), respectively.

A new isoflavanone from Ficus tikoua Bur.

A new isoflavanone compound, ficustikounone A (1), together with 22 known flavones, was isolated from Ficus tikoua Bur. The structures of these isolates were determined by UV, ECD, HRESIMS, 1D and 2D spectral analyses.