Phytochemical Characterization, Antioxidant Activity, and Cytotoxicity of Methanolic Leaf Extract of Chlorophytum Comosum (Green Type) (Thunb.) Jacq.

Chlorophytum genus has been extensively studied due to its diverse biological activities. We evaluated the methanolic extract of leaves of Chlorophytum comosum (Green type) (Thunb.) Jacques, the species that is less studied compared to C. borivilianum. The aim was to identify phytoconstituents of the methanolic extract of leaves of C. comosum and biological properties of its different fractions. Water fraction was analyzed with matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry. Nineteen compounds belonging to different chemical classes were identified in the methanolic extract of leaves of C. comosum (Green type) (Thunb.) Jacques. In addition to several fatty acids, isoprenoid and steroid compounds were found among the most abundant constituents. One of the identified compounds, 4'-methylphenyl-1C-sulfonyl-ß-d-galactoside, was not detected earlier in Chlorophytum extracts. The water fraction was toxic to HeLa cells but not to Vero cells. Our data demonstrate that methanolic extract of leaves of C. comosum can be a valuable source of bioactive constituents. The water fraction of the extract exhibited promising antitumor potential based on a high ratio of HeLa vs. Vero cytotoxicity.

Investigation of the effective components inhibited macrophage foam cell formation in Ophiopogonis Radix.

ETHNOPHARMACOLOGICAL RELEVANCE: Ophiopogonis Radix, the commonly used traditional Chinese medicine in clinic for treating cardiovascular diseases, is returned to the stomach, lung and heart meridian. It is reported to nourish yin, moisten lung and is used to treat heart yin deficiency syndromes and asthenia of heart and lung, which indicated that Ophiopogonis Radix may have a protective effect on heart disorders. Atherosclerosisis is an important process in the development of cardiovascular diseases and abnormal lipid deposition induced macrophage foam cells is its crucial foundation. Our previous study showed the extract of Ophiopogonis Radix (EOR) ameliorates atherosclerosis in vitro. However, it may protect against cardiovascular diseases through inhibiting macrophage foam cell formation and its potential effective components and mechanisms are still unclear. AIM OF THE STUDY: Our study aimed to investigate the effect of Ophiopogonis Radix on macrophage foam cell formation and its potential active constituents and mechanisms. MATERIALS AND METHODS: Ox-LDL induced macrophage cells were employed to evaluate the effect of Ophiopogonis Radix on macrophage foam cell formation. Then the potential active constituents inhibited formation of macrophage foam cells were screened by biospecific cell extraction and its underlying mechanisms were also explored by Western blot. RESULTS: The extract of Ophiopogonis Radix was found to significantly inhibit macrophage foam cell formation, evidenced by the decrease of TG and TC and Oil Red O staining analysis in macrophage cells, which indicated that EOR reduced the formation of macrophage foam cells. At the same time, EOR was showed to increase antioxidant capacity in macrophage cells. After treatment with EOR, two potential active components interacted with macrophage foam cells specifically were identified to inhibit macrophage foam cell formation including methylophiopogonanone A and methylophiopogonanone B. Methylophiopogonanone A was then proved to decrease the expression of CD36, Lox-1 and SREBP2, increase the expression of ABCA1 obviously, while the expression of ABCG1 and SREBP1 had no changes. CONCLUSIONS: In our study, Ophiopogonis Radix was found to protect against atherosclerosis through suppressing ox-LDL induced macrophage foam cell formation and two potential compounds were identified by biospecific cell extraction including methylophiopogonanone A and methylophiopogonanone B. Moreover, methylophiopogonanone A was proved to inhibit foam cells through reducing uptake, synthesis and increasing efflux, which may provide guidance and reference for application of Ophiopogonis Radix and investigation of the effective components of TCMs.

High-performance thin-layer chromatography based approach for bioassay and ATR-FTIR spectroscopy for the evaluation of antioxidant compounds from Asparagus racemosus Willd. aerial parts.

Asparagus racemosus Willd. is widely used to combat various diseases owing to its medicinal properties. In this study, arial parts of A. racemosus were investigated for their total phenolic content, total flavonoid content and antioxidative potential. A high-performance thin-layer chromatography (HPTLC) method combined with effect-directed-analysis was also developed to screen the antioxidant effects of A. racemosus and quantify biologically active compounds on chromatograms from A. racemosus. Total phenolics (154 mg gallic acid equivalent/g), flavonoid contents (497 mg quercetin/g) and IC50 (15.25 µg/ml) were found to be higher in methanolic extract of A. racemosus than in n-hexane, chloroform and ethyl acetate extracts. HPTLC hyphenated with chemical derivatizations (DPPH•, p-anisaldehyde/sulfuric acid, and ferric chloride) was used to evaluate antioxidant activity and the presence of phytosterols, terpenoids and polyphenolic contents. The same compounds at 100*retention factor = 58, 68, 74 and 65 in extracts were responsible for antioxidant activity. Hyphenated HPTLC allowed a rapid characterization of the active compound with a combination of effect-directed-analysis and attenuated total reflectance-Fourier transform infrared spectroscopy. Spectral analysis of the band from attenuated total reflectance identified myricetin, quercetin, p-coumaric acid and caffeic acid as responsible for the antioxidant activity.

Phytochemical analysis of UV active and inactive bioactive compounds present in Polianthes tuberosa (Linn.) flower.

Polianthes tuberosa (Linn.) is traditionally considered an ornamental and medicinal plant worldwide. However, extensive studies on its phytochemical composition are very limited. Hence the present work aims to identify the total phytochemical ingredients present in different crude extracts of tuberosa. Phytochemical analysis has been carried out for differential cold solvent extracts of various parts of tuberosa such as petals, stamens, and ovary by gas chromatography coupled with mass spectrometry, ultra-performance liquid chromatography to quadrupole time-of-flight mass spectrometry, and evaporative light scattering detector analyzers for the identification of bioactive components. Among the various solvents used for the extraction, diethyl ether is found to be the most suitable and efficient solvent, as its total differential recovery from the crude extract is about 0.24% as compared to 0.04% obtained by using n-hexane or petroleum ether. Numerous phytochemicals have been identified by the chromatography and MS techniques, which demonstrate the presence of essential fatty acids along with other pharmacological importance phytoconstituents. Identification of additional phytochemicals present in the crude extract of tuberosa flower further enhances its biological and pharmacological significance. The present work lays a foundation for further research and development of phytoconstituents of the tuberosa flower.

Total saponins from Tupistra chinensis baker inhibits growth of human gastric cancer cells in vitro and in vivo.

ETHNOPHARMACOLOGICAL RELEVANCE: Tupistra chinensis Baker (syn. Rohdea chinensis), an antitumor folk herb mainly distributed in China, its rhizome has been historically used to treat gastric cancer. Studies showed that the steroidal saponins were the main bioactive components in the rhizome of T. chinensis. Our previous studies have confirmed that the steroidal saponins have a variety of anti-tumor activities. However, the underlying anti-tumor mechanism of the total steroidal saponins of T. chinensis (TCS) remains to be revealed. AIM OF THE STUDY: In the present study, we studied the potential anti-proliferative activity and anti-tumor mechanism of TCS on gastric cancer in vitro and in vivo. METHODS: In vitro, 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay was used to detect the proliferation ability of TCS on SGC-7901 cells and AGS cells. Flow cytometry were performed to analyze cell apoptosis, cell cycle, mitochondrial membrane potential and reactive oxygen species expression level. Western blotting was performed to validate the expression of proteins in related pathways. In vivo, a xenograft model was established by injecting SGC-7901 cells into nude mice. RESULTS: In vitro, TCS inhibited the proliferation of gastric cancer cells. TCS effectively induced apoptosis by PI3K/Akt/mTOR signaling pathway in SGC-7901 cells, and promoted apoptosis via p53-mediated pathway in AGS cells. TCS also exhibited inhibitory activity in blocking the migration of gastric cancer cells. In vivo, TCS significantly inhibited the growth of xenograft tumor. CONCLUSION: These results indicated that TCS exhibited significant anti-gastric cancer effects in vitro and in vivo.

Effects of triangle grass decoction on bone metabolism in rats with chronic kidney disease complicated with mineral and bone abnormalities.

ETHNOPHARMACOLOGICAL RELEVANCE: Triangle grass is a liliaceous Chlorophytum perennial herb of ChlorophytumlaxumR.Br. It is distributed mainly in Guangdong and Guangxi Provinces of China. The initial use of triangle grass was mainly to treat bone pain and swelling caused by a fall injury. Triangle grass tablets (NO. Z20070544) are also used as a preparation in our hospital because of their analgesic, anti-inflammatory, anti-snake venom and microcirculation improvement properties and other pharmacological effects (Mei et al., 2006). Triangle grass tablets have been widely used in our hospital to treat patients with bone pain from chronic kidney disease-mineral and bone disorder (CKD-MBD). However, the effects and mechanism of triangle grass on bone metabolism in chronic kidney disease complicated with mineral and bone abnormalities are unclear. AIM OF THE STUDY: The aim of the present study was to investigate the effects of a triangle grass decoction on bone metabolism in CKD-MBD rats. MATERIALS AND METHODS: CKD-MBD model rats were subjected to 5/6 nephrectomy combined with 0.5 g NaH2PO4/rat. Serum blood urea nitrogen (BUN), creatinine (Cr), phosphorus (P), calcium (Ca), and intact parathyroid hormone (iPTH) levels were measured with an automatic biochemical analyser. Bone mineral density was determined with a Viva CT 40 system. Bone morphogenetic protein 7(BMP-7),runt-related transcription factor 2 (Runx2) and Osterix protein levels were measured by Western blot analysis. Kidney, vertebra and thoracic aorta tissue samples were assessed by histopathology and immunohistochemistry (IHC). RESULTS: The degrees of membrane thickening, necrosis, swelling and cast deposition were significantly reduced in high-dose rats and Low-dose rats. Serum BUN levels were significantly reduced in the Pre-H group (P < 0.05). Hypocalcaemia and hyperphos phataemia were detected in triangle grass (P < 0.05, P < 0.05). In addition, iPTH levels were significantly increased in the Pre-H group (P < 0.05). Alkaline phosphatase (ALP)levels were significantly decreased in the Pre-H group (P < 0.05). The bone mineral density was improved in the Pre-H and Pre-L groups. BMP-7 protein levels were significantly increased in the Pre-H group (P < 0.05). The pathological changes in muscle fibres in the thoracic aorta middle membranes were significantly alleviated in rats in the Pre-H and Pre-L groups. Changes in SM22α and SMα-act in protein levels were significantly attenuated in the Pre-H group (P < 0.05, P < 0.05). Changes in Runx2 and Osterix protein levels were also significantly attenuated in the Pre-H and Pre-L groups (P < 0.05, P < 0.05). CONCLUSIONS: Triangle grass can simultaneously ameliorate vertebral bone loss and abnormal calcification in the thoracic aorta. Triangle grass has a definite effect on bone metabolism disorder in CKD-MBD rats.

Engineering Exosome-Like Nanovesicles Derived from Asparagus cochinchinensis Can Inhibit the Proliferation of Hepatocellular Carcinoma Cells with Better Safety Profile.

BACKGROUND: Exosomes are a type of membrane vesicles secreted by living cells. Recent studies suggest exosome-like nanovesicles (ELNVs) from fruits and vegetables are involved in tissue renewal process and functional regulation against inflammatory diseases or cancers. However, there are few reports on ELNVs derived from medicinal plants. METHODS: ELNVs derived from Asparagus cochinchinensis (Lour.) Merr. (ACNVs) were isolated and characterized. Cytotoxicity, antiproliferative and apoptosis-inducing capacity of ACNVs against hepatoma carcinoma cell were assessed. The endocytosis mechanism of ACNVs was evaluated on Hep G2 cells in the presence of different endocytosis inhibitors. In vivo distribution of ACNVs was detected in healthy and tumor-bearing mice after scavenger receptors (SRs) blockade. PEG engineering of ACNVs was achieved through optimizing the pharmacokinetic profiles. In vivo antitumor activity and toxicity were evaluated in Hep G2 cell xenograft model. RESULTS: ACNVs were isolated and purified using a differential centrifugation method accompanied by sucrose gradient ultracentrifugation. The optimized ACNVs had an average size of about 119 nm and showed a typical cup-shaped nanostructure containing lipids, proteins, and RNAs. ACNVs were found to possess specific antitumor cell proliferation activity associated with an apoptosis-inducing pathway. ACNVs could be internalized into tumor cells mainly via phagocytosis, but they were quickly cleared once entering the blood. Blocking the SRs or PEGylation decoration prolonged the blood circulation time and increased the accumulation of ACNVs in tumor sites. In vivo antitumor results showed that PEGylated ACNVs could significantly inhibit tumor growth without side effects. CONCLUSION: This study provides a promising functional nano platform derived from edible Asparagus cochinchinensis that can be used in antitumor therapy with negligible side effects.

Muscari comosum L. Bulb Extracts Modulate Oxidative Stress and Redox Signaling in HepG2 Cells.

Muscari comosum L. bulbs are commonly used as food in South Italy and also in folk medicine. By evaluating in vitro antioxidant activity and biological activities of their aqueous and methanol extracts, we shed light on the potential role, including both the nutraceutical and health benefits, of this plant. Total polyphenol content (TPC) and total flavonoid content (TFC) were evaluated by the Folin-Ciocalteu method and by the aluminum chloride method, respectively. Antioxidant activity was investigated by three in vitro assays and relative antioxidant capacity index (RACI) was calculated to compare results obtained by different tests. The extracts were tested to evaluate their possible involvement in redox homeostasis, using the human hepatoma (HepG2) cell line used as model. The extracts exhibited concentration/solvent dependent radical scavenging activity, as well as dysregulation of some genes involved in redox pathways by promoting Nrf2, SOD-2, GPX1, ABCC6 and ABCG2 expression. NMR metabolomics analysis suggests that HepG2 cells treated with Muscari comosum extracts experience changes in some metabolites involved in various metabolic pathways.

Isolation of secondary metabolites from the Iranian medicinal plant Eremurus persicus.

Eremurus persicus (Jaub. & Spach) Boiss. belonging to Xanthorrhoeaceae family is an endemic medicinal plant widely distributed in Iran. Its leaves have been traditionally used as a food and also as medicinal plant. Regarding the widespread application of E. persicus in Iranian folk medicine, and the insignificant investigation of its components, this study aimed at the isolation and identification of major secondary metabolites of this plant. By applying various chromatographic techniques, corchoionoside A (1), 4-amino-4-carboxychroman-2-one (2), isoorientin (3), ziganein 5-methyl ether (4), auraptene (5), and imperatorin (6) were isolated from the EtOAc and CHCl3 fractions of the crude extract. Except isoorientin (3), all the identified phytoconstituents were reported for the first time from Eremurus genus.

Chemical Profiling of Chlorophytum comosum (Thunb.) Jaques by GC-MS/LC-ESIMS and its Antiproliferative Effects on Human Carcinoma Cell Lines.

BACKGROUND: Chlorophytum comosum, popularly known as Spider Ivy, is used as a medicinal plant in traditional Chinese medicine, however, its detailed chemical composition and biological activity are yet unexplored. OBJECTIVE: To carry out the phytochemical investigation on different parts of Chlorophytum comosum using GCMS/ LC-ESI-MS and evaluation of its antioxidant, hemolytic and antiproliferative potential on breast cancer (MCF-7), lung cancer (A549, H1299) and normal lung (L-132) cell lines. METHODS: Chemical constituents from aqueous roots and leaves extracts were identified using LC-ESI-MS/GCMS. The identified compounds were annotated based on the match of mass spectra with the literature using NIST 14 and METLIN databases. Antioxidant activity was studied using DPPH, FRAP and TPC assays. The antiproliferative effects of ethanolic roots and leaves extracts of Chlorophytum comosum were measured by MTT assay on breast cancer (MCF-7), lung cancer (A549 & H1299) and normal lung (L-132) cell lines. The toxicity studies of the extracts were carried out using Hemolysis assay. RESULTS: GC-MS analysis identified 34 metabolites in roots and 17 from leaves, while 17 compounds from roots and 7 from leaves were detected by LC-ESI-MS. Significant antiproliferative effects were observed on the A549 and MCF-7 cancer cell lines with IC50 values ranging from 56.86 µg/ml to 68.68 µg/ml while no marked response was observed against normal cell line L-132. CONCLUSION: Our study represents the first report on the detailed chemical composition and antiproliferative potential of Chlorophytum comosum against lung and breast cancer cell lines.

Antihyperglycaemic activity of ethylacetate extract of Chlorophytum alismifolium in type 2 diabetes: The involvement of peroxisome proliferator-activated receptor-γ and dipeptidyl peptidase-4.

OBJECTIVE: This research is to investigate the antihyperglycaemic activity and the underlying mechanisms of action of the ethylacetate extract of Chlorophytum alismifolium (EACA) tubers in a type 2 diabetes model. METHODS: The tubers were processed and sequentially extracted in hexane followed by ethylacetate, using a Soxhlet apparatus, and subjected to gas chromatography-mass spectrometry (GC-MS). The acute toxicity of EACA was investigated in albino Wistar rats. An antihyperglycaemic study was carried out using high-fat diet (pelletized diet and margarine in the ratio of 10:1 and 20% fructose solution) and streptozotocin-induced hyperglycaemic Wistar rats. The effects of the extract (150, 300 and 600 mg/kg) on blood glucose level, insulin, peroxisome proliferator-activated receptor-γ (PPAR-γ) and dipeptidyl peptidase-4 (DPP-4) were evaluated using enzyme-linked immunosorbent assay. RESULTS: The oral median lethal dose in Wistar rats was estimated to be > 5000 mg/kg. Treatment with EACA at all doses significantly reduced the fasting blood glucose levels, compared to the hyperglycaemic control, and over time. Administration of EACA increased the serum insulin and PPAR-γ levels while decreasing DPP-4 levels. GC-MS analysis revealed the presence of 13 compounds, with isothiazole and isoxazolidine covering total area of 24.6% and 22.69%, respectively. CONCLUSION: The findings from this study showed that EACA has important compounds with beneficial effect in type 2 diabetes and acts by increasing insulin secretion and PPAR-γ level and decreasing DPP-4 activity.

Three new steroidal saponins from Aspidistra letreae plants and their cytotoxic activities.

Three new steroidal saponins, aspiletreins A-C (1-3), together with 2H-chromen-2-one (4), and α-tocopherol (5), were isolated from whole Aspidistra letreae plants collected in Vietnam. Their structures were elucidated by a combination of spectroscopic analyses, including 1D- and 2D-NMR, IR, and HRESIMS, and by comparison with the reported data in the literature. Compounds 1-3 exhibited moderate cytotoxicities against the LU-1, HeLa, MDA-MB-231, HepG2, and MKN-7 human cancer cell lines, with IC50 values ranging from 7.69 ± 0.40 to 20.46 ± 3.11 µM.

Bufadienolides and anti-angiogenic homoisoflavonoids from Rhodocodon cryptopodus, Rhodocodon rotundus and Rhodocodon cyathiformis.

BACKGROUND: Homoisoflavonoids have been shown to have potent anti-proliferative activities in endothelial cells over other cell types and have demonstrated a strong antiangiogenic potential in vitro and in vivo in animal models of ocular neovascularization. Three species of Rhodocodon (Scilloideaea subfamily of the Asparagaceae family), endemic to Madagascar, R. cryptopodus, R. rotundus and R. cyathiformis, were investigated. PURPOSE: To isolate and test homoisoflavonoids for their antiangiogenic activity against human retinal microvascular endothelial cells (HRECs), as well as specificity against other ocular cell lines. METHODS: Plant material was extracted at room temperature with EtOH. Compounds were isolated using flash column chromatography and were identified using NMR and CD spectroscopy and HRESIMS. Compounds were tested for antiproliferative effects on primary human microvascular retinal endothelial cells (HRECs), ARPE19 retinal pigment epithelial cells, 92-1 uveal melanoma cells, and Y79 retinoblastoma cells. HRECs exposed to compounds were also tested for migration and tube formation ability. RESULTS: Two homoisoflavonoids, 3S-5,7-dihydroxy-(3'-hydroxy-4'-methoxybenzyl)-4-chromanone (1) and 3S-5,7-dihydroxy-(4'-hydroxy-3'-methoxybenzyl)-4-chromanone (2), were isolated along with four bufadienolides. Compound 1 was found to be non-specifically antiproliferative, with GI50 values ranging from 0.21-0.85 µM across the four cell types, while compound 2 showed at least 100-fold specificity for HRECs over the other tested cell lines. Compound 1, with a 3S configuration, was 700 times more potent that the corresponding 3R enantiomer recently isolated from a Massonia species. CONCLUSION: Select homoisoflavonoids have promise as antiangiogenic agents that are not generally cytotoxic.

Antifungal, anti-inflamatory and neuritogenic activity of newly-isolated compounds from Disporopsis aspersa.

A new ester (1) and a terpenoid (2) were isolated from the dried whole plant of Disporopsis aspersa (HUA) ENGL. ex DIELS for the first time and their structures were elucidated, as well as their biological activities are described. The two compounds all showed good antifungal activities, especially furanone (2) exhibited better antifungal activity against Pseudoperonospora cubensis and Phytophthora infestans with EC50 value of 22.82, 18.90 µg/mL, respectively. Compound 1 exhibited a significant promotion on the neurite outgrowth in NGF-induced PC-12 cells, and moderate inhibition on the NO production induced by lipopolysaccharide (LPS) in BV-2 microglial cells.

Regulation of circadian rhythms by NEAT1 mediated TMAO-induced endothelial proliferation: A protective role of asparagus extract.

Trimethylamine N-oxide (TMAO) promotes atherosclerosis in association with the functions of endothelial cells. Clock and Bmal1, as two main components of molecular circadian clock, play important regulatory roles during progression of atherogenesis. However, whether Clock and Bmal1 are involved in the regulation of endothelial proliferation disturbed by TMAO are unclear. We observed that cell proliferation of human umbilical vein endothelial cells (HUVECs) was inhibited after exposed to TMAO for 24 h. Besides, TMAO caused increased expression of lncRNA-NEAT1, Clock and Bmal1, and inhibited MAPK pathways. While MAPK pathways were blocked, the expression of Clock and Bmal1 was elevated. NEAT1 showed a circadian rhythmic expression in HUVECs, and its overexpression reduced cell proliferation. Knockdown or overexpression of NEAT1 might decrease or increase the expression of Clock and Bmal1 respectively, while raised or suppressed the expression of MAPK pathways correspondingly. Asparagus extract (AE) was found to improve the TMAO-reduced HUVECs proliferation. Moreover, it ameliorated the disorders of NEAT1, Clock, Bmal1, and MAPK signaling pathways induced by TMAO. Therefore, our findings indicated that NEAT1 regulating Clock-Bmal1 via MAPK pathways was involved in TMAO-repressed HUVECs proliferation, and AE improved endothelial proliferation by TMAO, proposing a novel mechanism for cardiovascular disease prevention.

The Antiangiogenic Activity of Naturally Occurring and Synthetic Homoisoflavonoids from the Hyacinthaceae ( sensu APGII).

Excessive blood vessel formation in the eye is implicated in wet age-related macular degeneration, proliferative diabetic retinopathy, neovascular glaucoma, and retinopathy of prematurity, which are major causes of blindness. Small molecule antiangiogenic drugs are strongly needed to supplement existing biologics. Homoisoflavonoids have been previously shown to have potent antiproliferative activities in endothelial cells over other cell types. Moreover, they demonstrated a strong antiangiogenic potential in vitro and in vivo in animal models of ocular neovascularization. Here, we tested the antiangiogenic activity of a group of naturally occurring homoisoflavonoids isolated from the family Hyacinthaceae and related synthetic compounds, chosen for synthesis based on structure-activity relationship observations. Several compounds showed interesting antiproliferative and antiangiogenic activities in vitro on retinal microvascular endothelial cells, a disease-relevant cell type, with the synthetic chromane, 46, showing the best activity (GI50 of 2.3 × 10-4 µM).

Steroids from herbs of Reineckia carnea and their anticomplement activities.

A new polyhydroxylated pregnane, named lß,2ß,3ß,4ß,5ß,6ß-hexolhydroxy-pregn-16-en-20-one (1), along with nine known (2-10) steroidal saponins were isolated from the whole plant of Reineckia carnea. Structure elucidations of all compounds were established by interpretation of their NMR spectral data, HR-ESI-MS and comparing with literatures. In addition, these compounds were evaluated with anticomplement activity. The result showed that compound 1 exhibited anticomplement effects with the CH50 values of 0.043 mg/mL, but saponins (2-10) showed no inhibition. Interestingly, hydrolysis of steroidal saponins (2-10) resulted in its aglycones (2a-10a) correspondingly which showed anticomplement activity with the CH50 values of 0.049-0.156 mg/mL.

Comparison of biofunctional activity of Asparagus cochinchinensis (Lour.) Merr. Extract before and after fermentation with Aspergillus oryzae.

Asparagus cochinchinensis root (ACR) is used in traditional Chinese medicine. In this study, ACR was first extracted with 25% ethyl acetate (EA) and then fermented by Aspergillus oryzae to enhance its antioxidant activity and evaluate its potential antityrosinase activity. The physiological activity and cytotoxicity of A. oryzae-fermented ACR extract, along with its antityrosinase activity and effects on melanogenic factor levels in human epidermal melanocytes (HEMs), were analyzed and compared with those of the unfermented extract. The results showed that the physiological activity of the fermented extract in vitro or in cells was significantly higher than that of the unfermented extract. The IC50 values for 2,2-diphenyl-1-picrylhydrazine radical scavenging activity, reducing power, and antityrosinase activity in vitro for the fermented extract were 250.6 ± 32.5, 25.7 ± 3.5, and 50.6 ± 3.1 mg/L, respectively. The fermented extract favored cellular antityrosinase activity with low melanin production in human melanoma cells compared with the unfermented extract. The inhibitory mechanism of melanin synthesis by unfermented extract was independent of the tested melanogenesis-related proteins. However, the inhibitory mechanism of the fermented extract was possibly caused by synergistic inhibition of these proteins. Thus, A. oryzae-fermented ACR extract may be used for developing new health food or cosmetic ingredients.

The Potential Chondrogenic Effect of Eucomis autumnalis Aqueous Extracts on Porcine Adipose-Derived Mesenchymal Stem Cells.

IMPACT STATEMENT: Eucomis autumnalis is one plant that is used by various traditional healers to alleviate the signs and symptoms associated with osteoarthritis. Although the exact mechanisms remain unknown, we hypothesized that this plant can induce chondrogenesis. In this work, we explored the potential for an aqueous crude extract from E. autumnalis to induce chondrogenesis in porcine adipose-derived mesenchymal stem cells (MSCs). The results reported in our article indicate that the aqueous crude extract from E. autumnalis was able to indeed induce chondrogenesis. Our research is relevant to communities that rely on plant-based remedies for their well-being.

Metabolism, pharmacokinetics, and hepatic disposition of xanthones and saponins on Zhimu treatments for exploratively interpreting the discrepancy between the herbal safety and timosaponin A3-induced hepatotoxicity.

Timosaponin A3, a saponin in Zhimu, elicited hepatotoxicity via oxidative stress. However, the clinical medication of Zhimu has been historically regarded as safe, probably associated with the antioxidants it contains. However, the related information on the in vivo levels of timosaponin A3 and antioxidants remained unclear on Zhimu treatments. Therefore, a combination of the in vitro metabolism, including microbiota-mediated and liver-mediated metabolism, and in vivo pharmacokinetics and hepatic disposition, was conducted for three xanthones (neomangiferin, mangiferin, and norathyriol) and three saponins (timosaponin B2, timosaponin B3, and timosaponin A3) on Zhimu treatments. Consequently, following oral administration of Zhimu decoction to rats, those saponins and xanthones were all observed in the plasma with severe liver first-pass effect, where mangiferin was of the maximum exposure. Despite the ignorable content in the herb, timosaponin A3 elicited sizable hepatic exposure as the microbiota-mediated metabolite of saponins in Zhimu. The similar phenomenon also occurred to norathyriol, the microbiota-mediated metabolite of xanthones. However, the major prototypes in Zhimu were of limited hepatic exposure. We deduced the hepatic collection of norathyriol, maximum circulating levels of mangiferin, and timosaponin B2 and mangiferin interaction may directly or indirectly contribute to the whole anti-oxidation of Zhimu, and then resisted the timosaponin A3-induced hepatotoxicity. Thus, our study exploratively interpreted the discrepancy between herbal safety and timosaponin A3-induced hepatotoxicity. However, given the considerable levels and slow eliminated rate of timosaponin A3 in the liver, more attention should be paid to the safety on the continuous clinical medication of Zhimu in the future.