GC-MS analysis of curculigo orchiodes and medicinal herbs with cytotoxic, hepatoprotective attributes of ethanolic extract from Indian origin.

OBJECTIVES: Liver illnesses are a major public health issue all over the world. Medicinal plants constituents a viable alternative for the development of phytopharmaceuticals with hepatoprotective activity in order to solve some of these health-related problems. The present study is focused on the phytochemical and biological investigation on Indian traditional medicinal plant extracts, for their cytotoxic and hepatoprotective activity. The isolated compounds showed the presence of phenolic constituents which lead to cytotoxicity and hepatoprotective activity of medicinal plant. Cancer causes about 13% of all human deaths in 2007 (7.6 million) (American Cancer Society and WHO December 2006-07). The American Cancer Society estimates that 12,990 new cases of cervical cancer will be diagnosed in the United States year 2016. Cancer-related deaths are expected to increase, with an estimated 11.4 million deaths in 2030. METHODS: The ethanolic extracts of Centella asiatica, Myristica fragrans, Trichosanthes palmata, Woodfordia fruticosa, Curculigo orchioides were evaluated against HEP-G2 cell lines for hepatoprotective activity and Curculigo orchioides was further promoted for the isolation of secondary metabolites based on inhibitory concentration. RESULTS: The ethanolic extracts of C. asiatica, M. fragrans, T. palmata, W. fruticosa, Curculigo orchioides shown significant cytotoxic activity (IC50≤100 µg/mL). The plant extracts also shown significant hepatoprotective activity in a dose dependent manner when tested against HEP-G2 cell lines and cytotoxicity studies against HeLa and HEP-G2 cells. CONCLUSIONS: The extract of Curculigo orchiodes rhizome showed significant cytotoxicity results. Hence the Curculigo orchiodes rhizome was selected for further phytochemical studies to isolate active compounds and their Characterization by GCMS.

Phytochemistry and Pharmacological Activity of Plants of Genus Curculigo: An Updated Review Since 2013.

The genus Curculigo, as a folk herbal medicine, has been used for many years in China, treating impotence, limb limpness, and arthritis of the lumbar and knee joints. The last systematic review of the genus Curculigo was written in 2013, scientifically categorizing the phytochemistry and biological activities. Hitherto, the original compounds and their pharmacological activities were presented as the development of this genus, but there is not an updated review. To conclude the progression of the genus Curculigo, we collected the new literature published from 2013 to 2021 in PubMed, Web of Science, Google Scholar databases, and the Chinese National Knowledge Infrastructure. The novel chlorophenolic glucosides, curculigine, phenolic glycosides, orcinosides and polysaccharides were isolated from Curculigo. The new analyzing methods were established to control the quality of Curculigo as a herbal medicine. In addition, the pharmacological effects of Curculigo focused on anti-diabetes, antibacterial, anti-inflammatory, osteoporosis, antioxidation, etc. The antitumor and neuroprotective activities were newly explored in recent years. The application of herbal medicine was gradually developed in scientific methods. The medicinal value of the genus Curculigo needs to further investigate its pharmacological mechanisms. This new review offers more insights into the exploitation of the pharmacological value of the genus Curculigo.

Inhibitory evaluation of Curculigo latifolia on α-glucosidase, DPP (IV) and in vitro studies in antidiabetic with molecular docking relevance to type 2 diabetes mellitus.

The inhibition of α-glucosidase and DPP enzymes capable of effectively reducing blood glucose level in the management of type 2 diabetes. The purpose of the present study is to evaluate the inhibitory potential of α-glucosidase and DPP (IV) activity including with the 2-NBDG uptake assay and insulin secretion activities through in vitro studies. The selected of active compounds obtained from the screening of compounds by LC-MS were docked with the targeted enzyme that involved in the mechanism of T2DM. From the results, root extracts displayed a better promising outcome in α-glucosidase (IC50 2.72 ± 0.32) as compared with the fruit extracts (IC50 3.87 ± 0.32). Besides, root extracts also displayed a better activity in the inhibition of DPP (IV), enhance insulin secretion and glucose uptake activity. Molecular docking results revealing that phlorizin binds strongly with α-glucosidase, DPP (IV) and Insulin receptor (IR) enzymes with achieving the lowest binding energy value. The present work suggests several of the compounds have the potential that contribute towards inhibiting α-glucosidase and DPP (IV) and thus effective in lowering post-prandial hyperglycaemia.

African crocus (Curculigo pilosa) and wonderful kola (Buchholzia coriacea) seeds modulate critical enzymes relevant to erectile dysfunction and oxidative stress.

Background The seeds of African crocus (AC) (Curculigo pilosa) and wonderful kola (WK) (Buchholzia coriacea) are commonly used in folklore medicine in managing erectile dysfunction (ED) without the full understanding of the possible mechanism of actions. This study investigated and compared the effects of aqueous extracts from the seeds of AC and WK on arginase and acetylcholinesterase (AChE) activities and some pro-oxidant [FeSO4 and sodium nitroprusside (SNP)]-induced lipid peroxidation in rat penile homogenate in vitro. Method Aqueous extracts of AC and WK were prepared, and their effects on arginase and AChE activities as well as FeSO4- and SNP-induced lipid peroxidation in rat penile homogenate were assessed. Furthermore, phenolic constituents of the extract were determined using high-performance liquid chromatography coupled with diode-array detector (HPLC-DAD). Results Both extracts exhibited concentration-dependent inhibition on arginase (AC, IC50=0.05 mg/mL; WK, IC50=0.22 mg/mL) and AChE (AC, IC50=0.68 mg/mL; WK, IC50=0.28 mg/mL) activities. The extracts also inhibited FeSO4- and SNP-induced lipid peroxidation in rat penile homogenate. HPLC-DAD analysis revealed the presence of phenolic acids (gallic, caffeic, ellagic and coumaric acids) and flavonoids (catechin, quercetin and apigenin) in AC and WK. AC had higher arginase inhibitory and antioxidative activities but lower AChE inhibitory properties when compared with WK. Conclusions These effects could explain the possible mechanistic actions of the seeds in the management/treatment of ED and could be as a result of individual and/or synergistic effect of the constituent phenolic compounds of the seeds.

Antioxidative and anti-proliferative potential of Curculigo orchioides Gaertn in oxidative stress induced cytotoxicity: In vitro, ex vivo and in silico studies.

Plant phytoconstituents have been a valuable source of clinically important anticancer agents. Antioxidant and anticancerous activity of plant Curculigo orchioides Gaertn were explored In vitro antioxidant activity, antioxidant enzyme activity of oxidatively stressed tissue, and cell culture studies on human cancer cell lines HepG2, HeLa and MCF-7 were carried out. Active plant fractions were subjected to GC-MS analysis and compounds selected on the basis of their abundance were screened in silico with the help of Auto Dock 4.2 tools with pre-selected antioxidant enzymes. Curculigo orchioides Gaertn plant fractions exhibited significant antioxidant activities by virtue of scavenging of free radicals having IC50 value of ethylacetate fraction (EA) for DPPH radical scavenging assay to be 52.93 ±â€¯0.66 µg/ml. Further, antioxidant enzyme defense of mammalian tissue when treated with plant fractions revealed that enzyme concentrations were refurbished which were increased during oxidative stress. MTT assay on cell lines HepG2, HeLa and MCF-7 presented IC50 values of ethylacetate (EA) fraction as 171.23 ±â€¯2.1 µg/ml, 144.80 ±â€¯1.08 µg/ml and 153.51 µg/ml and aqueous ethylacetate (AEA) fraction as 133.44 ±â€¯1.1 µg/ml, 136.50 ±â€¯0.8 µg/ml and 145.09 µg/ml respectively. Further EA and AEA plant fractions down regulated the levels of antiapoptotic Bcl-2 expression and upregulated the expression of apoptotic proteins caspase-3 and caspase-8 through an intrinsic ROS-mediated mitochondrial dysfunction pathway. KEY MESSAGE: Key findings explained that fractions of Curculigo orchioides Gaertn inhibited oxidative stress by increasing the antioxidant enzyme content and have anticancerous potential on cancer cell lines HepG2, HeLa and MCF-7.

A Network Pharmacology Approach to Determine the Active Components and Potential Targets of Curculigo Orchioides in the Treatment of Osteoporosis.

BACKGROUND Osteoporosis is a complex bone disorder with a genetic predisposition, and is a cause of health problems worldwide. In China, Curculigo orchioides (CO) has been widely used as a herbal medicine in the prevention and treatment of osteoporosis. However, research on the mechanism of action of CO is still lacking. The aim of this study was to identify the absorbable components, potential targets, and associated treatment pathways of CO using a network pharmacology approach. MATERIAL AND METHODS We explored the chemical components of CO and used the five main principles of drug absorption to identify absorbable components. Targets for the therapeutic actions of CO were obtained from the PharmMapper server database. Pathway enrichment analysis was performed using the Comparative Toxicogenomics Database (CTD). Cytoscape was used to visualize the multiple components-multiple target-multiple pathways-multiple disease network for CO. RESULTS We identified 77 chemical components of CO, of which 32 components could be absorbed in the blood. These potential active components of CO regulated 83 targets and affected 58 pathways. Data analysis showed that the genes for estrogen receptor alpha (ESR1) and beta (ESR2), and the gene for 11 beta-hydroxysteroid dehydrogenase type 1, or cortisone reductase (HSD11B1) were the main targets of CO. Endocrine regulatory factors and factors regulating calcium reabsorption, steroid hormone biosynthesis, and metabolic pathways were related to these main targets and to ten corresponding compounds. CONCLUSIONS The network pharmacology approach used in our study has attempted to explain the mechanisms for the effects of CO in the prevention and treatment of osteoporosis, and provides an alternative approach to the investigation of the effects of this complex compound.

Total glucosides of Curculigo rhizome to perimenopausal period mice model.

To investigate the effects of total glucosides of Curculigo rhizome (TGC) to perimenopausal period (PMS) mice model. After removed the bilateral ovaries induced the PMS mice model, high, medium and low doses of TGC group were partly given TGC solution 400,200,100mg•kg-1, administered once a day, continuously 21 days. Compared with the model group (MG) mices, each dose of TGC group could significantly improve the activities of mice, increase thymus, uterus, spleen index(TI, UI, SI), the levels of testosterone(T), estradiol (E2), reduce the level of luteinizing hormone (LH), the high dose of TGC group(HD-C) group has the best effects. It prompted that TGC has the effect in treatment of PMS mice model, the HD-C group of TGC has the best effects.

Curculigoside augments cell-mediated immune responses in metastatic tumor-bearing animals.

A positive modulation of immune system is necessary for preparing the body to fight against malignant tumor cells. In the present study, the stimulatory effect of Curculigoside on cell-mediated immune response against the metastasis of B16F10 melanoma cells was analyzed in C57BL/6 mice. Curculigoside is a phenolic glucoside present in the plant Curculigo orchioides Gaertn. (Family - Amaryllidaceae). Administration of Curculigoside enhanced the natural killer (NK) cell activity, antibody-dependent cell-mediated cytotoxicity and complement-mediated cytotoxicity in metastatic tumor-bearing animals, when compared to the untreated control animals. The compound was also found to be effective in reducing the levels of proinflammatory cytokines such as TNF-α, IL-1ß, IL-6 and GM-CSF during metastasis. Besides these, levels of TH1 cytokines, such as IL-2 and IFN-γ, were significantly enhanced (p < 0.001) by Curculigoside administration and thereby reduces the metastatic lung colony formation along with an increased lifespan of the experimental animals. These studies provide an evidence for the stimulation of cell-mediated immune responses by Curculigoside against B16F10-induced metastatic tumor progression in experimental animals.

Curculigo orchioides Gaertn Effectively Ameliorates the Uro- and Nephrotoxicities Induced by Cyclophosphamide Administration in Experimental Animals.

Background Curculigo orchioides Gaertn is an ancient medicinal plant (Family: Amaryllidaceae), well known for its immunomodulatory and rejuvenating effects. Cyclophosphamide (CPA) is an alkylating agent widely used for treating a variety of human malignancies, but associated with different toxicities too. Our previous reports regarding the hemoprotective and hepatoprotective effects of the plant against CPA toxicities provide the background for the present study, which is designed to analyze the ameliorative effect of the methanolic extract of C orchioides on the urotoxicity and nephrotoxicity induced by CPA. Methods CPA was administered to male Swiss albino mice at a single dose of 1.5 mmol/kg body weight to induce urotoxicity after 5 days of prophylactic treatment with C orchioides extract (20 mg/kg body weight). Mesna (2-mercaptoethanesulfonate) was used as a control drug. Serum, tissue, and urine levels of kidney function markers and antioxidant levels were checked along with the serum cytokine levels. Results The plant extract was found to be effective in ameliorating the urotoxic and nephrotoxic side effects of CPA. Upregulation of serum interferon-γ and interleukin-2 levels were observed with C orchioides treatment, which was decreased by CPA administration. Besides these, serum tumor necrosis factor-α level was also downregulated by C orchioides treatment. Conclusion Curculigo orchioides was found to be effective against the CPA-induced bladder and renal toxicities by its antioxidant capability and also by regulating the pro-inflammatory cytokine levels.

Phytochemical profile and bioactivity of traditional ayurvedic decoctions and hydro-alcoholic macerations of Boerhaavia diffusa L. and Curculigo orchioides Gaertn.

Decoctions (DECs) and hydro-alcoholic extracts (HEs) prepared from roots of Boerhaavia diffusa L. (Nyctaginaceae) and Curculigo orchioides Gaertn. (Hypoxidaceae) were phytochemically characterised by HPLC-DAD and profiled for their antioxidant, antigenotoxic and cytotoxic activities. B. diffusa DEC was rich in ferulic acid and vanillin, while the HE also contained boeravinone B and eupalitin. Both C. orchioides HE and DEC displayed the main occurrence of orcinol-ß-d-glucoside and curculigoside A. Antioxidant activity was assayed through spectrophotometric DPPH, ABTS and ß-carotene bleaching test, and using (HP)TLC bioautographic strategies. For both crude drugs, HE was the best performing preparation. Properly modified SOS-Chromotest evidenced a 10% inhibition by phytocomplexes against 4-nitroquinoline-N-oxide, and a higher bioactivity for vanillin (36.60 ± 1.68%) and ferulic acid (35.09 ± 1.53%). C. orchioides HE was the preparation which showed higher cytotoxicity against drug-sensitive human T-lymphoblastoid cell line (CCRF-CEM) and multidrug-resistant leukaemia cell line (CEM/ADR5000), and eupalitin was the only pure compound to exhibit an IC50 value.

Enhancement of cancer chemotherapeutic efficacy of cyclophosphamide by Curculigo orchioides Gaertn and its ameliorative effects on cyclophosphamide-induced oxidative stress.

Cyclophosphamide (CTX) is a synthetic antineoplastic drug with severe and life-threatening side effects. Studies in search of protective agents, preferably natural products, that can alleviate these side effects are valuable because they can contribute to improve current chemotherapeutic treatment strategies. Curculigo orchioides Gaertn (family Hypoxidaceae) is well known for its medicinal use in the Indian Ayurvedic system of medicine, and various studies have been reported that proved its immunomodulatory and anti-inflammatory properties. In this study, the tumor reduction capacity of CTX in combination with C orchioides methanolic extract was studied using Dalton's lymphoma ascites-induced solid tumor models. Effect of C orchioides on the reversal of the damage induced by CTX administration (intraperitoneally) was also determined in this study. For this, solid tumor volume, serum cytokine levels, hematolological parameters, intestinal histopathology, and serum and tissue biochemical parameters (Glutathione [GSH], alkaline phosphatase [ALP], glutamate pyruvate transaminase [GPT], lipid peroxidation [LPO]) were analyzed. Immune suppression and increased serum proinflammatory cytokine levels caused by CTX administration (25 mg/kg body weight) were reversed by C orchioides (20 mg/kg body weight). The alcoholic extract enhanced the tumor reduction capacity of CTX and reduced GPT and ALP levels in liver and serum, which were elevated by CTX administration. The LPO level was also lower in the CTX-administered animals when treated with the C orchioides extract. In conclusion, the plant extract when administered in combination with CTX, can result in enhanced anticancer properties; it also ameliorates the toxic side effects of CTX.

Curculigoside promotes osteogenic differentiation of bone marrow stromal cells from ovariectomized rats.

OBJECTIVES: Curculigoside, a natural compound isolated from the medicinal plant Curculigo orchioides has been reported to prevent bone loss in ovariectomized rats. However, the underlying molecular mechanisms are largely unknown. This study investigated the effects of curculigoside on proliferation and osteogenic differentiation of bone marrow stromal cells (BMSCs). METHODS: The toxicity, proliferation and osteogenic differentiation of BMSCs cultured with various concentrations (0 as control, 10, 100 and 500 µm) of curculigoside were measured by viability assay, MTT analysis, alkaline phosphatase (ALP) activity assay, alizarin red staining and mineralization assay, real-time PCR analysis on osteogenic genes including ALP, type I collagen (Col I), osteocalcin (OCN) and osteoprotegerin (OPG), runt-related transcription factor 2 (Runx2), as well as OPG enzyme-linked immunosorbent assay. KEY FINDINGS: No significant cytotoxicity was observed for BMSCs after supplementation with curculigoside. The proliferation of BMSCs was enhanced after administration of curculigoside, especially 100 µm curculigoside. Moreover, the osteogenic gene expression was significantly enhanced with 100 µm curculigoside treatment. Importantly, curculigoside significantly increased OPG secretion. CONCLUSIONS: The data indicate that curculigoside could promote BMSC proliferation and induce osteogenic differentiation of BMSCs. The most profound response was observed with 100 µm curculigoside. These findings may be valuable for understanding the mechanism of the effect of curculigoside on bone, especially in relation to osteoporosis.

Curculigo orchioides protects cisplatin-induced cell damage.

Cisplatin is commonly used as a chemotherapeutic agent against many human cancers. However, it generates reactive oxygen species (ROS) and has serious dose-limiting side effects, including ototoxicity. The roots of Curculigo orchioides (C. orchioides) have been used to treat auditory diseases such as tinnitus and hearing loss in Chinese traditional medicine. In the present study, we investigated the protective effects of an ethanol extract obtained from C. orchioides rhizome (COR) on cisplatin-induced cell damage in auditory cells (HEI-OC1). COR (2.5-25 µg/ml) inhibited cisplatin-induced HEI-OC1 cell damage in a dose-dependent manner. To investigate the protective mechanism of COR on cisplatin cytotoxicity in HEI-OC1 cells, we measured the effects of COR on ROS generation and lipid peroxidation in cisplatin-treated cells as well as its scavenging activities against superoxide radicals, hydroxyl radicals, hydrogen peroxide, and DPPH radicals. COR (1-25 µg/ml) had scavenging activities against superoxide radicals, hydroxyl radicals, hydrogen peroxide, and DPPH radicals, as well as reduced lipid peroxidation. In in vivo experiments, COR was shown to reduce cochlear and peripheral auditory function impairments through cisplatin-induced auditory damage in mice. These results indicate that COR protects from cisplatin-induced auditory damage by inhibiting lipid peroxidation and scavenging activities against free radicals.

Medicinal plants of genus Curculigo: traditional uses and a phytochemical and ethnopharmacological review.

ETHNOPHARMACOLOGICAL RELEVANCE: In the genus Curculigo, Curculigo orchioides Gaertn, Curculigo capitulata (Lour) O. Ktze and Curculigo pilosa (Schumach. & Thonn.) Engl are often used in traditional medicine. Curculigo orchioides is used for the treatment of impotence, limb limpness, arthritis of the lumbar and knee joints, and watery diarrhea in traditional Chinese medicine, and also used as a potent immunomodulator and aphrodisiac in the Ayurvedic medical system. Curculigo capitulata is used for the treatment of consumptive cough, kidney asthenia, impotence and spermatorrhea, hemorrhoids, asthma, jaundice, diarrhea, colic and gonorrhea in traditional Chinese and India medicine, and to treat urinary tract infection, acute renal pelvis and nephritis, nephritis-edema, cystitis, nephrolithiasis, hypertension and rheumatic arthritis in traditional Dai medicine. Curculigo pilosa are applied to treat gastrointestinal and heart diseases in Africa. AIM OF THE REVIEW: This review aims to exhibit up-to-date and comprehensive information about traditional uses, phytochemistry, pharmacology and toxicology of medicinal plants in the genus Curculigo, and has an insight into the opportunities for the future research and development of Curculigo plant. METHODS: A bibliographic investigation was performed by analyzing the information available on Curculigo plant from worldwide accepted scientific databases (Pubmed, Scopus and Web of Science, SciFinder, Google Scholar, Yahoo). Furthermore, information also was obtained from some local and foreign books on ethnobotany and ethnomedicines. RESULTS: Curculigo orchioides, Curculigo capitulata and Curculigo pilosa have been used as traditional medicine to treat kinds of diseases such as impotence, limb limpness, gastrointestinal and heart diseases, etc. Phytochemical investigation of eight species of the genus Curculigo has resulted in identification of more than 110 compounds. The content of curculigoside is used as an indicator to evaluate the quality of rhizome of Curculigo orchioides. The medicinal plants have showed a wide spectrum pharmacological activities, including adaptive, immunostimulatory, taste-modifying and sweet-tasting, antioxidant, mast cell stabilization, antihistaminic and antiasthmatic, hepatoprotective and neuroprotective activity. Toxicological test indicated that Curculigo orchioides at the dose of 120 g/kg after administrating rats for 180 days may cause injury of liver and kidney. CONCLUSION: The medicinal plants of genus Curculigo have emerged as a good source of the traditional medicines. Some uses of these plants in the traditional medicines have been validated by pharmacological investigation. However, the mechanism of their actions should be further elucidated; the particular constituent responsible for toxicity should be isolated and identified, and the target tissue and mechanism of toxic ingredients also deserve to be further investigated; more reference substances should be prepared, and sophisticated analytical technologies should be developed to comprehensively assess the quality of Curculigo herbs. These investigations will be helpful for further utilization of the plants of genus Curculigo.

Effect of Curculigo orchioides on reflux esophagitis by suppressing proinflammatory cytokines.

This study was performed to investigate effects of Curculigo orchioides rhizome (curculiginis rhizome) on acute reflux esophigitis (RE) in rats that are induced by pylorus and forestomach ligation operation. Proinflammatory cytokine, as well as tumor necrosis factor (TNF)-α, interleukin (IL)-1ß and IL-6 were all assayed and the expression of TNF-α and COX2 analyzed by RT-PCR. The esophagic tissue damage of reflux esophagitis rat was increased compared to that of normal intact group. However, the esophagic damage percentage from the extract of curculiginis rhizoma (ECR) 600 mg/kg and ECR 300 mg/kg were significantly lower than that of the RE control group. Administration of α-tocopherol (30 mg/kg) and ECR (600 mg/kg, 300 mg/kg, and 150 mg/kg) had a significant effect on the gastric acid pH in rats with induced reflux esophagitis (p < 0.05). The treatment with ECR significantly reduced the production of cytokines TNF-α, IL-1ß and IL-6 levels compared to the model group (p < 0.05). The expression of TNF-α and COX2 in the intact esophageal mucosa was low while those of the RE control group were significantly higher due to an inflammatory reaction in the esophagus. Compare to the model group, treatment with α-tocopherol or ECR significantly inhibited the expression levels of COX2 and TNF-α in a dose-dependent manner. These results suggest that anti-inflammatory and protective effects of ECR could attenuate the severity of reflux esophagitis and prevent esophageal mucosal damage.

Curculigoside isolated from Curculigo orchioides prevents hydrogen peroxide-induced dysfunction and oxidative damage in calvarial osteoblasts.

Reactive oxygen species (ROS), including H(2)O(2), play a critical role in the pathophysiology of osteoporosis. Therefore, agents or antioxidants that can inhibit ROS production have a high clinical value in the treatment of osteoporosis. Curculigoside (CUR), one of the main bioactive phenolic compounds isolated from the rhizome of Curculigo orchioides Gaertn., is reported to have potent antioxidant and anti-osteoporotic properties. However, there is no direct evidence to link the antioxidant capacity of CUR with the observed anti-osteoporotic effect, and relevant molecular mechanisms remain unclear. Therefore, we investigated the protective effects of CUR against oxidative stress in calvarial osteoblasts and discussed the related mechanisms. It was found that osteoblast viability decreased significantly after 48-h exposure to 400 µM of H(2)O(2), compared with vehicle-treated cells, and the cytotoxic effect of H(2)O(2) was reversed significantly when pretreated with 0.1-10 µM of CUR (P< 0.05). Pretreatment with 0.1-10 µM of CUR decreased ROS production and lipid peroxidation, and increased the activities of antioxidant enzymes, such as superoxide dismutase and glutathione peroxidase in osteoblasts induced by H(2)O(2). In addition, H(2)O(2)-induced reduction of differentiation markers such as alkaline phosphatase, calcium deposition, and Runx2 level was significantly recovered in the presence of CUR. CUR also reversed H(2)O(2)-induced stimulation of extracellular signal-regulated kinase 1/2, and nuclear factor-κB signaling and the inhibition of p38 mitogen-activated protein kinase activation. These results provide new insights into the osteoblast-protective mechanisms of CUR through reducing the production of ROS, suggesting that CUR may be developed as a bio-safe agent for the prevention and treatment of osteoporosis and other bone-related human diseases.

Curculigo orchioides, natural compounds for the treatment of noise-induced hearing loss in mice.

Noise exposure is one of the most common causes of hearing loss. Noise-induced hearing loss (NIHL) is thought to primarily involve damage to the sensory hair cells of the cochlea via mechanical and metabolic mechanisms. Curculigo orchioides Gaerten (C. orchioides) is considered to have immunostimulant, hepatoprotective, antioxidative, anticancer, and antidiabetic activities. But the effect of C. orchioides on NIHL is not yet reported, this study focused on examining the therapeutic effects of C. orchioides on NIHL in a mouse model. Oral treatment with the extract of C. orchioides began 24 h following an examination that determined a shift in hearing threshold induced by noise exposure. Hearing threshold shifts were assessed by analyzing auditory brainstem responses at 1, 5, and 7 days following noise exposure. Central auditory function was evaluated using auditory middle latency responses, and cochlear function was determined based on transient-evoked otoacoustic emissions. C. orchioides reduced hearing threshold shifts, central auditory function damage, and cochlear function deficits. Our results suggest that C. orchioides can be utilized as a potential therapeutic natural product for NIHL.

Up-regulation of VEGF by MC3T3-E1 cells treated with curculigoside.

Empirical evidence has shown that curculigoside, the main active compound of the traditionally used Chinese herb, Curculigo orchioides (Amaryllidaceae, rhizome), affects bone formation and fracture healing. However, the mechanistic details of these processes remain unclear. Therefore, the effects of curculigoside on immortalized, pre-osteoblastic mouse MC3T3-E1 cells was investigated. Following treatment with curculigoside, MC3T3-E1 cells exhibited an increased rate of proliferation. Higher levels of vascular endothelial growth factor (VEGF), Fms-like tyrosine kinase-1 (Flt-1) and bone morphogenetic protein-2 (BMP-2) were also detected in cell supernatants and cell lysates by ELISA and western blot analysis, respectively. Furthermore, the stimulatory effect of curculigoside was observed at relatively low doses (i.e. 10-100 µg/mL). In combination, these responses to treatment with curculigoside elucidate mechanistic details underlying the therapeutic effects of Curculigo orchioides on bone, and identifies these molecules as potential targets for the treatment of common metabolic bone diseases.

Cycloartane glycosides from the rhizomes of Curculigo orchioides.

Cycloartane glycosides (1-9) were isolated from rhizomes of Curculigo orchioides (Hypoxidaceae), and this structures were determined by spectroscopic analysis and a few chemical transformations. Cytotoxic activity of glycosides (1-9) and their common aglycone (1a) against HL-60 human promyelocytic leukemia cells was also examined.

Three new phenolic glycosides from Curculigo orchioides G.

Three new phenolic glycosides, curculigosides F-H (1-3), were isolated from rhizomes of Curculigo orchioides Gaertn. Their structures were elucidated based on comprehensive spectroscopic analyses including IR, MS, 1D- and 2D NMR (HSQC, COSY, and HMBC). Curculigosides F-H (1-3) were evaluated for their anti-HBV activity in vitro using the HBV transfected Hep G2.2.15 cell line. Compound 1 exhibited weak activity with an IC(50) value of 2.08 mM on hepatitis B virus (HBV) e antigen (HBeAg) secretion of the HepG2.2.15 cell line.