Compounds from the Petroleum Ether Extract of Wedelia chinensis with Cytotoxic, Anticholinesterase, Antioxidant, and Antimicrobial Activities.

Wedelia chinensis is a folk medicine used in many Asian countries to treat various ailments. Earlier investigations reported that the petroleum ether extract of the plant has potential biological activity, but the compounds responsible for activity are not yet completely known. Therefore, the current work was designed to isolate and characterize the compounds from the petroleum ether extract and to study their bioactivities. Four compounds including two diterepenes (-) kaur-16α-hydroxy-19-oic acid (1) and (-) kaur-16-en-19-oic acid (2), and two steroids ß-sitosterol (3), and cholesta-5,23-dien-3-ol (4) were isolated and characterized. Among the compounds, the diterpenes were found to have more biological activities than the steroidal compounds. Compound 1 showed the highest cytotoxicity with LC50 of 12.42 ± 0.87 µg/mL. Likewise, it possesses good antioxidant activity in terms of reducing power. On the contrary, compound 2 exerted the highest antiacetylcholinesterase and antibutyrylcholinesterase activity. Both the diterpenes showed almost similar antibacterial and antifungal activity. The identification of diterpenoid and steroid compounds with multifunctional activities suggests that W. chinensis may serve as an important source of bioactive compounds which should be further investigated in animal model for therapeutic potential in the treatment of different chronic diseases.

Evaluation of cholinesterase inhibitory and antioxidant activity of Wedelia chinensis and isolation of apigenin as an active compound.

BACKGROUND: Wedelia chinensis has been reported as a folk medicine for the treatment of different diseases including neurodegenerative disease. Although the plant has been studied well for diverse biological activities, the effect of this plant in neurological disorder is largely unknown. The present study was undertaken to evaluate the cholinesterase inhibitory and antioxidant potential of W. chinensis. METHODS: The extract and fractions of the plant were evaluated for acetylcholinesterase and butyrylcholinesterase inhibitory activity by modified Ellman method. The antioxidant activity was assessed in several in vitro models/assays such as reducing power, total antioxidant capacity, total phenolic and flavonoid content, scavenging of 2,2'-diphenyl-1-picrylhydrazyl (DPPH) free radical and hydroxyl radical, and inhibition of brain lipid peroxidation. Chromatographic and spectroscopic methods were used to isolate and identify the active compound from the extract. RESULTS: Among the fractions, aqueous fraction (AQF) and ethylacetate fraction (EAF) exhibited high inhibition against acetylcholinesterase (IC50: 40.02 ± 0.16 µg/ml and 57.76 ± 0.37 µg/ml) and butyrylcholinesterase (IC50: 31.79 ± 0.18 µg/ml and 48.41 ± 0.05 µg/ml). Similarly, the EAF and AQF had high content of phenolics and flavonoids and possess strong antioxidant activity in several antioxidant assays including DPPH and hydroxyl radical scavenging, reducing power and total antioxidant activity. They effectively inhibited the peroxidation of brain lipid in vitro with IC50 values of 45.20 ± 0.10 µg/ml and 25.53 ± 0.04 µg/ml, respectively. A significant correlation was observed between total flavonoids and antioxidant and cholinesterase inhibitory activity. Activity guided chromatographic separation led to the isolation of a major active compound from the EAF and its structure was elucidated as apigenin by spectral analysis. CONCLUSIONS: The potential ability of W. chinensis to inhibit the cholinesterase activity and peroxidation of lipids suggest that the plant might be useful for the management of AD.

[Study on chemical constituents of Wedelia trilobata].

A new taraxer-based triterpenoid ester, taraxer-14-en-30-al-3ß-O-palmitate(1), was isolated from the whole plant of Wedelia trilobata, along with six known compounds, ent-kaur-16-en-19-oic acid(2), 16α-hydroxy-ent-kauran-19-oic acid(3), tara-xerol(4), ß-amyrin(5), 1ß-acetoxy-4α, 9α-dihydroxy-6ß-isobutyroxyprostatolide(6), and stigmasterol(7). Their structures were elucidated with use of a combination of spectroscopic techniques(IR, HR-ESI-MS, 1 D, 2 D NMR data) and chemical methods.

Differential Effects of Wedelia chinensis on Human Glioblastoma Multiforme Cells.

INTRODUCTION: Glioblastoma multiforme (GBM) is the most aggressive glioma, and its diffuse nature makes resection of it difficult. Moreover, even with the administration of postoperative radiotherapy and chemotherapy, prolonged remission is often not achieved. Hence, innovative or alternative treatments for GBM are urgently required. Traditional Chinese herbs and their functional components have long been used in the treatment of various cancers, including GBM. The current study investigated the antitumor activity of Wedelia chinensis and its major functional components, luteolin and apigenin, on GBM. MATERIALS AND METHODS: MTT assay, Transwell migration assay, and flow cytometry analysis were adopted to assess the cell viability, invasive capability, and cell cycle. Immunofluorescence staining and Western blotting were used to detect the expressions of apoptotic and autophagy-related signaling molecules. RESULTS: The W. chinensis extract (WCE) significantly inhibited the proliferation and invasive ability of both GBM8401 and U-87MG cells in a dose-dependent manner. Moreover, differential effects of WCE on GBM8401 and U-87MG cells were observed: WCE induced apoptosis in GBM8401 cells and autophagy in U-87MG cells. Notably, WCE had significant effects in reducing the cell survival and invasive capability of both GBM8401 and U-87MG cells than the combination of luteolin and apigenin. CONCLUSIONS: Taken together, these findings indicate the potential of using WCE and the combination of luteolin and apigenin for GBM treatment. However, further investigations are warranted before considering recommending the clinical use of WCE or the combination of luteolin and apigenin as the standard for GBM treatment.

3α-Angeloyloxy-ent-kaur-16-en-19-oic Acid Isolated from Wedelia trilobata L. Alleviates Xylene-Induced Mouse Ear Edema and Inhibits NF-κB and MAPK Pathway in LPS-Stimulated Macrophages.

Uncontrolled inflammation is associated with many major diseases, and there is still an urgent need to develop new anti-inflammatory drugs. 3α-Angeloyloxy-ent-kaur-16-en-19-oic acid (WT-25) is an ent-kaurane dieterpenoid extracted from Wedelia trilobata, a medicinal plant with potential anti-inflammatory activity. The anti-inflammatory activity of WT-25 is better than that of its analog kaurenoic acid, but the underlying mechanism is still unknown. In this study, our aim was to study the anti-inflammatory effect of WT-25. In xylene-induced edema in mice, WT-25 produced 51% inhibition. WT-25 suppressed nitric oxide (NO) and prostaglandin E2 (PGE2) production in LPS-stimulated RAW264.7 cells by downregulating the expression of nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). WT-25 reduced expression and secretion of TNF-α and IL-6. Moreover, WT-25 inhibited NF-κB activation and its upstream signaling, decreasing phosphorylation IKK and p65 levels. WT-25 also inhibited the phosphorylation of the mitogen-activated protein kinases (MAPKs) family. Additionally, it reduced LPS-induced excessive release of reactive oxygen species (ROS) and maintained mitochondrial integrity in RAW264.7 cells. All these results indicate that WT-25 is a bioactive molecule with the potential to be developed as a novel structured anti-inflammatory drug.

Silver nanoparticles synthesis using Wedelia urticifolia (Blume) DC. flower extract: Characterization and antibacterial activity evaluation.

Silver nanoparticles (AgNPs), synthesized by green methods with the property to kill microbes, are highly valuable in medical sciences. So, the current study was aimed at using the flower extract of Wedelia urticifolia for synthesizing AgNPs with antibacterial properties. The AgNPs were produced by adding the extract to three different AgNO3 concentrations (1, 10, and 100 mM) in nine possible flower extract to metal salt ratios (9:1, 8:2, 7:3, 6:4, 5:5, 4:6, 3:7, 2:8, and 1:9). The formation of brown color and the presence of a peak at 431 nm in the UV-Vis spectrum of the colloidal solution indicates the synthesis of AgNPs, which were also characterized by dynamic light scattering (DLS), Fourier transform infrared spectroscopy, X-ray diffraction, scanning electron microscopy, transmission electron microscopy, and energy-dispersive X-ray spectroscopy. The DLS results exposed that the smallest sized AgNPs were obtained in 10 mM AgNO3 solution and 4E6M was the optimized extract to metal salt solution ratio. The characterization techniques revealed that the synthesized AgNPs were spherical shaped and crystalline with a diameter of less than 30 nm. Furthermore, the synthesized nanoparticles were tested against two Gram-positive (Klebsiella pneumonia and Staphylococcus aureus) and two Gram-negative (Pseudomonas aeruginosa and Escherichia coli) bacterial strains for their antibacterial efficiency. Although the studied strains showed limited growth, overall, the effect of nanoparticles was found to be insignificant. It is concluded that the current study is advantageous over other previous studies because the AgNPs were synthesized at room temperature from 10 mM AgNO3 concentration in only 2 hours. Additionally, the present work is simple, ecofriendly, and in-expensive.

Anti-proliferative and anti-neuroinflammatory eudesmanolides from Wedelia (Sphagneticola trilobata (L.) Pruski).

Wedelia (Sphagneticola trilobata, Syn. Wedelia trilobata), a notoriously invasive agricultural weed, can inhibit the growth and development of crops in the field. Eight new eudesmanolides (1-8), along with twelve known congeners (9-20), were isolated and identified from the flowers of Wedelia. Their chemical structures were elucidated through various spectroscopic techniques. The isolates were tested for anti-proliferative activities against HeLa, HepG2, and SGC-7901 tumor cell lines. Most eudesmanolides exhibited significant anti-proliferative activities with good selectivity. Meanwhile, the cells morphology and clonogenic survival assays were observed for compounds 1-3. Moreover, compound 6 displayed obvious anti-neuroinflammatory effect by inhibition of NO production in LPS-induced microglia BV-2 cells with the IC50 value of 11.77 ± 0.83 µM. Hence, this study demonstrated that the eudesmanolides from Wedelia possessed significant antitumor and anti-inflammatory activity, which provided some guides for the further development and a new thinking for its control.

Wedtrilosides A and B, two new diterpenoid glycosides from the leaves of Wedelia trilobata (L.) Hitchc. with α-amylase and α-glucosidase inhibitory activities.

In the ongoing research to find new diabetes constituents from the genus Wedelia, the chemical constituent of Wedelia trilobata leaves, a Vietnamese medicinal plant species used to treat type 2 diabetes mellitus, was selected for detailed investigation. From a methanolic extract, two new ent-kaurane diterpenoids, wedtrilosides A and B (1 and 2), along with five known metabolites (3-7), were isolated from W. trilobata. The chemical structures of (1-7) were assigned via spectroscopic techniques (IR, 1D, 2D NMR and HR-QTOF-MS data) and chemical methods. The isolates were evaluated for α-amylase and α-glucosidase inhibitory activities compared to the clinical drug acarbose. Among them, compounds 4, 6, and 7 showed the most potent against α-glucosidase enzyme with IC50 values of 27.54 ±â€¯1.12, 173.78 ±â€¯2.37, and 190.40 ±â€¯2.01 µg/mL. While moderate inhibitory effect against α-amylase was observed with compounds 6 and 7 (with IC50 = 181.97 ±â€¯2.62 and 52.08 ±â€¯0.56 µg/mL, respectively). The results suggested that the antidiabetic properties from the leaves of W. trilobata are not simply a result of each isolated compound, but are due to other factors such as the accessibility of polyphenolic groups to α-amylase and α-glucosidase activities.

Chemical composition and antimicrobial activities of essential oil from Wedelia urticifolia growing wild in Hunan Province, China.

The essential oil obtained from Wedelia urticifolia growing in Hunan Province, China, was analyzed for the first time by capillary GC and GC-MS. A total of 67 constituents, representing 98.68% in essential oil were identified. The major constituents of the oil were: α-pinene (8.85%), limonene (6.38%), carvacrol (6.15%), caryophyllene (6.08%), spathulenol (5.49%), sabinene (5.36%), camphor (4.34%). Antimicrobial potential of oil against bacterial strains (Pseudomonas aeruginosa, Escherichia coli and Bacillus subtilis, and Staphylococcus aureus), yeast strains (Hansenula anomala and Saccharomy cescerevisiae) and molds (Aspergillus niger, Chaetomium globosum, Mucor racemosus, and Monascus anka) was determined by disc diffusion method and broth micro dilution method, respectively. The oil exhibited promising antimicrobial effect as a diameter of zones of inhibition (16.8-24.9 mm). Minimum inhibitory concentration values of oil were ranged 62.5-1000 µg/mL.

Transcriptomic analysis reveals a controlling mechanism for NLRP3 and IL-17A in dextran sulfate sodium (DSS)-induced colitis.

The incidence of inflammatory bowel disease (IBD) has markedly increased. Our research findings during the past showed that medicinal plant extracts and the derived phytochemical components from Wedelia chinensis (WC) can have strong anti-colitis activities. Here, we further identified the key component phytochemicals from active fractions of different WC preparations (WCHA) that are responsible for the protective effect of WCHA in colitis mice. Of the 3 major compounds (wedelolactone, luteolin and apigenin) in this fraction, luteolin had the highest anti-inflammatory effect in vivo. Using a next-generation sequencing (NGS) (e.g., RNA-seq) system to analyze the transcriptome of colorectal cells/tissues in mice with dextran sulfate sodium (DSS)-induced colitis with/without phytochemicals treatment, luteolin was found to strongly suppress the DSS-activated IL-17 pathway in colon tissue. In addition, co-treatment with wedelolactone and luteolin had a synergistic effect on the expression level of some IL-17 pathway-related genes. Interestingly, our NGS analyses also indicated that luteolin and wedelolactone can specifically suppress the expression of NLRP3 and NLRP1. Using a 3-dimensional cell co-culture system, we further demonstrated that luteolin could efficiently suppress NLRP3 expression via disruption of IL-17A signaling in inflamed colon tissue, which also indicates the pharmacological potential of luteolin and wedelolactone in treating IBD.

Exploration of Wedelia chinensis leaf-assisted silver nanoparticles for antioxidant, antibacterial and in vitro cytotoxic applications.

Green synthetic route of silver nanoparticles (AgNPs) has already been proved to be an advantageous over other physico-chemical approaches due to its simplicity, cost effectiveness, ecofriendly and nontoxicity. In this finding, aqueous Wedelia chinensis leaf extract (WLE) mediated synthesis of AgNPs was approached. Surface plasmon resonance (SPR) band at 408 nm preliminary indicated the formation of AgNPs, while TEM and XRD characterization confirmed the formation of spherically shaped and crystalline AgNPs with an average size of 31.68 nm, respectively. The plausible biomolecules in the aqueous leaf extract responsible for the reduction and stabilization of AgNPs were identified by FTIR analysis and found to be polyphenolic groups in flavonoid. Further, synthesized AgNPs was explored for different biological applications. Biosynthesized AgNPs showed significant free radical scavenging activity as compared to Wedelia leaf extract and antibacterial activity against clinically isolated test pathogens where Gram-negative bacteria were found more susceptible to AgNPs than Gram-positive one. In addition, in vitro cytotoxic response was also evaluated on hepatocellular carcinoma Hep G2 cell lines and showed a dose-dependent cytotoxic response with an IC50 value of 25 µg/mL.

Eudesmanolides and Other Constituents from the Flowers of Wedelia trilobata.

Two eudesmane sesquiterpene lactones, wedetrilides B (1) and C (2), along with five known analogues (3 - 8), an ent-kaurane diterpenoid (9), a steroid (10), as well as cinnamic acid derivatives (11 - 13), were isolated from the flowers of Wedelia trilobata. Their structures were elucidated on the basis of extensive spectroscopic analyses and by comparison of their NMR data with those of related compounds. Furthermore, the structures of 1 and 3 - 5 were confirmed by X-ray single-crystal diffraction analyses. Compounds 4 and 5 exhibited weak cytotoxic activities against the MCF-7, HeLa, and A549 cell lines. Compounds 3 - 5 were also evaluated for their inhibitory effects against HIV lytic replication.

High toxicity of camphene and γ-elemene from Wedelia prostrata essential oil against larvae of Spodoptera litura (Lepidoptera: Noctuidae).

The development of eco-friendly biopesticides in the fight against agricultural pests is an important challenge nowadays. The essential oil of Wedelia prostrata Hemsl. is known for its multipurpose biological activities in Chinese folk medicine. However, limited efforts attempted to understand the potential insecticidal activity of its main individual constituents and related mechanism of action. In this research, we investigated the insecticidal activity of W. prostrata against the crop pest Spodoptera litura (Fabricius) (Lepidoptera: Noctuidae). Toxicity on 4th instar larvae was assessed after 24 h of exposure. The LC50 and LC90 of the W. prostrata essential oil were 167.46 and 322.12 µg/ml, respectively. GC-MS analyses were carried out to shed light on the oil chemical composition. Main constituents were the monoterpene camphene (9.6%) and the sesquiterpenes γ-elemene (7.6%), α-humulene (6.9%), and (E,E)-α-farnesene (7.3%). The pure constituents were evaluated for their insecticidal activity on S. litura 4th instar larvae. The most toxic molecule was camphene (LC50 = 6.28 µg/ml), followed by γ-elemene, (LC50 = 10.64 µg/ml), α-humulene (LC50 = 12.89 µg/ml), and (E,E)-α-farnesene (LC50 = 16.77 µg/ml). Overall, our experiments highlighted the promising potential of camphene and γ-elemene from W. prostrata essential oil against larvae of S. litura, allowing us to propose these two compounds for the development of newer pesticides in the fight against crop pests. Further studies aimed at evaluating the potential synergy between these two molecules, as well as their stability in field conditions are ongoing.

Triterpenoids principle of Wedelia calendulacea attenuated diethynitrosamine-induced hepatocellular carcinoma via down-regulating oxidative stress, inflammation and pathology via NF-kB pathway.

The aerial part of Wedelia calendulacea have been used in Ayurveda, Unani, Tibetan, Siddha and other folk medicine systems to protect the liver and renal tissue. Liver is considered as primary metabolizing site of body, which is prone to damage by endogenous and exogenous toxicants. A reason for liver toxicity, and major causes of the hepatocellular carcinoma (HCC). 19-α-Hydroxyurs-12(13)-ene-28 oic acid-3-O-ß-D-glucopyranoside (HEG), a triterpenoids found in the higher plants, has been known to possess protective effect against various toxicants. The aim of the current study was to scrutinize the hepatoprotective mechanism of HEG against DEN-induced oxidative stress, hyperproliferation, inflammation and apoptosis tissue injury in Wistar rats. Invitro cell lines study of HEG scrutinized against the Hep-G2 and HuH-7 cells. A single dose of DEN (200 mg/kg) and double dose of phenobarbitol were administered to induce the liver damage in rats; the dose treatment of HEG was terminated at the end of 22 weeks. Macroscopical study was performed for the confirmation of hepatic nodules. The serum and hepatic samples were collected for further biochemical and histopathological analysis. Hepatic; non-hepatic; Phase I and II antioxidant enzymes were also examined. Additionally, we also scrutinized the inflammatory cytokines viz., tumor necrosis factor-α, interlukin-6, interlukin-1ß, and Nuclear factor kappa beta (NF-kB), respectively. Histopathological study was also performed for analyzing the changes during the HCC. HEG confirmed the reduction of growth and deoxyribonucleic acid synthesis of both cell lines. DEN successfully induced the HCC in all group, which was significantly (p < 0.001) altered by the HEG in a dose-dependent manner. The decreased level of pro-inflammatory cytokines and altered membrane-bound enzyme activity were also observed. HEG inhibits the phase I, II and antioxidant enzymes at the effective dose-dependent manner, which were considered as the precursor of the HCC. The alteration of phase I, II and antioxidant enzymes confirmed the inhibition of inflammatory reaction and oxidative stress, which directly or indirectly inhibited the NF-kB expression. Collectively, we can conclude that the HEG inhibited the growth of Hepatocellular carcinoma via attenuating the NF-kB pathway.

A standardized herbal extract mitigates tumor inflammation and augments chemotherapy effect of docetaxel in prostate cancer.

Activation of the NFκB pathway is often associated with advanced cancer and has thus been regarded as a rational therapeutic target. Wedelia chinensis is rich in luteolin, apigenin, and wedelolactone that act synergistically to suppress androgen receptor activity in prostate cancer. Interestingly, our evaluation of a standardized Wedelia chinensis herbal extract (WCE) concluded its efficacy on hormone-refractory prostate cancer through systemic mechanisms. Oral administration of WCE significantly attenuated tumor growth and metastasis in orthotopic PC-3 and DU145 xenografts. Genome-wide transcriptome analysis of these tumors revealed that WCE suppressed the expression of IKKα/ß phosphorylation and downstream cytokines/chemokines, e.g., IL6, CXCL1, and CXCL8. Through restraining the cytokines expression, WCE reduced tumor-elicited infiltration of myeloid-derived suppressor cells (MDSCs), tumor-associated macrophages (TAMs) and endothelial cells into the tumors, therefore inhibiting angiogenesis, tumor growth, and metastasis. In MDSCs, WCE also reduced STAT3 activation, downregulated S100A8 expression and prevented their expansion. Use of WCE in combination with docetaxel significantly suppressed docetaxel-induced NFκB activation, boosted the therapeutic effect and reduced the systemic toxicity caused by docetaxel monotherapy. These data suggest that a standardized preparation of Wedelia chinensis extract improved prostate cancer therapy through immunomodulation and has potential application as an adjuvant agent for castration-resistant prostate cancer.

Two new kaurane-type diterpenoids from Wedelia chinensis (Osbeck.) Merr.

Two new kaurane-type diterpenoids, 3α-(angeloyloxy)-17-hydroxy-ent-kaur-15-en-19-oic acid (1) and 3α-(tigloyloxy)-17-hydroxy-ent-kaur-15-en-19-oic acid (2), along with 10 known compounds (3-12) were isolated from the whole plant of Wedelia chinensis (Osbeck.) Merr. Their structures were elucidated on the basis of extensive spectroscopic analyses (UV, IR, MS and NMR) and comparison with literature data. Compounds 3 and 4 showed moderate inhibitory activity against the Staphylococcus aureus subsp. aureus ATCC29213 with MIC50 19.35 and 18.31 µg/mL, respectively.

PURIFICATION AND FRACTIONAL ANALYSIS OF METHANOLIC EXTRACT OF WEDELIA TRILOBATA POSSESSING APOPTOTIC AND ANTI-LEUKEMIC ACTIVITY.

BACKGROUND: Wedelia trilobata (L.) Hitch (WT), commonly known as yellow dots or creeping daisy, is a shrub possessing potent biological activities, and is traditionally used a medicinal plant in Ayurveda, Siddha and Unani systems of medicines, and it has also been tried against leukemia cell line MEG- 01. In the present study, purification and screening of the plant was done for bioactive compounds in methanolic extract of WT for apoptotic and anti-leukemia activity. MATERIALS AND METHODS: The methanolic extract of WT was initially purified through thin layer chromatography (TLC) and screened for the apoptotic and anti-leukemia activities. The positive band of TLC was subjected to silica gel column chromatography for further purification and the fractions obtained from it were screened again for anti-leukemia activity through thymidine uptake assay and apoptotic activity by DNA fragmentation, nuclear staining and flow cytometry assays. The fraction with positive result was subjected to HPLC for analysis of bioactive components. RESULTS: Out of many combinations of solvents, the methanol and dichloromethane combination in the ratio 6:4 has revealed two bands in TLC, among which the second band showed positive results for apoptotic and anti-leukemic activities. Further purification of second band through silica gel chromatography gave five fractions in which the 3rd fraction gave positive results and it shows single peak during compositional analysis through HPLC. CONCLUSION: The single peak revealed through HPLC indicates the presence of pure compound with apoptotic and anti-leukemia activities encouraging for further structural analysis.

Novel glycoside from Wedelia calendulacea inhibits diethyl nitrosamine-induced renal cancer via downregulating the COX-2 and PEG2 through nuclear factor-κB pathway.

A new compound derivative of glycoside 19-α-hydroxy-ursolic acid glucoside (19-α-hydroxyurs-12(13)-ene-28-oic acid-3-O-ß-D-glucopyranoside (HEG) was isolated from whole plant of Wedelia calendulacea (Compositae). The structure was elucidated and established by standard spectroscopy approaches. Diethylnitrosamine (DEN) (200 mg/kg) and ferric nitrilotriacetate (Fe-NTA) (9 mg/kg) were used for induction of renal cell carcinoma (RCC) in the rats. The rats were further divided into different groups and were treated with HEG doses for 22 weeks. Anti-cancer effect in RCC by HEG was dose dependent to restrict the macroscopical changes as compared to DEN + Fe-NTA-control animals. Significant alteration in biochemical parameters and dose-dependent alleviation in Phase I and Phase II antioxidant enzymes were responsible for its chemo-protective nature. HEG in dose-dependent manner was significant to alter the elevated levels of pro-inflammatory cytokines and inflammatory mediators during RCC. The histopathological changes were observed in the HEG pre-treated group, which was proof for its safety concern as far as its toxicity is concerned. The isolated compound HEG can impart momentous chemo-protection against experimental RCC by suppressing the cyclooxygenase (COX-2) and prostaglandin E2 (PGE2) expression via nuclear factor-kappa B (NF-κB) pathway.

Three new ent-kaurane diterpenes from the herbs of Wedelia prostrata.

Three new ent-kaurane diterpenes, 3α-angeloyloxy-17-hydroxy-ent-kaur-15-en-19-oic acid (1), 3α-tigloyloxy-17-hydroxy-ent-kaur-15-en-19-oic acid (2) and 3α-cinnamoyloxykaur-9(11),16-dien-19-oic acid (3), along with five known compounds (4-8), were isolated from the herbs of Wedelia prostrata (Asteraceae). The structures were determined by extensive analysis of their spectroscopic data (IR, UV, HRESIMS, 1D and 2D NMR). The isolated compounds were evaluated for their cytotoxic activity on human hepatocellular carcinoma HepG2 cells. Among them, all isolates exhibited cytotoxic activities with IC50 values ranging from 9.55 ± 0.45 to 53.92 ± 1.22 µM.

Antimicrobial Diterpenoids of Wedelia trilobata (L.) Hitchc.

Continued interest in the metabolites of Wedelia trilobata (L.) Hitchc, a notoriously invasive weed in South China, led to the isolation of twenty-six ent-kaurane diterpenoids, including seven new ones 1-7. Their structures and relative configuration were elucidated on the basis of extensive spectroscopic analysis, including 1D- and 2D-NMR experiments. The antimicrobial activities of all isolated diterpenoids were evaluated against a panel of bacteria and fungi.