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The present study evaluates the potentiality of green silver nanoparticles from the leaves and fruit extracts of Phyllanthus acidus L. against third instar larvae of two vector mosquitoes namely Culex quinquefasciatus and Culex vishnui. Various spectroscopic techniques were used to characterize the synthesized silver nanoparticles (AgNPs). Synthesized silver nanoparticles from both the leaf and fruits of P. acidus were spherical to quasi-spherical in shape and showed Surface Plasmon Resonance (SPR) bands at 420 and 409 nm respectively. In larvicidal bioassay with synthesized AgNPs from the leave of P. acidus, 100% mortality was observed at 20 ppm against third instar larvae of both the mosquito species with LC50 values of 1.64 and 0.87 ppm respectively. 100% mortality was observed in 5 ppm concentration against both Cx. quinquefasciatus and Cx. vishnui in synthesized AgNPs from fruits of P. acidus with LC50 values of 1.62 and 1.24 ppm respectively. The above findings suggest that the AgNPs synthesized from P. acidus leaves and fruit extracts have the potential to be employed in vector mosquito population control.

The present study evaluates the potentiality of green silver nanoparticles from the leaves and fruit extracts of Phyllanthus acidus L. against third instar larvae of two vector mosquitoes namely Culex quinquefasciatus and Culex vishnui. Various spectroscopic techniques were used to characterize the synthesized silver nanoparticles (AgNPs). Synthesized silver nanoparticles from both the leaf and fruits of P. acidus were spherical to quasi-spherical in shape and showed Surface Plasmon Resonance (SPR) bands at 420 and 409 nm respectively. In larvicidal bioassay with synthesized AgNPs from the leave of P. acidus, 100% mortality was observed at 20 ppm against third instar larvae of both the mosquito species with LC50 values of 1.64 and 0.87 ppm respectively. 100% mortality was observed in 5 ppm concentration against both Cx. quinquefasciatus and Cx. vishnui in synthesized AgNPs from fruits of P. acidus with LC50 values of 1.62 and 1.24 ppm respectively. The above findings suggest that the AgNPs synthesized from P. acidus leaves and fruit extracts have the potential to be employed in vector mosquito population control. [ABSTRACT FROM AUTHOR]

To provide reference for the safety consumption of Phyllanthus acidus (PA) as food and its further medicinal development and utilization, a comparative study on acute and short-termtoxicity and α-glucosidase inhibitory ability of different components of its branches and leaves was conducted. The crude extract of PA, prepared under aqueous ethanol reflux extraction, was partitioned successively with petroleum ether, ethyl acetate and N-butanol according to the polarity. Furthermore, an alcohol-eluted and water-eluted fractions were obtained from water-soluble residue by column chromatography. The half inhibitory concentration (IC50) of α-glucosidase was used as the evaluation index to compare the in vitro hypoglycemic activity of different extracts. The acute toxicity of these fractions was screened by maximum tolerated dose (MTD), median lethal dose (LD50) values, and their subacute toxicity was evaluated by continuous oral administration of samples for 20 days. The results showed that each component of PA had a certain inhibitory ability to α-glucosidase. The MTD of crude extract of PA was 2.0 g/kg, and the order of acute toxicity for different fractions was ethanol-eluted fraction>water-eluted fraction>petroleum ether fraction>ethyl acetate fraction>N-butanol fraction>crude extract. The main acute toxicity symptoms were startle followed by idling, writhing, and shortness of breath. Subacute toxicity test showed no obvious toxicity and lesions. It was indicated that it was safe to take 2 g/kg/d (equivalent to 8.6 g/kg of dried branches and leaves) of the whole component of PA at oral ingestion. Thus, they have the potential to be developed as hypoglycemic, weight-loss food and medicine.

Phyllaciduloids E (1) and F (2), two new cleistanthane diterpenoids, were isolated from the leaves of Phyllanthus acidus (L.) Skeels (Phyllanthaceae). Their planar structures were established by spectroscopic analysis and comparison with literature values. The relative configurations of phyllaciduloids E and F were confirmed by DFT-NMR chemical shift calculations and subsequent CP3 probability methods. Phyllaciduloids E and F were evaluated for their cytotoxicity. However, no significant activities were detected at concentrations up to 40 μM. [ABSTRACT FROM AUTHOR]

Background: This study describes the isolation of chemical constituents from the leaves and bark of Phyllanthus acidus, a medicinal plant widely used for the treatment of several ailments. Materials and Methods: The crude extract of P. acidus was chromatographed on a gravity column dry packed with silica gel and was fractionated by increasing proportions of acetone in CH2Cl2. The purified isolates were subjected to NMR for structure elucidation. Their structures were identified mainly by using 1H-NMR and by comparing current NMR data with those reported in the literature. Results: The results showed that the air-dried leaves extracts of the plant afforded mixture of β-sitosterol and stigmasterol while the bark yielded mixture of phyllanthol, α-amyrin, β-amyrin and lupeol. Conclusion: The air-dried of DCM extract of P. acidus resulted in the isolation of the mixture of phyllanthol, α- amyrin, β-amyrin and lupeol from the bark and mixture of β-sitosterol and stigmasterol from the leaves of the plant. It is important to conduct detailed pharmacological and toxicity investigations as well as clinical studies using different doses or concentrations to verify its traditional uses. [ABSTRACT FROM AUTHOR]

A new diterpenoid, phyllane C (1), along with three known compounds, ovoideal E (2), spruceanol (3), and fluacinoid B (4) were isolated from the leaves of Phyllanthus acidus growing in Thailand. The structures were determined by analysis of their MS and NMR data as well as by comparison with literature values. DFT-NMR chemical shift calculations and subsequent DP4/DP4+ probability methods were applied to define the relative configuration of 1. Compound 3 showed a weak cytotoxicity against K562 cell line (IC50 41.9 ± 2.31 µg/mL). [ABSTRACT FROM AUTHOR]

Phyllanthus acidus, an evergreen shrub or tree in Euphorbiaceae, is mainly distributed in Thailand, Vietnam, Myanmar, Laos, etc. It is also introduced and cultivated in Xishuangbanna and Yuanjiang areas of Yunnan Province, China. The fruits are edible and the plant has been widely used to treat various diseases, such as hypertension, asthma, diabetes, dermatitis, fever, smallpox, and so on, by the local people of its growing areas. Moreover, the young leaves are utilized as edible vegetables in Indonesia, Thailand and India. Phytochemical studies yielded sesquiterpenes, diterpenes and triterpenes from roots and stems, and flavonoids as the major chemical constituents from the leaves. Some constituents showed obvious anti-hepatitis B virus(HBV), anti-bacterial, anti-inflammatory, hepatoprotective and anti-hypertensive activities. For example, parts of the norbisabolane sesquiterpenes displayed potential anti-HBV activities, with IC50 values of 0.8-36 μmol·L-1 against HBV surface antigen(HBsAg)and HBV excreted antigen(HBeAg), and the results indicate that the ketal group at C-5 and sugar moieties at C-13 play important roles in the selectivity of HBsAg and HBeAg. This paper reviews the research progress of chemical constituents and pharmacological activities of the plant from 1966 to 2020, which provides scientific evidence and reference for its future study, spread, application and development. [ABSTRACT FROM AUTHOR]

A novel highly oxygenated norbisabolane sesquiterpene, namely phyllanthacidoid U (1), along with nine known sesquiterpenes (2–10) was isolated from the roots and stems of Phyllanthus acidus (L.) Skeels (Phyllanthaceae), collected from Xishuangbanna, Yunnan province, China. Their structures were elucidated by means of extensive spectroscopic analysis and by comparison of their data with reported values in literatures. Instead of the C-13 ester O-glycosyl found mostly in the titled plant growing in Thailand, compound 1 possessed a rare N-β-glucosamine-2-N-acetate moiety linked directly to the carbonyl at C-13 through an amido bond. Moreover, the acyl group at C-10 in 1 was (Z)-2-(2-hydroxyethyl)-pent-2-enedioyl group, instead of benzoic or p-hydroxybenzoic moieties found commonly in the reported norbisabolane sesquiterpenes. The known sesquiterpene 5 displayed stronger anti hepatitis B virus (HBV) activity with IC50 values of 1.69 ± 0.22 and 2.79 ± 0.69 μM towards HBV surface antigen (HBsAg) and HBV excreted antigen (HBeAg) secretion, respectively. [ABSTRACT FROM AUTHOR]

A new norlupane triterpenoid, 29-norlupane-1β-hydroxy-3,20-dione (1), along with ten known compounds, 29-norlup-1-ene-3,20-dione (2), phyllanthol (3), phyllanthone (4), glochidone (5), lupeol (6), lupeone (7), 4-hydroxybenzoic acid (8), 4-hydroxybenzaldehyde (9), phyllane A (10) and methyl β-orsellinate (11) were isolated the twigs and leaves of Phyllanthus acidus. The structure of 1 was identified by interpretation of their spectroscopic data and comparison with those reported in the literature. In addition, all isolated compounds 1–11 were evaluated for their antioxidant activity. [ABSTRACT FROM AUTHOR]

• The screening of biological activities of medicinal plants are emphasized due to the adverse effects of synthetic drugs. • The present study demonstrates antioxidant, cytotoxic, and haemagglutination activity as well as EAC cell growth inhibitory effect of methanolic extract of Phyllantus acidus (L.) (MEPA) fruit pulp and seed. • P. acidus is traditionally used as herbal medicine in China, Brazil, and South Asian countries like Bangladesh for the treatment of digestive, respiratory, genitourinary, and skin disorder. • The result of this study suggested that MEPA fruit pulp has a more antioxidant potentiality and EAC cell growth inhibitory property than seed which indicates the presence of effective phytochemicals in MEPA fruit pulp. • Therefore, the MEPA fruit pulp can be considered as a promising biological source to search novel compounds for therapeutic purposes. Medicinal plant-derived bioactive compounds have recently gained more interest in biological research as an important source of novel drug candidates. Phyllanthus acidus (L.) is a widely distributed herbal medicinal plant naturally used in Ayurvedic medicine in Bangladesh. The present study focused on exploring the biological potential as well as the inhibitory effect of EAC cell growth with a comparative analysis between Phyllanthus acidus fruit pulp and seed. Crude methanol extract of P. acidus (MEPA) fruit pulp and seed was assessed as DPPH and NO free radical scavengers. While Brine Shrimp lethality bioassay, the standard protocol of phytochemical screening and hemagglutination assay were performed successively to determine the toxic effect on normal cells, the identification of some crucial phytochemicals, and the existence of lectin protein. EAC (Ehrlich's Ascites Carcinoma) cell growth inhibition was determined by hemocytometer and morphological changes of EAC cells were observed by a fluorescence microscope using Swiss albino mice. The IC 50 value of MEPA fruit pulp and seed was obtained as 57.159 µg/ml and 288.743 µg/ml respectively where minimal toxic effects on Brine Shrimp nauplii demonstrates that it is a good source of natural antioxidant compounds. Again, MEPA fruit pulp and seed-mediated effective agglutination of mouse blood erythrocyte strongly support the presence of lectin protein. Furthermore, MEPA fruit pulp and seed extract-treated EAC cells showed 65.71% and 28.57% growth inhibition respectively. The fluorescent microscopic examination of EAC cells treated with MEPA fruit pulp has shown more remarkable structural changes in the nucleus than that of seed. Based on the above findings, the present study reveals that MEPA fruit pulp can be considered as a novel biological candidate for the treatment of fatal diseases shortly. [ABSTRACT FROM AUTHOR]

Abstract In our present investigation, synthesis of nontoxic, eco friendly and cost effective silver nanoparticles, Phyllanthus acidus (P. acidus) was used as starting material. The influence of phyto-constituents present in aqueous extracts of Phyllanthus acidus was found to be effective in reduction of silver nitrate to free silver nanoparticles (PA-AgNPs). HPTLC finger print analysis reveals the presence of flavonoid, quercetin in aqueous extracts of Phyllanthus acidus. Surface plasmon racemonance exhibited λ max at 462 nm through UV–Vis spectroscopy. Zeta size revealed that the size of nanoparticles were with in the range of 65–250 nm with polydisperse index (PDI) of 0.451. The negative charge of zeta potential value (− 16.4) indicates repulsion among PA-AgNPs with their excellent stability. FESEM-EDAX, XRD and TEM analysis confirmed the presence of nano-crystalline PA-AgNPs with different morphological textures. Further, PA-AgNPs has shown potent antibacterial effect on E. coli cells. The greater antibacterial effect (viable and dead cells) of PA-AgNPs were confirmed by using acridine orange (AO) dye which can able to provide insight of healthy as well as damaged DNA. Live cells emit florescence green and dead cells (treated with PA-AgNPS at 20 and 40 µg/ml) appear as pale orange red colour. Post treatment, investigations of PA-AgNPs on E. coli cells under SEM was found to be effective against cell membrane damages which leads to cell death or cell growth arrest. Hence, from the above findings, we strongly recommend silver nanoparticles from Phyllanthus acidus can be used as a potential source for antimicrobial agent for chronic infections and also against other harmful microorganisms.

Oxidative stress is an important part of diabetic physiopathology; therefore, naturally derived antioxidants as therapeutic agents are needed. The present work examined the antioxidant and antidiabetic potentials of seed extract of Phyllanthus acidus (L.) Skeels. Ethanolic seed extract of P. acidus (PSE) was prepared using Soxhlet extraction. Preliminary phytochemical analysis, total phenolic (TPC), and total flavonoid (TFC) contents of PSE were determined. The in vitro inhibitory effects of PSE on 1,1-diphenyl-2 picrylhydrazyl (DPPH), 2, 2-azino-bis (3-ethylbenzthiazoline-6-sulphonic acid) (ABTS) free radicals, α-amylase, and α-glucosidase enzyme inhibitory activities were also assessed. Acute oral toxicity of PSE was carried out in female Sprague Dawley (SD) rats. PSE's hypoglycaemic effect was demonstrated in normoglycemic and streptozotocin-induced (STZ, 55 mg/kg, ip) diabetic rats. The TPC and TFC were found to be 3.19 mg of gallic acid equivalent/g (GAE/g), and 2.58 mg of quercetin equivalent/ g of extract (QE/g), respectively. The inhibitory concentration 50% (IC50) values, based on the inhibition of DPPH (IC50 28.26 ± 0.39 μg/mL), ABTS (IC50 23.44 ± 0.48 μg/mL) radicals, α-amylase (IC50 26.83 ± 0.39 μg/mL), and α-glucosidase (IC50 19.12 ± 0.26 μg/mL) enzymes were generally lower, which demonstrated their potent antioxidant and antidiabetic effects, respectively. Based on the acute oral toxicity test, two doses (100 and 200 mg/kg) of PSE were tested in normoglycemic rats. A significant (p < 0.01) fall in blood glucose was observed at 8 and 12 h after PSE (200 mg/kg) treatment. The same dose was tested in STZ rats and compared with glibenclamide (5 mg/kg). A significant (p < 0.01 and p < 0.001) decrease in the blood glucose level was observed after 8 and 12 h of PSE treatment, respectively. These findings suggest that PSE could be used as an active ingredient in herbal formulations to manage diabetes mellitus. [ABSTRACT FROM AUTHOR]

Monkeypox is a communicable disease similar to smallpox, primarily occurring in African countries. However, recently it has spread to countries outside Africa and may arise as the next threat after COVID-pandemic. The causative organism, i.e. Monkeypox Virus (MPV) spreads from one individual to another primarily through inhalation of respiratory droplets or through contact with skin lesions of infected individuals. No known drugs are available specifically for MPV. Due to its similarity with smallpox, treatment of monkeypox is being attempted through the administration of the smallpox vaccine. Therefore, we evaluated the efficacy of the plant Phyllanthus acidus against MPV since it is traditionally used in the treatment of chickenpox and smallpox. Through functional annotation, PASS prediction and Network pharmacology analysis, the effectiveness of these chosen P. acidus -derived phytocompounds against MPV was confirmed. Target prediction of the phytocompounds identified in GC-MS analysis of the plant extract showed them to be associated with 76 human proteins. The compounds also show good binding affinity with selected viral proteins: DNA polymerase (DNApol), Putative Virulence Factor (vPVF) and Cytokine Binding Protein. Prediction of Activity Spectra for Substances (PASS) and functional annotation of the target proteins further support their antiviral nature through interaction with these proteins. The compounds were found to modulate pathways related to symptoms of viral infection and this may help in maintaining homeostasis. Our study demonstrates antiviral activity as well as the therapeutic potential of the plant against MPV infection.Communicated by Ramaswamy H. Sarma.

Graphical abstract Highlights • A strongest multiple fluorescent N-CQDs were synthesized from the P. acidus fruits. • Synthesized N-CQDs showed low-toxic and were employed for in vivo live-cell imaging. • The N-CQDs were uniformly stained within the body of the nematodes (C. elegans). • The live-cell imaging result reveals the usage of N-CQDs in drug delivery. Abstract In this work, nitrogen-doped carbon quantum dots (N-CQDs) have been synthesized successfully by a simple hydrothermal method and demonstrated its application for multicolor imaging in Caenorhabditis elegans (C. elegans) as an in vivo model. The synthesized N-CQDs were characterized by various physicochemical techniques such as XRD, Raman spectroscopy, ATR-FTIR spectroscopy, XPS, HRTEM, UV–vis spectroscopy, and fluorescence spectroscopy. The synthesized N-CQDs exhibited a strong fluorescence due to the uniform size distribution with nitrogen-containing and oxygen-containing functional groups onto the surface of N-CQDs which induce the excellent dispersibility in aqueous media. The N-CQDs has an excitation-dependent fluorescence behavior and the strongest fluorescence appeared at 411 nm (emission peak position) under the excitation of 340 nm. Also, the N-CQDs displayed a high quantum yield (QY) of 12.5. The fluorescence behaviour of the aqueous N-CQDs suspension retains for a long time up to 1 year. The prolonging fluorescent N-CQDs was utilized as a staining agent for bioimaging and toxicity of N-CQDs on C. elegans that was conducted by killing assay. In-vivo studies suggested that the N-CQDs displayed excellent biocompatibility and successfully used for high-contrast imaging of N-CQDs in living and dead C. elegans. Based on the strongest fluorescence along with excellent aqueous dispersibility and biocompatibility, the green synthesized N-CQDs would be an ideal candidate for many biological applications. [ABSTRACT FROM AUTHOR]

Four new cleistanthane diterpenoids, phyllaciduloids A–D ( 1 – 4 ), were isolated from the roots and stems of Phyllanthus acidus (L.) Skeels (Phyllanthaceae). Their structures were elucidated on the basis of extensive spectroscopic analysis. Phyllaciduloids B–D ( 2 – 4 ) present in their structures with ether bond between C-7 and C-16, which were rarely reported. All the isolates were evaluated for their cytotoxic activities against five human cancer cell lines. [ABSTRACT FROM AUTHOR]

A facile, economical and one-step hydrothermal method is used to synthesize highly durable fluorescent nitrogen-doped carbon dots (FNCDs) by utilizing Phyllanthus acidus ( P. acidus ) and aqueous ammonia as the carbon and nitrogen sources, respectively. The synthesized FNCDs have an average size of 4.5±1 nm and showed bright blue fluorescence under the irradiation of UV-light at an excitation wavelength of 365 nm. It exhibits a quantum yield (QY) of 14% at an excitation wavelength of 350 nm with maximum emission at 420 nm. X-ray photoelectron spectroscopy (XPS) and Fourier transform infrared (FTIR) spectroscopy characterizations clearly showed the formation of FNCDs that predominantly consists of nitrogen and hydroxyl groups which can provide more adsorption sites. In addition, the above study reveals the successful bonding of nitrogen with carbon (C–N) in the FNCDs. The synthesized FNCDs with high QY can be used as efficient fluorescent probes for the detection of Fe 3+ . Based on the linear relationship between normalized fluorescence intensity and concentration of Fe 3+ ions, the prepared FNCDs can be used for label-free sensitive and selective detection of Fe 3+ ions in a wide concentration range of 2–25 μM with a detection limit of 0.9 μM. The present study proves that synthesized FNCDs has durable fluorescence, soluble in water very well and thus act as a promising candidate for the diverse applications such as label-free sensitive and selective detection of Fe 3+ , fluorescent ink and cellular imaging with good biocompatibility and low cytotoxicity. [ABSTRACT FROM AUTHOR]

Two novel diterpenes, phyllanes A and B, were isolated from the roots of Phyllanthus acidus , along with the cleistanthane diterpene, spruceanol. Their chemical structures were unambiguously elucidated by extensive 1D and 2D NMR analyses and high resolution mass spectroscopic data, as well as by comparison with literature data. While phyllanes A and B are respectively reminiscent of amphilectane and serrulatane diterpenoids, their highly unusual substitution patterns and their co-occurrence with spruceanol led us to assume that they might correspond to an unprecedented type of re-arranged cleistanthane-diterpenoid precursors, resulting in final products that display a unique scaffold among terrestrial diterpenoids. Accordingly, a possible biosynthetic route to the two new compounds from the readily accessible spruceanol is proposed herein. These two compounds were evaluated for their cytotoxic activities against two cancer cell lines. Only phyllane B exerted a moderate activity against K562 and HepG2 cell line with IC 50 values of 28.90 and 45.23 μg/mL, respectively. [ABSTRACT FROM AUTHOR]

A new derivative kaempferol glycoside, kaempferol-3- O-(2- α- l-rhamnopyranosyl)- β- d-glucuronopyranosyl methyl ester ( 3), together with six other known kaempferol glycosides, kaempferol-3- O-[ α- l-rhamnopyranosyl (1→2)]- β- d-galactopyranoside ( 1), kaempferol-3- O-(2- α- l-rhamnopyranosyl)- β- d-glucuronopyranoside ( 2), rutin ( 4), isoquercitrin ( 5), quercitrin ( 6), and myricitrin ( 7) were isolated from the leaves of Phyllanthus acidus (L.) Skeels (Phyllanthaceae). Here, is the first report described the isolation of compound ( 1) and ( 2) from the genus Phyllanthus. Compound ( 1) presents antioxidant activity in 2,2-diphenyl-1-picryl-hydrazyl-hydrate assay. Compound ( 2) and ( 3) performed no antioxidant activity in 2,2-diphenyl-1-picryl-hydrazyl-hydrate and thiobarbituric acid reactive substances assays (IC > 100 µM). However, compound ( 2) showed anti-inflammation activity through inhibiting interleukin 6 and tumor necrosis factor alpha production ( P < 0.05). Compound ( 3) also exhibited cytokine modulating activities such as inhibiting tumor necrosis factor alpha, activating interleukin 10 at concentration of 10 µM ( P < 0.05). The interleukin 6 cytokine level was also up or down-regulated by compound ( 3) at two time points; 24 and 48 h. This activeness of compound ( 3) might induce hepatoprotection in the acute-phase response by activating the signal transducer and activator of transcription 3(STAT3) through cytokine modulation. Together with other kaempferol glycosides, this new derivative compound may mediate the liver-protective activity of the Vietnamese medicinal plant Phyllanthus acidus. [ABSTRACT FROM AUTHOR]

Aim: The present study aimed to investigate toxicity and oral glucose tolerance test (OGTT) of Phyllanthus acidus leaf extract (PAE) on Wistar rat. Methods: PAE was prepared and administered orally to experimental animals used. The extract was tested for toxicity in rats at a dose of 0, 1,000, 1,500 and 2,000 mg/kg body weight p.o once daily for 14 days. The hypoglycemic effects of PAE on normal rats and orally glucose-induced hyperglycemic rats were compared with distilled water and glibenclamide. A single dose (250 mg/kg body weight) of PAE was administered and blood glucose level was obtained by pricking the tail vain using glucometer at time -30, 0, 30, 60, 120 and 240 minutes. Results: All doses of the extract did not exert any sign or symptom of toxicity and the dead rat was not found. The body weight, white blood cell (WBC), mean corpuscular volume (MCV), platelet (PLT), plateletcrit (PCT), mean platelet volume (MPV), platelet distribution width (PDW), blood chemistry, blood urea nitrogen (BUN), creatinine, alkaling phosphatase (ALP) and organ weight of liver were not significantly different between control and treated rats. However, red blood cell (RBC), hematocrit (HCT), lymphocyte (LYM), and hemoglobin (Hb) at a dose 1,500 mg./kg body weight were significantly lower than those in the control group. The blood glucose levels of PAE treated groups were not different with control and Glybenclamide treated. Conclusion: The findings of the present study can be concluded that the PAE are practically non-toxic at a lower dose. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Leaves of Phyllanthus acidus (PA) have been used in Thai traditional medicine for the treatment of hypertension. We have previously shown that chronic treatment of a PA water extract to middle-aged male rats caused a lowering of the body and serum lipids, two of the parameters that are implicated in cardiovascular disease. Aim of the study To investigate if chronic treatment of middle-aged male rats with a PA water extract affected the perivascular (aortic) adipose tissue (PVAT) and/or their vascular functions Materials and methods Fresh leaves of PA were extracted with water and orally gavaged to the middle-aged male rats for 6 weeks. Vascular functions were studied in vitro using isolated thoracic aorta with and without PVAT, and mesenteric rings in Krebs Heinseleit solution with results recorded with a Polygraph or a Myograph system. The amount of blood vessel eNOS and CSE (cystathionine-γ-lyase) expression was measured by Western blotting. Results PA treatment caused a lower maximal contractile response to phenylephrine (Phe) of the endothelium-intact aortic ring than that of the control group. This effect was abolished by N G -nitro- l -arginine ( l -NA) or by denudation of the endothelium. dl -propargylglycine (PAG, H 2 S inhibitor) and TEA (Ca 2+ -activated K + channel blocker), but not glybenclamide (ATP-activated K + channel blocker), caused a similar increase in the baseline of the endothelium-intact aortic ring in the presence of l -NA in both the PA-treated and control aortic rings. This effect sequentially resulted in a greater contractile response of the aortic rings of both groups to Phe. Glybenclamide also caused a similar increase in the maximal contraction of the endothelium-intact blood vessels with l -NA to both groups. PAG, TEA or glybenclamide did not modify the phenylephrine C–R curves for either group of the PVAT-endothelium-intact aortic rings preincubated with l -NA. The CSE levels of the thoracic aorta and at the PVAT were not different between the PA-treated and the control group. Relaxation of the Phe-precontracted thoracic aortic ring to acetylcholine, but not to glyceryl trinitrate, was higher for the PA-treated than for the control aortic rings and this effect was abolished by l -NA. The mesenteric rings of the PA treated group showed a lower sensitivity on the contractile response to Phe than that of the control group, and this effect was abolished by l -NA. Vasodilatation to acetylcholine, but not to glyceryl trinitrate, of the PA treated-mesenteric ring was more sensitive than that of the control group and this effect was abolished by l -NA. The expression of eNOS by the PA treated thoracic aorta and the mesenteric arteries was higher than the control group. These results demonstrated that chronic treatment with a PA water extract to middle-aged rats affected their vascular functions by increasing the nitric oxide production from the endothelial cells and also modulated the responsiveness of the thoracic aortic- and mesenteric rings to phenylephrine and acetylcholine. [ABSTRACT FROM AUTHOR]

Background: Alzheimer's disease (AD) is a progressive neurodegenerative disorder clinically characterized by loss of memory and cognition. Cholinergic deficit and oxidative stress have been implicated in the pathogenesis of AD. Therefore, inhibition of acetylcholinesterase and oxidation are the two promising strategies in the development of drug for AD. Phyllanthus acidus, belonging to the family Euphorbiaceae, is a tree and has been used in traditional medicine to treat several pain, inflammatory and oxidative stress related disorders such as rheumatism, bronchitis, asthma, respiratory disorder, also important to promote intellect and enhance memory, thus supporting its possible anti-Alzheimer's properties. In this study, P. acidus was evaluated for its cholinesterase inhibitory and antioxidant activities. Methods: In this study, we evaluated the antioxidant potential and neuroprotective activity of P. acidus by assessing total phenol content (FCR assay), total flavonoid content, total antioxidant capacity, Fe3+ reducing power capacity, DPPH (2, 2-diphenyl-1-picrylhydrazyl) and hydroxyl radical scavenging capacity, lipid peroxidation inhibition activity & metal chelating activity. In addition acetylcholinestrase (AChE) and butyrylcholinestrase (BChE) inhibitory activities were performed using Ellman's method. Results: Total phenolic content and total flavonoid content of the extract were 116.98 mg of gallic acid equivalent and 168.24 mg of quercetin equivalent per gm of dried extract. The methanolic extract of P. acidus (MEPA) showed considerable total antioxidant activity and reducing capacity. In DPPH scavenging assay and hydroxyl radical scavenging assay, the MEPA showed 84.33 % and 77.21 % scavenging having IC50 of 15.62 and 59.74 µg/ml respectively. In lipid peroxidation inhibition activity MEPA showed moderate inhibition of peroxidation at all concentrations with IC50 value of 471.63 µg/ml and exhibited metal chelating activity with IC50 value 308.67 µg/ml. The MEPA exhibited inhibition of rat brain acetylcholinesterase and human blood butyrylcholinesterase in a dose dependent manner and the IC50 value was found to be 1009.87 µg/ml and 449.51 µg/ml respectively. Conclusion: These results of the present study reveal that MEPA has considerable amount of antioxidant activity as well as anti-acetylcholinesterase and anti-butyrylcholinesterase activity which suggest its effectiveness against Alzheimer's disease and other neurodegenerative disorders. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Phyllanthus acidus (L.) Skeels (Phyllanthaceae) has traditionally been used to treat gastric trouble, rheumatism, bronchitis, asthma, respiratory disorders, and hepatitis. Despite this widespread use, the pharmacological activities of this plant and their molecular mechanisms are poorly understood. Therefore, we evaluated the immunopharmacological activities of the methanolic extract of the aerial parts of this plant (Pa-ME) and validated its pharmacological targets. Materials and methods Lipopolysaccharide (LPS)-treated macrophages, an HCl/EtOH-induced gastritis model, and an acetic acid-injected capillary permeability mouse model were employed to evaluate the anti-inflammatory activity of Pa-ME. Potentially active anti-inflammatory components of this extract were identified by HPLC. The molecular mechanisms of the anti-inflammatory activity were studied by kinase assays, reporter gene assays, immunoprecipitation analysis, and overexpression of target enzymes. Results Pa-ME suppressed the production of nitric oxide (NO) and prostaglandin E 2 (PGE 2 ) and prevented morphological changes in LPS-treated RAW264.7 cells. Moreover, both HCl/EtOH-induced gastric damage and acetic acid-triggered vascular permeability were restored by orally administered Pa-ME. Furthermore, this extract downregulated the expression of inducible NO synthase (iNOS) and cyclooxygenase (COX)-2 and reduced the nuclear levels of NF-κB. Signalling events upstream of NF-κB translocation, such as phosphorylation of Src and Syk and formation of Src/Syk signalling complexes, were also inhibited by Pa-ME. The enzymatic activities of Src and Syk were also suppressed by Pa-ME. Moreover, Src-induced and Syk-induced luciferase activity and p85/Akt phosphorylation were also inhibited by Pa-ME. Of the identified flavonoids, kaempferol and quercetin were revealed as partially active anti-inflammatory components in Pa-ME. Conclusion Pa-ME exerts anti-inflammatory activity in vitro and in vivo by suppressing Src, Syk, and their downstream transcription factor, NF-κB. [ABSTRACT FROM AUTHOR]

Cubic ZrO 2 : Fe 3+ (0.5–4 mol%) nanoparticles (NPs) were synthesized via bio-inspired, inexpensive and simple route using Phyllanthus acidus as fuel. PXRD, SEM, TEM, FTIR, UV absorption and PL studies were performed to ascertain the formation of NPs. Rietveld analysis confirmed the formation of cubic structure. The influence of Fe 3+ on the structure, morphology, UV absorption, PL emission and photocatalytic activity of NPs were investigated. The CIE chromaticity coordinates (0.36, 0.41) show that NPs could be a promising candidate for white LEDs. The influence of Fe 3+ on ZrO 2 matrix for photocatalytic degradation of AO7 was evaluated under UVA and Sunlight irradiation. The enhanced photocatalytic activity of spherical shaped ZrO 2 : Fe 3+ (2 mol%) under UVA light was attributed to dopant concentration, crystallite size, narrow band gap, textural properties and capability for reducing the electron–hole pair recombination. The trend of inhibitory effect in the presence of different radical scavengers were followed the order SO 4 2− > Cl − > C 2 H 5 OH > HCO 3 − > CO 3 2− . The recycling catalytic ability of the ZrO 2 : Fe 3+ (2 mol%) was also evaluated with a negligible decrease in the degradation efficiency even after the sixth successive run. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Advancing age is associated with an increased accumulation of visceral fat and liver lipid which is then responsible for an age-related risk for cardiovascular disease. Looking after ourselves well with suitable micronutrients could prevent disease or prolong our healthy cardiovascular functions. In Thai traditional medicine, leaves of Phyllanthus acidus (PA) have been used for many purposes including as an antihypertensive agent and to provide relief from a headache caused by hypertension. We aimed to investigate the effects of a chronic oral administration of PA extracts to middle-aged (12-14 months) rats on their body weight, food intake, body fats, liver and kidney functions, fasting blood glucose and lipid profiles, liver lipid accumulation and on blood pressure. Materials and methods Three different kinds of PA extracts were used: (1) a PA water extract, (2) a heated PA water extract, and (3) an n-butanol fraction of the PA water extract, prepared from fresh leaves of Phyllanthus acidus. The rats were orally gavaged with the three PA extracts at 1.0 g/kg body weight or, as a control, with distilled water once a day for 6 weeks. Fasting blood sugar, lipid profile and ALP, SGOT, SGPT, BUN and creatinine levels were measured by enzymatic methods. Liver lipid accumulation was measured using oil red O staining on fresh thin cryostat liver tissue sections. The animal basal blood pressure and heart rate were measured in anesthetized rats via a common carotid artery using a polygraph. Results Results showed that after 6 weeks of treatment using gavaged heated PA extract and PA n-butanol extract there were no changes in any of the parameters studied. However, the initial PA water extract caused a slight decrease in the animal body weight with no change in food intake. No changes were observed in the liver and kidney functions (serum ALP, SGOT, SGPT, BUN and creatinine did not change), nor did the fasting blood sugar or triglyceride levels differ significantly. Serum cholesterol, HDL and LDL levels, as well as visceral and subcutaneous adipose tissue and liver lipid accumulation were significantly decreased compared to that of the control group. There were no differences found in the basal systolic and diastolic blood pressure and the basal heart rate between the PA water extract treatment and the control group. Conclusions These results indicated that the PA water extract had an effect on lipid metabolisms that resulted in a decrease of the serum lipid profile, visceral and subcutaneous fat, as well as on liver lipid accumulation in middle-aged rats. The active component that is responsible for these effects is likely to be a water soluble substance(s) and is heat labile. As a consequence of these beneficial effects of the PA water extract, it would be a good choice for further development for use as a nutraceutical or health product to prevent and/or to slow down the development of obesity and/or cardiovascular disease. [ABSTRACT FROM AUTHOR]

Six diterpenoids including three ent -kauranes (1 – 2 , 4) and three cleistanthanes (3 , 5 – 6) were isolated from the roots and stems of Phyllanthus acidus (L.) Skeels. Of them, (16 S)- ent -16,17,18-tri-hydroxy-19-nor-kaur-4-en-3-one (1), phyllanthone A (2), and 6-hydroxycleistanthol (3) are new compounds, while the ent -kaurane diterpenoids were reported from the titled plant for the first time. Their structures were elucidated on the basis of the extensive spectroscopic analyses. Compounds 2 and 4 – 6 displayed cytotoxic potential with IC 50 values ranging from 1.96 to 29.15 μM. They also showed moderate anti-inflammatory activities (IC 50 = 6.30–12.05 μM). Particularly, the new ent -kaurane 2 displayed cytotoxic potential against HL-60 (IC 50 = 2.00 μM) and MCF-7 (IC 50 = 3.55 μM) cells, and anti-inflammatory activity (IC 50 = 6.47 μM). [Display omitted] [ABSTRACT FROM AUTHOR]

Star gooseberry Phyllanthus acidus (L.) Skeels, lead tree Leucaena leucocephala (Lam.) de Wit. and guava Psidium guajava (L.) are commonly well known plants and have been widely used in folk medicine for the treatment of many diseases in Thailand. Some pharmacological activities of leaf extracts from the plants in animal model of diabetes have been studied. To increase the pharmacological document of the plants, the present study was therefore carried out to investigate hypoglycemic and hypolipidemic properties of leaf extracts from P. acidus, L. leucocephala and P. guajava. The extracts at a dose of 250 mg/kg were administered to streptozotocin (65 mg/kg)-induced diabetic rats orally and daily for eight weeks. Blood glucose level, body weight, hematological values, lipid profiles, blood chemistry, and serum insulin in the rats were examined. Antioxidant activity of the extracts was also assessed by using l,l-diphenyl-2-picryl-hydrazyl (DPPH) radical scavenging assay. Moreover, to see whether the extracts have acute toxicity, once oral administration of the extracts at a dose of 1000, 1500 and 2000 mg/kg was performed in healthy rats. The results revealed that the extracts significantly (p<0.05) decreased blood glucose level, total cholesterol (TC), triglyceride, (TG), low density lipoprotein (LDL), blood urea nitrogen (BUN), and creatinine but increased high density lipoprotein (HDL) and serum insulin in the diabetic treated rats. However, hematological values including white blood cell (WBC), red blood cell (RBC), hemoglobin (Hb), hematocrit (Hct) in both normal and diabetic rats were not affected by the extracts. DPPH assay revealed that the leaf extracts from P. acidus, L. leucocephala and P. guajava possessed the antioxidant activity with EC50 values of 232.37+15.27, 296.10+16.40 and 39.40+3.82 ¿ig/ml respectively which was less potent than ascorbic acid (1.48+0.86 ¿ig/ml). Moreover, the extracts at a dose up to 2000 mg/kg did not exhibit sign of acute toxicity as well as mortality of the rats within a period of observation. These findings indicate that the leaf extracts from P. acidus, L. leucocephala and P. guajava possess hypoglycemic and hypolipidemic activities. The activities seem to relate to hyperinsulinemia and antioxidant activities. Utilization of the extracts is safe with LD50>2000 mg/kg. Furthermore, the leaf extract from P. guajava is to be the most effective extract in the study. [ABSTRACT FROM AUTHOR]

Pollen from staminate flowers and pistillate flowers with 'staminodes' of Phyllanthus acidus Skeels were analyzed under scanning electron microscopy, and tests of pollen viability and in vitro germination were carried out to verify possible similarities between the three types of flowers. The results show that pistillate flowers with 'staminodes' are bisexual, indicating the occurrence of trimonoecy in this species. [ABSTRACT FROM AUTHOR]

The present study was under taken to investigate the biochemical characterization of Phyllanthus acidus, Phyllanthus emblica and Citrus limon. The results suggest that among the three varieties the level of storage polysaccharides (Total Carbohydrate & Starch) and total protein seems to be higher in Phyllanthus emblica than phyllanthus acidus and citrus limon. The amount of cholesterol in Phyllanthus acidus showed better level than the rest of the two varieties. When compared to Phyllanthus acidus and Phyllanthus emblica, the ascorbic acid content was found to be higher in Citrus limon. Phyllanthus emblica contain high amount of calcium than the other two varieties. The amount of phosphorous and iron in Citrus limon posses better level than phyllanthus acidus and emblica. Thereby to conclude the fruits selected Phyllanthus acidus, Phyllanthus emblica and Citrus limon varieties showed very impressive biochemical components which is of therapeutic and economic importance. [ABSTRACT FROM AUTHOR]

Abstract: Objective: To investigate and compare the hepatoprotective effects of crude ethanolic and aqueous extracts of Phyllanthus acidus (L.) Skeels (P. acidus) leaves on acetaminophen (APAP) and thioacetamide (TAA) induced liver toxicity in wistar rats. Silymarin was the reference hepatoprotective agent. Methods: In two different sets of experiments, the P. acidus extracts (200 and 400 mg/kg, body weight) and silymarin (100 mg/kg, body weight) were given orally for 7 days and a single dose of APAP (2 g/kg, per oral) or TAA (100 mg/kg, subcutaneous) were given to rats. The level of serum aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP), total bilirubin and total protein were monitored to assess hepatotoxicity and hepatoprotection. Results: APAP or TAA administration caused severe hepatic damage in rats as evident from significant rise in serum AST, ALT, ALP, total bilirubin and concurrent depletion in total serum protein. The P. acidus extracts and silymarin prevented the toxic effects of APAP or TAA on the above serum parameters indicating the hepatoprotective action. The aqueous extract was found to be more potent than the corresponding ethanolic extract against both toxicants. The phenolic and flavonoid content (175.02±4.35 and 74.68±1.28, respectively) and 2,2-diphenyl-1-picrylhydrazil (DPPH) [IC50 = (33.2±0.31)μg/mL] scavenging potential was found maximum with aqueous extract as compared to ethanolic extract. Conclusions: The results of present study suggests that the aqueous extract of P. acidus leaves has significant hepatoprotective activity on APAP and TAA induced hepatotoxicity, which might be associate with its high phenolic and flavonoid content and antioxidant properties. [Copyright &y& Elsevier]

Abstract: We aimed to investigate the effects, identify the active substances and establish the mechanisms involved in the hypotensive activity of an n-butanol extract from leaves of Phyllanthus acidus (PA extract). PA extract caused a decrease in blood pressure of anesthetized rats that was not modified by atropine or propranolol. PA extract caused a persistent dilatation of thoracic aortic rings preconstricted with either phenylephrine or KCl, and these effects were not modified by LNA or removal of the vascular endothelium. For phenylephrine-preconstricted aortic rings, the dilatory activity of the PA extract was not modified by atropine, propranolol or indomethacin. TEA, glybenclamide or ODQ significantly inhibited the dilatory activity of the PA extract on endothelium-denuded aortic rings. Nifedipine or a Ca2+-free medium depressed the aortic rings constrictor response to phenylephrine, and that was further augmented by the PA extract. Adenosine, 4-hydroxybenzoic acid, caffeic acid, hypogallic acid, and kaempferol were isolated from the PA extract. Each caused a decrease in blood pressure and dilatation of the aortic rings. LNA or removal of the endothelium reduced this activity. ODQ and TEA attenuated the vasodilatory activity of adenosine whereas glybenclamide and ODQ attenuated the effect of hypogallic acid. These results suggest that the hypotensive activities of the PA extract is likely the result of the direct action of these five compounds on the blood vessels by stimulating release of nitric oxide from the vascular endothelium, in part through stimulation of soluble guanylate cyclase, and opening of KATP and KCa channels in the vascular smooth muscle. [ABSTRACT FROM AUTHOR]

[Display omitted] • Four new rare dichapetalins (1–4) were isolated from Phyllanthus acidus. • Their structures were elucidated by extensive spectroscopic data and X-ray diffraction analysis. • The isolated dichapetalins showed cytotoxicity against seven human cancer or normal cell lines. The young leaves of Phyllanthus acidus (Euphorbiaceae) are commonly used as edible vegetables in Indonesia, Thailand, and India, and their water infusions as dieting aids for people trying to remain slim. However, it is regarded as a poisonous plant in Malaya, and current researches are insufficient to provide a conclusion on its toxicity and safety under large doses. In this study, we firstly found that the refined nonpolar extracts of P. acidus leaves showed significant cytotoxic effect against BEAS-2B and L02 normal cell lines with IC 50 values of 2.15 and 1.64 mg/mL, respectively. Further bioactivity-guided isolation produced four new rare dichapetalins (pacidusins A – D) from the most active fraction. Their structures including absolute configurations were elucidated by extensive spectroscopic data and X-ray diffraction analysis. All the isolated dichapetalins exhibited moderate cytotoxicity against, BEAS-2B and L02 normal cell lines with IC 50 values ranging from 12.44 to 22.55 μM, as well as five human cancer cell lines with IC 50 values ranging from 3.38 to 22.38 μM. Furthermore, the content of the main dichapetalins in the leaves were determined by analytical HPLC, which showed that the leaves contained a very high amount of the four isolated dichapetalins with a total yield of 0.488 mg/g of dry plant material. These toxic dichapetalins may lead to adverse health effects in higher doses. Our findings indicate that the dichapetalin containing leaves may not be suitable for consumption in large quantities as food, but demonstrate their potency as anti-cancer agents for new drug discovery. [ABSTRACT FROM AUTHOR]

Four new ent -cleistanthane type diterpenoids, phyacioids A–D (1 – 4), along with two known analogues (5 and 6) were isolated from the powered twigs and leaves of Phyllanthus acidus. Compound 1 was characterized as the third reported structure that possesses a 4,5- seco -20(10 → 5)- abeo -(ent)-cleistanthane scaffold, and compounds 2 and 3 feature a rare alkynyl group. The structures of 1 – 4 were assigned by spectroscopic data, with their absolute structures being determined through electric circular dichroism (ECD) calculations. Compounds 3 , 5 and 6 showed moderate cytotoxicity with IC 50 values ranging from 13.8 to 36.0 μ M. [Display omitted] • Four novel ent -cleistanthane diterpenoids were isolated from the twigs and leaves of Phyllanthus acidus. • The plausible biosynthetic pathway of compounds 1 – 6 were proposed. • Compounds 3 , 5 and 6 exhibited moderate cytotoxic activity with IC 50 values ranging from 13.8 to 36.0 μ M. [ABSTRACT FROM AUTHOR]

A new norlupane triterpenoid, 29-norlupane-1 β -hydroxy-3,20-dione ( 1 ), along with ten known compounds, 29-norlup-1-ene-3,20-dione ( 2 ), phyllanthol ( 3 ), phyllanthone ( 4 ), glochidone ( 5 ), lupeol ( 6 ), lupeone ( 7 ), 4-hydroxybenzoic acid ( 8 ), 4-hydroxybenzaldehyde ( 9 ), phyllane A ( 10 ) and methyl β -orsellinate ( 11 ) were isolated the twigs and leaves of Phyllanthus acidus . The structure of 1 was identified by interpretation of their spectroscopic data and comparison with those reported in the literature. In addition, all isolated compounds 1-11 were evaluated for their antioxidant activity.

Premature Totapuri mangoes (Mangifera indica L. var. Totupura) often drop during strong winds, while star gooseberry (Phyllanthus acidus) fruits are often underutilized and/or considered as agricultural waste, resulting in the huge loss of agricultural revenue. Thus, the present study aimed to develop new value-added star gooseberry (SGFSS), and Totapuri mango fruit sugar syrup (TMFSS) and evaluated for microbial, nutritional, organoleptic, and functional characteristics. TMFSS displayed higher amount of total sugars (722.66 mg/mL), polyphenols (4.51 ± 0.21 GAE mg/mL), flavonoids (0.48 ± 0.02 QE mg/mL), and tannins (4.87 ± 0.09 TAE mg/mL) and have better antioxidant activity compared to SGFSS. Contrary to this SGFSS have a higher amount for minerals (11287.55 ± 13.39 mg/L) and yeasts and molds (2.97 ± 0.03 Log CFU/mL). Both TMFSS and SGFSS possess diverse volatile compounds and are free form pathogenic microorganisms with an acceptable amount of biogenic amines 38.60 ± 0.06 mg/L and 45.31 ± 0.83 mg/L, respectively. Furthermore, 1:5 and 1:3 dilution of TMFSS and SGFSS displayed high hedonic scores for color, aroma, and flavor. The findings collectively suggest the effective preparation of TMFSS and SGFSS that may deliver significant nutrition and value, counteracting the issues of malnutrition and revenue loss. • Fruit sugar syrup with added value was developed from agricultural waste. • Fruit sugar syrup properties depend on raw material and microbial fermentation. • Fruit sugar syrup has vital minerals and bioactive compounds, low biogenic amines. • Diluted fruit sugar syrup has good hedonic scores for aroma, color, and flavor. • Fruit sugar syrup has antimicrobial, antioxidant, and antiproliferative potential. [ABSTRACT FROM AUTHOR]

Phytochemical investigation on the nonpolar extracts of P. acidus leaves afforded three new cleistanthane diterpenoids, named phyllanacidins A–C (1 – 3), in addition to three known ones (4 – 6). Among them, compounds 2 and 3 represent the first examples of 17- nor cleistanthane diterpenoids. Their structures including absolute configurations were elucidated on the basis of extensive spectroscopic data and single crystal X-ray diffraction analysis. All the isolated cleistanthane diterpenoids were evaluated for their cytotoxic activities against five human cancer cell lines. Compounds 4 – 6 exhibited moderate cytotoxicity with IC 50 values ranging from 16.11 to 30.82 μM. Unlabelled Image • Three new cleistanthane diterpenoids (1 – 3) were isolated from Phyllanthus acidus. • Their structures were elucidated on the basis of spectroscopic analysis. • 2 and 3 represent the first examples of 17- nor cleistanthane diterpenoids. [ABSTRACT FROM AUTHOR]

Phyllanthus acidus L. (jimbilin), a species within the Phyllanthaceae family has origins in Madagascar. The tree is now established as a native of the South American countries of Colombia and Brazil with wide distribution within tropical and sub-tropical countries. The fruit which is tart in taste has a greenish yellow exterior and a white to cream colored fleshy interior covering a pit of seeds. Studies have revealed that plant extracts exhibit medicinal properties. This paper reviews the nutritional and medicinal properties of the plant and its commercial applications. [ABSTRACT FROM AUTHOR]

• The multi-platform metabolomics was applied to discriminate P. acidus extracts. • The tested bioactivities showed the potency of 50% ethanol extract. • The PLS was performed to correlate bioactivities with metabolites of P. acidus. • The MS and NMR correlation identified chemical markers of P. acidus. Proton nuclear magnetic resonance (1H NMR)- and ultra-high performance liquid chromatography-mass spectrometry (UHPLC-MS)-based analytical tools are frequently used in metabolomics studies. These complementary metabolomics platforms were applied to identify and quantify the metabolites in Phyllanthus acidus extracted with different ethanol concentrations. In total, 38 metabolites were tentatively identified by 1H NMR and 39 via UHPLC-MS, including 30 compounds are reported for the first time from this plant. The partial least square analysis (PLS) revealed the metabolites that contributed to α-glucosidase and nitric oxide (NO) inhibitory activities, including kaempferol, quercetin, myricetin, phyllanthusol A, phyllanthusol B, chlorogenic, catechin, cinnamic coumaric, caffeic, quinic, citric, ellagic and malic acids. This study shows the significance of combining 1H NMR- and UHPLC-MS-based metabolomics as the best strategies in identifying metabolites in P. acidus extracts and establishing an extract with potent antioxidant, anti-diabetic, and anti-inflammatory properties. [ABSTRACT FROM AUTHOR]

The norbisabolane-type sesquiterpenoids bearing a spiroketal functionality have been found in Phyllanthus spp. and showed anti-HBV activities. As part of an ongoing effort to search for promising anti-HBV sesquiterpenes from Phyllanthus plants, we report four new norbisabolane-type sesquiterpenoids, phyacidusin A (1), phyacidusin B (2), phllanthacidoid A1 (3) and phllanthacidoid N1 (4), from stem of P. acidus collected in Xishuangbanna, Yunnan province, China. The absolute configuration of new compounds was established by coupling constants and ROESY correlations, as well as comparation of NMR data with those of known compounds. The absolute configuration of new compounds 1 and 2 was further confirmed by X-ray diffraction. Compound 2 showed effect to HBsAg with an IC 50 value of 11.2 ± 0.01 μM, while compound 3 inhibited HBeAg secretion with an IC 50 value of 57.1 ± 0.02 μM. The results enriched the diversity of anti-HBV norbisabolane sesquiterpenes. Unlabelled Image [ABSTRACT FROM AUTHOR]