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Cytotoxic constituents from Plumbago zeylanica

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Abstract

The bioassay-guided fractionation of the dichloromethane extract of aerial parts of Plumbago zeylanica led to the isolation of beta-sitosterol, beta-sitosteryl-3beta-glucopyranoside, beta-sitosteryl-3beta-glucopyranoside-6'-O-palmitate (1), lupenone, lupeol acetate, plumbagin and trilinolein. Compound 1 showed cytotoxic activity against MCF7 and Bowes cancer cell lines (IC50 113 microM and 152 microM, respectively), beta-sitosterol inhibited Bowes cell growth (IC50 36.5 microM) and plumbagin was cytotoxic against MCF7 and Bowes cells (IC50 1.28 microM and 1.39 microM, respectively). Cytotoxic constituents from Plumbago zeylanica. Available from: https://www.researchgate.net/publication/8448995_Cytotoxic_constituents_from_Plumbago_zeylanica [accessed Apr 6, 2015].

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... Hydroplumbagin glucoside [80] β-sitosteryl glucoside [83] 3'-O-β-glucopyranosyl plumbagic acid [33] ...
... Linoleic acid [67] Palmitic acid [67] Trilinolein [83] Nonyl nonanoate [56] Nonyl 8-methyl-dodec-7-enoate [56] Hentriacontane [65] 1,2-Benzenedicarboxylic acid [50] Diisooctyl phthalate [50] Gugultetrol-18-ferrulate [65] Vanillic acid [68] ...
... All parts of the plant are used, but the roots have tremendous pharmacological properties. The pulped roots or aerial parts are reported abortifacient, while powdered bark, root or leaves are used to treat gonorrhea, syphilis, tuberculosis, rheumatic pain, swellings, wound healing [87] dyspepsia, piles, diarrhoea, skin diseases, leprosy and also reported to possess antibacterial, antifungal [88] , cantharides [83] . The pharmacological importance of this perennial shrub lies in its ability to produce a napthoquinone, called plumbagin [89] . ...
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Plumbagin is the most common and broad spectrum phytochemical of P. zeylanica. The leaves and root bark contains plumbagin. The root yield new pigments, viz, 3-chloroplumbagin, 3, 3-biplumbagin, binaphthoquinone identify as 3', 6'-biplumbagin, and four other pigments identify as isozeylanone, zeylanone, elliptinone, and droserone. The isolation of plumbagin, droserone, isoshinanolone and a new napthalenone i.e., 1, 2 (3)-tetrahydro-3, 3'-plumbagin is reported from the phenolic fraction of the light petrol extract of the roots. Two plumbagic acid glucosides; 3'o-beta-glucopyranosyl plumbagic acid and 3'-o-beta-glucopyranosyl plumbagic acid methyl ester along with five naphthaquinones. All parts of the plant are used, but the roots have tremendous pharmacological properties. The pulped roots or aerial parts are reported abortifacient, while powdered bark, root or leaves are used to treat gonorrhoea, syphilis, tuberculosis, rheumatic pain, swellings, wound healing dyspepsia, piles, diarrhoea, skin diseases, leprosy and also reported to possess antibacterial, antifungal, and cantharides.
... The pharmacological properties of C. dichotoma have been described since ancient times. It possesses antimicrobial 10 , antioxidant, analgesic, antiinflammatory 5, 6 , hepatoprotective, aphrodisiac, diuretic, expectorant, laxative, antifertility 2 , anticancer 4,8,14 and anthelmintic activity 18 . ...
... Moreover, these phytoconstituents might cause certain toxic effects in the development or normal functioning of the reproductive system. Coumarin, flavonoid and sitosterol 8,14 are phytoconstituents that have been related to the occurrence of certain adverse effects to the reproductive system and hence possess a potent antifertility activity. Flavonoids like quercitin, apigenin 2,5 , luteolin 2,5 and β-sitosterol 8,14 are the active constituents of this plant that suggests the possible antifertility activity in female rats. ...
... Coumarin, flavonoid and sitosterol 8,14 are phytoconstituents that have been related to the occurrence of certain adverse effects to the reproductive system and hence possess a potent antifertility activity. Flavonoids like quercitin, apigenin 2,5 , luteolin 2,5 and β-sitosterol 8,14 are the active constituents of this plant that suggests the possible antifertility activity in female rats. ...
Article
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The use of phytoconstituents single or combined with standard medicines has been utilized in cure of different diseases. Many plants of genus Cordia comprise of trees and shrubs are widely distributed in warmer regions and have been utilized in management of various diseases. Various phytoconstituents like flavonoids, alkaloids, terpenes, tannins, and glyceridess having different activities were screened and isolated from different parts of C. dichotoma. Various important Pharmacological properties including Antiulcer, Contraceptives, anti-inflammatory, anthelmintic, analgesic, anticancer, Antioxidant, antimicrobial, hepatoprotective, antidiabetic and others have been well documented for this plant. Therefore, we have briefly reviewed the various bioactivities of C. dichotoma to improve our knowledge on plant phytochemicals as therapeutic entities. The present review describes the various phytoconstituents and therapeutic potential of C. dichotoma that can be followed for future research on this plant for human health benefits. Keywords: Cordia Dichotoma, phytoconstituents, Antioxidant, Antimicrobial, Antifertility, Traditional medicine
... β-sitosterol from P. zeylanica showed cytotoxic activity on the human melanoma cell line (Bowes cells). Plumbagin β-sitosteryl-3β-glucopyranoside-6'-O palmitate showed cytotoxic activity on both human cell lines MCF7 (Breast cancer cells) and bowes melanoma cells 26 . Plumbagin suppressed growth of Raji (erythroleukemia), Calu-1 (human lung carcinoma cell line), Hela (human cervical carcinoma cell line) and Wish (transformed epithelial cell line) tumor cell lines 23 . ...
... Cytotoxic activity of bsitosteryl-3b-glucopyranoside-ad-O-palmitate from P. zeylanica was observed against MCF7 and Bowes cancer cell lines. b-Sitosterol inhibited Bowes cell growth and plumbagin was cytotoxic against MCF7 and Bowes cells 26 . Plumbagin was found to be a potential novel agent in the control of hormone-refractory prostate cancer which is the second leading cause of cancer-related deaths in men 56 . ...
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From ancient times of vedas, charaksamhita and sushrutsamhita, to modern day developments and research in medicine, the medicinal importance of Chitraka (Plumbago zeylanica) as a wonderful Indian remedy has been upheld through the test of time. Chitraka is used in ayurveda for relief from many ailments, especially digestive disorders, bronchitis, diseases of liver, leucoderma, inflammation, piles, itching, laryngitis, rheumatism, diseases of spleen, many skin disorders etc. The root extracts of P. zeylanica have been incorporated in various Indian indigenous ayurvedic drug formulations. This paper reviews various aspects of Chitraka like different pharmacological activities, medicinal properties including wound healing, antioxidant, antiulcer, anticancer, leishmanicidal, antifertility, antimalarial, antidiabetic, hypolipidemic, trypanocidal, antibacterial, antifungal, antiviral, anti-inflammatory, antimutagenic, anti-allergic, larvicidal, insecticidal and anxiolytic activities. P. zeylanica plant contains naphthoquinones, flavonoids, terpenes, alkaloids, glycosides, steroids, triterpenoids, tannins, phenolic compounds, glucopyranoside, sitosterol saponins, coumarins, carbohydrates, fixed oils, fats and proteins having a wide variety of bioactivities. The important compound responsible for bioactivity is plumbagin which is chemically 5-hydroxy-2-methyl-1,4-naphthoquinone. Studies of P. zeylanica roots resulted in identification of plumbagin and lawsone as an active principle exhibiting the plasmid elimination activity. Due to the toxicity of chemical curing agents like acridine orange or ethidium bromide, there is a constant need of developing novel curing agents which are more effective and at the same time their non- toxic nature. Bacterial strains resistant to multiple antibiotics have emerged to which the invention of new antibiotics has failed to match up. The effects of antibiotic resistance are serious with mortality and morbidity constantly on the rise. Therefore P. zeylanica root extracts containing lawsone and plumbagin would have great potential as drugs of choice in the treatment of antibiotic resistant bacterial strains. The already ineffective antibiotic therapy can be made effective by converting antibiotic resistant bacteria into sensitive ones. The present review for the first time depicts the use of P. zeylanica as antimicrobial and plasmid curing agent in medicinal formulations and it is a novel approach towards the spread of antibiotic resistance especially in the hospital environment.
... The CH 2 Cl 2 :MeOH extract of the aerial parts of S. lateriflorum displayed activity against a panel of cancer cell lines and also showed antiinflammatory activity in the mouse ear edema model induced by TPA. Chromatographic procedures applied to this extract allowed the isolation of an undescribed pentacyclic triterpene (1) and nine known compounds identified as 3β-palmitoyloxy olean-12-ene (2) [14], lupeyl palmitate (3) [15], lupeyl acetate (4) [16], 3β-palmitoyloxy-11-oxoolean-12-ene (5) [17], cycloeucalenol (6) [18], β-sitosterol (7) [19], stigmasterol (8) [20], 6´-O-palmitoyl 3-O-β-sitosteryl-β-D-glucopyranoside (9) [21] and 3-O-β-sitosteryl-β-D-glucopyranoside (10) [22], as determined by comparison with observed and reported data (Fig. 1). ...
... Fraction G (13.4 g) was chromatographed over a silica gel eluted with a gradient of n-hexane-ethyl acetate mixtures and acetone, to yield six pooled fractions (GF1-GF6). Fraction GF4 was further chromatographed over a silica gel column with a gradient of n-hexane-acetone, to yield 6´-O-palmitoyl 3-O-β-sitosteryl-β-D-glucopyranoside (9)[21] as an amorphous solid (29.7 mg). 3-O-β-Sitosteryl-β-D-glucopyranoside (10)[22] (35.0 mg) was isolated from fraction GF5 as an amorphous solid which was precipitated from a mixture of n-hexane-acetone-ethyl acetate, and finally washed with cold n-hexane.4.4. ...
Article
Ten compounds, including a new anti-inflammatory acyl triterpene, 3β-palmitoyloxy-1β,11α-dihydroxy-olean-12-ene, were isolated from the bioactive organic extract prepared from the leaves of Sapium lateriflorum (syn: S. nitidum). The isolated compounds were screened for their cytotoxic activity against selected human cancer cell lines and did not display significant activity. They were also evaluated as anti-inflammatory agents in mouse models (TPA-induced edema in the ear and in a carrageenan-induced paw edema model). The results indicated that the new compound, 3β-palmitoyloxy-1β,11α-dihydroxy-olean-12-ene, was the compound with major anti-inflammatory activity similar to that of indomethacin, being the hydroxyl at C-11 important for the observed activity. The results of docking studies of the 3β-palmitoyloxy esters of olean-12-ene with NF-κB and with COX-2 receptors were consistent with possible molecular mechanisms of the anti-inflammatory activity.
... β-sitosterol from P. zeylanica showed cytotoxic activity on the human melanoma cell line (Bowes cells). Plumbagin β-sitosteryl-3β-glucopyranoside-6'-O palmitate showed cytotoxic activity on both human cell lines MCF7 (Breast cancer cells) and bowes melanoma cells 26 . Plumbagin suppressed growth of Raji (erythroleukemia), Calu-1 (human lung carcinoma cell line), Hela (human cervical carcinoma cell line) and Wish (transformed epithelial cell line) tumor cell lines 23 . ...
... Cytotoxic activity of bsitosteryl-3b-glucopyranoside-ad-O-palmitate from P. zeylanica was observed against MCF7 and Bowes cancer cell lines. b-Sitosterol inhibited Bowes cell growth and plumbagin was cytotoxic against MCF7 and Bowes cells 26 . Plumbagin was found to be a potential novel agent in the control of hormone-refractory prostate cancer which is the second leading cause of cancer-related deaths in men 56 . ...
... Accordingly, the structure and relative configuration of 4 was established as shown. The known compounds were identified as (1'E,3'S,4'S,5'E)-2-(3',4'-dihydroxy-1',5'-heptadienyl)-6-hydroxybenzaldehyde (5) [16], (1'E,3'S,4'R,5'E)-2-(3',4'-dihydroxy-1',5'-heptadienyl)-6-hydroxy benzaldehyde (6) [17], (5'R,6'S)-pyriculariol (7) [18], (5'S,6'R)-pyriculariol (8) [18], dihydropyriculol (9) [7], epi-dihydropyriculol (10) [7], pyriculin A (11) [19], (R)-pyricuol (12) [20], (1'E,3'R,4'E)-2-hydroxymethyl-3-(3'-hydroxymethylhexa-1',4'-dienyl)phenol (13) [21], 1,3-dihydro-4-isobenzofuranol (14) [22], 4-hydroxyphthalide (15) [23], (−)-isosclerone (16) [24], bis (2-ethylhexyl) phthalate (17) [25], daucosterol palmitate (18) [26] and 5α,6β-dihydroxydaucosterol (19) [27] by comparison of their experimental and reported spectroscopic data. ...
... The fungal strain of Magnaporthe grisea M639 used in this study was isolated from the leaf spot lesions of rice collected from Yunnan province, China, in August 2012. The strain has been preserved The known compounds were identified as (1'E,3'S,4'S,5'E)-2-(3',4'-dihydroxy-1',5'-heptadienyl)-6-hydroxybenzaldehyde (5) [16], (1'E,3'S,4'R,5'E)-2-(3',4'-dihydroxy-1',5'-heptadienyl)-6-hydroxy benzaldehyde (6) [17], (5'R,6'S)-pyriculariol (7) [18], (5'S,6'R)-pyriculariol (8) [18], dihydropyriculol (9) [7], epi-dihydropyriculol (10) [7], pyriculin A (11) [19], (R)-pyricuol (12) [20], (1'E,3'R,4'E)-2-hydroxymethyl-3-(3'-hydroxymethylhexa-1',4'-dienyl)phenol (13) [21], 1,3-dihydro-4-isobenzo-furanol (14) [22], 4-hydroxyphthalide (15) [23], (−)-isosclerone (16) [24], bis (2-ethylhexyl) phthalate (17) [25], daucosterol palmitate (18) [26] and 5α,6β-dihydroxydaucosterol (19) [27] by comparison of their experimental and reported spectroscopic data. ...
Article
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Magnaporthe grisea is the causal agent of rice blast disease, which is the most serious disease of cultivated rice. Aromatic polyketides are its typical metabolites and are involved in the infection process. In the search for novel lead compounds, chemical investigation of the fungus M. grisea M639 has led to the isolation of four new aromatic polyketides (salicylaldehyde skeleton bearing an unsaturated side chain), griseaketides AD (1-4), as well as 15 known compounds (5-19). The structures of the new compounds were elucidated on the basis of extensive spectroscopic analyses, including HR-MS, 2D NMR. Compound 12 showed prominent activity that killed 94.5% of C. elegans at 400 ppm and 66.9% at 200 ppm over 24 h. This is the first report describing the nematicidal activity of this type aromatic polyketide.
... [23][24] Plumbagin and naphthoquinones, especially 5-hydroxy-1,4-naphthaquinone, are an important group of natural compounds that are very useful for the development of effective pesticides due to their abundance and relatively low toxicity. According to a literature review, Plumbagin from Plumbago zeylanica has many important biological effects, including antibacterial, 25 cytotoxic, 26 antimalarial, 27 antifilarial 28 and antiprotozoal properties. 29 The naphthoquinone skeleton, with its abundant abundance and favourable structural properties, is an excellent model for producing effective feeding suppressants. ...
Article
Abstract In recent years, the overuse of commercially obtainable synthetic pesticides against phytophagous insects has augmented their bioaccumulation in the biosphere, foremost to increased resistance and reduced soil biodiversity. Moreover, extreme uses of insecticides enter various environmental resources as an outcome of overflow, initiating deleterious health problems to agriculturalists and consumers of agricultural products. Hence, more attention is being paid towards the expansion of substitute eco-friendly insecticides that will help in an effective pest management system and also prevent longstanding exposure that causes diseases. As a result, important ecologically friendly and harmless alternative practice strategies to artificial compounds are essential. Azadirachtin and plumbagin (phytoproducts) have been identified as an extraordinary biocontrol agent with low toxicity and high efficacy among many plant products for latent chemotherapeutic compounds in plant pest and disease management systems. The biocidal effectiveness of neem is attributed to its azadirachtin active ingredient, which affect some metabolic processes in insects such as protein synthesis, deviations in biological fitness, reduced sexual communication, and chitin synthesis. Similarly, Plumbagin (Napthaquinones) have established substantial attention in agricultural chemistry because of a novel action mode, extremely high activity against a broad spectrum of insects, low acute toxicity to mammals, and environmentally benign characteristics. The present study indicated that Azadirachtin and Plumbagin can be significant alternatives to Chemical insecticides for Pericallia ricini control in short-cycle crops
... The chemical structures of them were clarified using 1D, 2D NMR, and HRMS experiment data, together with considerable comparison to those of previously published literature. Compounds (2)(3)(4)(5) were firstly reported from the Combretum genus. ...
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Five glycosides, including two steroid glycosides, β-sitosterol 3-O-β-D-glucopyranoside (1), β-sitosterol 3-O-β-D-(6’-O-margaroyl)glucopyranoside (2), two glycerol glycosides, (2S)-1-O-palmitoyl-sn-glycerol 3-O-α-D-(6-sulfo)quinovopyranoside sodium salt (3), (2S)-1,2-O-dipalmitoyl-sn-glycerol 3-O-α-D-(6-sulfo)quinovopyranoside sodium salt (4), and one ethanoid glycoside, ethyl β-D-glucopyranoside (5), were isolated from the ethyl acetate extract of the Combretum trifoliatum leaves. Their chemical structures were characterized using 1D, 2D NMR, and HRMS data, and compared to those of previously reported papers. For the first time, compounds (2-5) were noticed from the Combretum genus.
... Accordingly, 3 J correlations were observed between H-2″ (δ 2.31) and H-3″ (δ 1.61) (Supplementary Materials, Table S6, and Figure S16). Finally, the data generated match with the reported values [58] of β-sitosteryl-3β-glucopyranoside-6′-O-palmitate (4) (Figure 2 Table S7, and Figure S17). Table S7, and Figure S18). ...
Article
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Ziziphus spina-christi (Rhamnaceae family) is a medicinal plant traditionally used to treat dandruf, wounds, hair loss, diarrhea, mastitis, abdominal pain, and gastrointestinal complications. To support this, the present work aims to study the in vitro antibacterial and antioxidant activities of compound isolates from the roots of Ziziphus spina-christi along with their in silico computational analyses. Compounds were isolated on silica gel column chromatography and an agar disc difusion and DPPH radical scavenging assays were employed to study the antibacterial and antioxidant activities, respectively. Te ADME and toxicity properties of the compounds were evaluated using SwissADME and ProTox-II online Web tools, respectively. Conversely, the in silico molecular docking studies were attained via a Biovia Discovery Studio Visualizer 2021 in combination with the AutoDock Vina software. Te silica gel chromatographic separation of the combined CH 2 Cl 2 : CH 3 OH (1 : 1) and CH 3 OH root extracts aforded trimethyl trilinolein (1), stearic acid (2), 13-hydroxyoctadeca-9, 11-dienoic acid (3), β-sitosteryl-3β-glucopyranoside-6′-O-palmitate (4), and stigmasterol (5). Notably, the in vitro antibacterial study revealed the extract and β-sitosteryl-3β-gluco-pyranoside-6′-O-palmitate (4) with the highest inhibitory activities (15.25 ± 0.35 and 14.25 ± 0.35 mm, respectively) against E. coli compared to ciprofoxacin (21.00 ± 0.35 mm) at 2 mg/mL. Te CH 2 Cl 2 : CH 3 OH (1 : 1) extract (IC 50 : 1.51 µg/mL) and β-sitosteryl-3β-glucopyranoside-6′-O-palmitate (4) (IC 50 : 5.41 µg/mL) also exhibited auspicious DPPH scavenging activities, followed by stigmasterol (5) (IC 50 : 6.88 µg/mL) compared to the ascorbic acid standard (IC 50 : 0.46 µg/mL). Te molecular docking analyses unveiled the highest binding afnity by β-sitosteryl-3β-glucopyranoside-6′-O-palmitate (4) (−8.0 kcal/mol) against P. aeruginosa PqsA relative to the ciprofoxacin standard (−8.2 kcal/mol). Furthermore, the organ toxicity predictions showed that all the compounds exhibit no hepatotoxicity and cytotoxicity efects and stigmasterol (5) afords drug-likeness protocols. Overall, the combined experimental and computational investigations of this study support the traditional uses of Ziziphus spina-christi for antibacterial and natural antioxidant applications.
... Accordingly, 3 J correlations were observed between H-2″ (δ 2.31) and H-3″ (δ 1.61) (Supplementary Materials, Table S6, and Figure S16). Finally, the data generated match with the reported values [58] of β-sitosteryl-3β-glucopyranoside-6′-O-palmitate (4) (Figure 2 Table S7, and Figure S18). In agreement with the 13 C NMR spectral data, the DEPT-135 spectrum revealed three sp 2 olefnic carbons, one oxymethine, seven methine, six methyl signals pointing up, and nine methylene signals pointing down (Supplementary Materials, Table S7, and Figure S19 Table S7, and Figure S20). ...
Article
Full-text available
Ziziphus spina-christi (Rhamnaceae family) is a medicinal plant traditionally used to treat dandruff, wounds, hair loss, diarrhea, mastitis, abdominal pain, and gastrointestinal complications. To support this, the present work aims to study the in vitro antibacterial and antioxidant activities of compound isolates from the roots of Ziziphus spina-christi along with their in silico computational analyses. Compounds were isolated on silica gel column chromatography and an agar disc diffusion and DPPH radical scavenging assays were employed to study the antibacterial and antioxidant activities, respectively. The ADME and toxicity properties of the compounds were evaluated using SwissADME and ProTox-II online Web tools, respectively. Conversely, the in silico molecular docking studies were attained via a Biovia Discovery Studio Visualizer 2021 in combination with the AutoDock Vina software. The silica gel chromatographic separation of the combined CH2Cl2 : CH3OH (1 : 1) and CH3OH root extracts afforded trimethyl trilinolein (1), stearic acid (2), 13-hydroxyoctadeca-9, 11-dienoic acid (3), β-sitosteryl-3β-glucopyranoside-6′-O-palmitate (4), and stigmasterol (5). Notably, the in vitro antibacterial study revealed the extract and β-sitosteryl-3β-glucopyranoside-6′-O-palmitate (4) with the highest inhibitory activities (15.25 ± 0.35 and 14.25 ± 0.35 mm, respectively) against E. coli compared to ciprofloxacin (21.00 ± 0.35 mm) at 2 mg/mL. The CH2Cl2 : CH3OH (1 : 1) extract (IC50 : 1.51 µg/mL) and β-sitosteryl-3β-glucopyranoside-6′-O-palmitate (4) (IC50 : 5.41 µg/mL) also exhibited auspicious DPPH scavenging activities, followed by stigmasterol (5) (IC50 : 6.88 µg/mL) compared to the ascorbic acid standard (IC50 : 0.46 µg/mL). The molecular docking analyses unveiled the highest binding affinity by β-sitosteryl-3β-glucopyranoside-6′-O-palmitate (4) (−8.0 kcal/mol) against P. aeruginosa PqsA relative to the ciprofloxacin standard (−8.2 kcal/mol). Furthermore, the organ toxicity predictions showed that all the compounds exhibit no hepatotoxicity and cytotoxicity effects and stigmasterol (5) affords drug-likeness protocols. Overall, the combined experimental and computational investigations of this study support the traditional uses of Ziziphus spina-christi for antibacterial and natural antioxidant applications.
... The HMBC analysis ( Figure S4), particularly the correlations between H-7/C-2, C-6, C-9, C-8′, and C-11′ helped disclose the planar structure of 3 as that of caesalstilbene A, previously isolated from Caesalpinia cucullate (Liang et al. 2019). On the basis of NOE correlations between H-8′/H-2′, 6′; H-7/H-14; H-7′/H-14′, and H-8/H-2, 6 ( Figure S4) and comparison of the calculated and experimental ECD spectra of 3 ( Figure S5), the stereocenters at C-7, C-8, C-7′, C-8′ could be proposed as 7 R,8R,7′ R,8′ R. Compound 3, perfolostilbene, is thus a 7′,8′-di-epimer of caesalstilbene A. By comparison of their 1 H and 13 C NMR spectroscopic data with those previously reported, the 21 known compounds, pallidol (4) (Khan et al. 1986), oxyresveratrol (5) (Wu et al. 2010), resveratrol (6) (Khan et al. 1986;Wu et al. 2010), moracin M (7) (Basnet et al. 1993), scirpucin A (8) (Nakajima et al. 1978;Yang et al. 2005;Wu et al. 2010), scirpucin B (9) (Nakajima et al. 1978;Yang et al. 2005), naringenin (10) (Zhong et al. 2017), thymidine (11) (Breitmaier and Voelter 1989;Yu et al. 2007), 2′-O-ethyluridine (12) (Breitmaier and Voelter 1989), uridine (13) (Guoyou et al. 2005), 2′-deoxyuridine (14) (Breitmaier and Voelter 1989), β-sitosterol glucoside decahexanoate (15) (Kuo et al. 1998;Nguyen et al. 2004), lilioglycoside K (16) (Jin et al. 2002), angulvioside XV (17) (Honbu et al. 2002), methylprotodioscin (18) (Hirai et al. 1986;Sashida et al. 1992;Jin et al. 2002;Huang et al. 2009), protodioscin (19) (Hu et al. 1997;Huang et al. 2009) and psuedoprotodioscin (20) (Sashida et al. 1992;He et al. 2006;Huang et al. 2009), β-sitosterol (21), β-sitosterol glucoside (22), adenosine (23) (Breitmaier and Voelter 1989) and glycerol (24) could be identified. ...
Article
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Three undescribed compounds including two furosteroid glycosides (perfoloside and 22-O-methylperfoloside) and one stilbenedimer (perfolostilbene) together with 21 known compounds were isolated from the roots of Smilax perfoliata. The structural elucidation was established by extensive uses of HRMS, 1D and 2D spectroscopic techniques. The assignment of the stereocenters in perfolostilbene was based on NOESY data and ECD calculation. Among the isolates, two compounds showed marginal cytotoxic activity against KB and Hela cell lines while seven stilbenoids showed strong to weak antiacetylcholinesterase and antibutyrylcholinesterase activities with IC50 ranging between 2-197 µM.
... Due to their efficiency, lack of negative side effects, and affordability, herbal medications are frequently recommended even when the biologically active ingredients are unknown. The useful medical plant Plumbago zeylanica, often known as Plumbago, "white leadwort," "Ceylon leadwort," "Doctorbush," "Chitrak" in India, is used extensively in Africa and Asia to cure comon illnesses [5] . Plumbago zeylanica (Family: Plumbaginaceae) is a therapeutic plant. ...
... It is used for treating diarrhea, dysentery, piles and peptic ulcers. The bioassay-guided fractionation of the dichloromethane extract of aerial parts of Plumbago zeylanica led to the isolation of β-sitosterol, β-sitosteryl-3β-glucopyranoside, β-sitosteryl-3βglucopyranoside-6′-O-palmitate, lupenone, lupeol acetate, plumbagin and trilinolein (Nguyena et al., 2004). Plumbagin modulates cellular proliferation, carcinogenesis, and radioresistance, all known to be regulated by the activation of the transcription factor NF-κB, suggesting plumbagin might affect the NF-κB activation pathway (Santosh et al., 2006). ...
Chapter
According to one of the ancient proverbs in India," there is no plant on earth which has no medicinal property." More than 90% of the compounds used in modern medicine have their origin from plant sources. A large number of plants have been used by man from ancient times as medicine for curing various ailments. In recent times there is an upsurge of interest and focus on the importance of medicinal plants and traditional health systems in solving the health care problems of the world. This article gives an over view and a brief account of the important ethno-medicinal plants used in treating neoplastic diseases.
... Ethyl alcohol extract of C. dichotoma showed cytotoxic action on brine shrimp lethality assay (LC 50 =20 µg/mL) [65]. Cytotoxicity of C. dichotoma leaf methanolic extract on human cervical cancer cell line (HeLa) was evaluated using 4′,6-diamidino-2phenylindole (DAPI) and (3-[4,5-dimethylthiazol-2yl]-2,5 diphenyl tetrazolium bromide) (MTT) staining tests .The results showed that extract with gotten IC 50 of 202 μg/mL, prohibited in vitro proliferation and induced apoptosis of HeLa cell, which signified a powerful anticancer property in comparison to tamoxifen (IC 50 =48 μg/mL) [81,82]. ...
Article
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Genus Cordia has been well acknowledged in tropical and subtropical regions worldwide as traditional medicine, where its folk uses include uses in vital disorders. The current review considers the comparative geographical distribution, macromorphological characters, nutritional properties, phytochemical profile and biological prospective survey of Cordia dichotoma (G. Forst.) and Cordia sebestena (L.), aiming to highlight the pharmacological significance of the two species. Considering their nutritional value, fruits and leaves of Cordia dichotoma are rich in nutritional constituents, while limited data described the nutritional importance of Cordia sebestena. A chemical survey of both species revealed many metabolites as phenolic acids, coumarins, flavonoids, terpenoids, sterols, volatile oils, carbohydrates, amino acids, fatty acids and others. The bioactivity studies of both species have been directed to possess potential antioxidant, antidiabetic, anticancer, anti-inflammatory, anti-pyretic, analgesic, anti-microbial, hypoglycemic, hypolipidemic and antiulcer activities. Meanwhile, antidepressant, antifertility, antiaging, anti-atherosclerotic, anti-anemic and diuretic activities were limited to C. dichotoma. On the other hand, anti-Alzheimer and larvicidal activities were limited to Cordia sebestena. There are fewer reported studies on C. sebestena, in spite of its important folk uses, comparing to C. dichotoma. Thus, this review draws attention to further biological research on C. sebestena to discover its medicinal uses.
... Ethyl alcohol extract of C. dichotoma showed cytotoxic action on brine shrimp lethality assay (LC 50 =20 µg/mL) [65]. Cytotoxicity of C. dichotoma leaf methanolic extract on human cervical cancer cell line (HeLa) was evaluated using 4′,6-diamidino-2phenylindole (DAPI) and (3-[4,5-dimethylthiazol-2yl]-2,5 diphenyl tetrazolium bromide) (MTT) staining tests .The results showed that extract with gotten IC 50 of 202 μg/mL, prohibited in vitro proliferation and induced apoptosis of HeLa cell, which signified a powerful anticancer property in comparison to tamoxifen (IC 50 =48 μg/mL) [81,82]. ...
... Hexokinase, phosphoglucoisomerse and aldolase levels increased in hepatoma-bearing rats, but they decreased to near-normal levels in animals administered plumbagin. Levels of the gluconeogenic enzymes, glucose-6phosphate and fructose -1, 6-disphosphatase decreased in hepatoma bearing animals, but increased in the animals treated with plumbagin [29] . Plumbagin inhibit NF-kB activation induced by TNF, and other carcinogens and inflammatory stimuli (e.g. ...
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The present review deals with chemical compounds, medicinal properties, biological activities and pharmacological effects of Plumbago zeylanica. Plumbago zeylanica (Linn.) belongs to family Plumbaginaceae, commonly known as Chitrak is one of the medicinal plants used in the Indian traditional system of medicine. Traditionally P. zeylanica is used as a stimulant digestant, expectorant, laxative and in the treatment of muscular pain and rheumatic diseases. Some parts of P. zeylanica are used in various pharmacological activities. The different parts of P. zeylanica are used for various ethnomedicinal purposes and investigations have been carried out on different chemical compounds such as plumbagin and other compounds of this plant. Its biological activities like antibacterial, antimycotic, antiviral, antiplasmodial, leishmanicidal, trypanocidal and anticarcinogenic have been studied along with pharmacological effects of it.
... Flowers: Napthalene: Azulein (5-methoxy quercetin 3-rhamnoside) [17], Leaves and stem:-volatile oil [17], Root: Nepthaquonones: Plumbagin [7,8] ,3,3'-biplumbagin, plumbagic acid, vanillic acid [18], Isoshinanolone [18,38], Elliptinone, chitranone [18,37], Trans-cinnamic acids, betasitosterol, 4hydroxybenzaldehyde, 2, 5-dimethyl-7Hydroxy-chromone, Indole-3-carbox-aldehyde [38], maritinone [18,39], 3-chloroplumbagin, 1,2 (3)-tetrahydro-3,3`-biplumbagin, zeylinone, isozeylinone, catechol tannins droserone, steroidal glycoside, sitosterol [18], 3,8-dihydroxy-6-methoxy-2-iso propyl-1,4-naphthoquinone and 5, 7-dihydroxy-8-methoxy-2-methyl 1,4-naphtho-quinone [18,40],; Coumarins: Seselin,xanthyletin,5-methoxyseselin, xanthoxyletin [39],; Plumbagic acid glucosides: (1), lupenone, lupeol acetate, plumbagin, trilinolein [41], 3-chlor-plumbagin, isoshinanolone,3,3'-bi-plumbagin, droserone, elliptinone (6,6'biplumbagin), 3,6'biplumbagin (chitranone), zeylanone, iso-zeylanone, naphthazarine, maritinone, 2-methyl [27], 1,2(3)-tetrahydro-3,3'biplumbagin and plumba-zeylanone [21]; Terpenes: Lupeol, friedelinol lupeol acetate, and lupanone; Sterols: Stigmasterol acetate, Sitosterone, stigmasterol [5]; Vitamins: A, B1, B2 and C [6]; Enzymes: Protease, Amylase, Lipase [6,17]; Sugars: Free glucose, fructose [17]. ...
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Plumbago zeylanica also known as Sheetraj or Chitraka belongs to the family Plumbaginaceae. It is one of the important medicinal plants which is used worldwide due to its therapeutic value. Therefore, this work carried out on Sheetraj has been, gathered, analyzed and reviewed using references from different sources like classical text and indexed journals. The aim of this review is to provide data or comprehensive information related to the chemical composition, pharmacological activities and therapeutic uses of P. zeylanica Linn. To explore its therapeutic potential and future research opportunities. In Unani system of medicine (USM), the roots of Sheetraj are widely used for internal administration and external application to treat many diseases. It contains the most important chemical constituents like Napthoquinones, Coumarins, Terpenes, Sterols, Plumbagic acid glucosides, Vitamin, Sugars etc. Plumbagin is this plant's main chemical component and is what gives it its diverse medicinal effects. It is present in the plant's stem, leaves, and roots. It carries out the actions
... The results obtained in B16F10 were further confirmed in SK-MEL-28 human cell line where plumbagin downregulated the cell viability and inhibited the migration, adhesion, and invasion of the cells (Figure 44). In addition, it has been reported that plumbagin exhibited as well an anti-proliferative, anti-invasive, and apoptotic property both in human cancers cell line and in vivo 179,180 . ...
Thesis
Lawsonia inermis L. commonly called Henna belongs to the family Lythraceae. It is known for its traditional importance both as a cosmetic and medicinal agent, especially in the indigenous regions of North Africa, South Asia and Middle East countries. The different parts of this shrub; leaves, stems, seeds and roots have different chemical constituents such as naphthoquinones, polyphenols, flavonoids, tannins, etc, which have various biological activities.The interest of this Mediterranean plant, in addition to its cosmetic use, is its biological activity antimicrobial, anti-inflammatory, anticancer and many others.This research work has been particularly interested in studying its anticancerous effect and more particularly its potential anti-melanoma metastasis given its traditional use often as a topical treatment for irritated skin.This research work allowed, first of all, the development of an experimental plan for the optimization of the global yield of extraction of active molecules from Henna (Lawsonia inermis L.). In the second stage, the identification and quantification of active compounds by high performance liquid chromatography coupled with mass spectrometry. A geographical mapping of henna crops in southern Morocco, using principal component analysis and based on the nature of the climate of each region was carried out.Subsequently, the effect of plumbagin on metastatic melanoma was studied. The study of this activity was evaluated in-vitro on murine and human cells respectively B16F10 and SKMEL-28. Plumbagin was found to significantly inhibit three important metastatic processes: migration, adhesion and invasion of B16F10 cells. These results were confirmed in the human cell line SK-MEL-28.
... Glycerol derivates are active as anti-inflammatory agents. (Imbs, Ermakova, Fedoreyev, Anastyuk, & Zvyagintseva, 2013) and cytotoxic (Nguyen et al., 2004;Tsai, de Castro-Cruz, Shen, & Ragasa, 2012). Thai et al. (2020) have reported four compounds from F. rukam stems led, while three compounds others have reported by Muharni Elfita, Heni, Yasrina, & Miranti (2019) from the stem bark. ...
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Flacourtia rukam is a plant popular among people to treat hypertension, especially the Musi Banyuasin of south Sumatera, Indonesia. Isolation and identification of chemical compounds from F. rukam leaves and evaluation of their effects on antihypertensive activity have been conducted. Isolation of chemical compounds using chromatographic methods and identification using spectroscopic methods were compared with the reported data. The drug’s effects on antihypertension were determined using the angiotensin converting enzyme (ACE) inhibitory method. Two compounds were first reported and isolated from the leaves of F. rukam and identified as apigenin (1) and lupeol (2). These compounds were demonstrated to be effective in treating antihypertension with IC50 656.51 ± 1.55 µg/mL for apigenin and 15.12 ± 0.72 µg/mL for lupeol. It can be concluded that F. rukam leaves is a potential ACE inhibitor can be explored further as an effective antihypertensive agent.
... Sitotoksisitas, sebagai parameter awal potensi antikanker, yang ditunjukkan daun awarawar dan kandungannya telah banyak dilaporkan dan diulas (Nguyen et al., 2004;Mandhare, 2015), namun belum ada laporan yang secara spesifik mengupas potensi antimetastasisnya khususnya untuk kanker payudara. Artikel ini disusun untuk menelaah potensi daun awar-awar sebagai agen ko-kemoterapi penghambat metastasis secara detail dan komprehensif. ...
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p>Kematian akibat kanker payudara sebagian besar disebabkan oleh metastasis. Kemoterapi sebagai agen terapi kanker payudara juga menimbulkan efek samping metastasis. Daun awar-awar ( Ficus septica Burm. F.) mengandung senyawa golongan alkaloid fenantroindolisidin. Ekstrak daun awar-awar dan alkaloid fenantroindolisidinnya berefek sitotoksik pada sel kanker payudara dan sinergis terhadap agen kemoterapi. Artikel ini mengulas potensi daun awar-awar sebagai agen pendamping kemoterapi (ko-kemoterapi), khususnya melalui mekanisme antimetastasis. Aktivitas sitotoksik daun awar-awar pada sel kanker terjadi melalui peningkatan apoptosis dan modulasi siklus sel. Daun awar-awar menghambat metastasis sel kanker payudara dengan menurunkan ekspresi VEGF, MMP-9, dan Rac-1 yang terlibat dalam metastasis. Oleh karena itu, dapat disimpulkan bahwa daun awar-awar berpotensi untuk dikembangkan sebagai agen ko-kemoterapi antimetastasis untuk kanker payudara. </p
... Cytotoxicity of two plumbagic acid glucosides, 3'-O-beta-glucopyranosyl plumbagic acid and 3'O-beta-glucopyranosyl plumbagic acid methylester along with five naphthoquinones (plumbagin, chitranone, maritinone, elliptinone and isoshinanolone) to various tumor cells lines was evaluated by Nguyen (51)and reported that plumbagin significantly suppressed growth of Raji, Calu-1 HeLa, and Wish tumor cells lines. Compound b-sitosteryl-3b-glucopyranoside-ad-O-palmitate isolated from Plumbago zeylanica showed cytotoxic activity against MCF7 and Bowes cancer cell lines. ...
... Nguyen et al. 45 isolatet betasitosterol, beta-sitosteryl-3beta-glucopyranoside, beta-sitosteryl-3betaglucopyranoside-6'-Opalmitate (1) ...
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Plumbago zeylanica L. (also known as Doctorbush) is a shrub, widely distributed throughout the tropical and subtropical regions of the world. The literature reveals its wide application in traditional system of medicines against various diseases, as anti-inflammatory, anti-malarial, anti-fertility, anti-microbial, anti-oxidant, blood coagulation, wound healing, memory enhancer and anti-cancer. The therapeutic uses of the plant have been attributed to the presence of number of bioactive compounds, such as elliptinone, zeylanone, sistosterol and plumbagin. The objective of the present review is to give a comprehensive information; taxonomical description, phytochemistry, pharmacological properties and traditional uses.
... It is found throughout India in the wild state and mostly grown in Bengal, Malay peninsula, Ceylon-tropics of the old world. In India, it is mainly cultivated in districts of Andhra [48]. The chemical constituents present in the aerial part of the plant consist of plumbagin, isohinanolone, plumbagic acid, beta-sitosterol, 4hydroxybenzaldehyde, trans-cinnamic acid, vanillic acid, 2,5-dimethyl-7-hydroxychromonr, indole-3carboxaldehyde [49]. ...
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Plumbago zeylanica is also known as chitraka, doctor bush, or leadwort. It is the most popular herbal plant that belongs to the family Plumbaginaceae or leadwort. Plumbagin is the most important chemical constituent present in the roots, leaves and stem of the plant that is responsible for various pharmacological actions including anti-malarial, anti-obese, anti-diabetic, anti-microbial, anti-ulcer, anti-inflammatory, anti-oxidant and anti-cancer. Traditionally it is used to treat variety of diseases such as dysmenorrhea, leprosy, anemia, rheumatic pain, cold, cough, arthritis and many more. It is considered as the most significant herbal plant in the ayurveda medicinal system of India and is widely accepted as a rejuvenator because of the presence of bioactive compounds. Various formulations of chitraka plant have made this plant more effective in the field of medicine. The plant carries various therapeutic properties and acts as a cardiotonic, neuroprotective and cns stimulant. The review aim is to provide data or information related to chitraka plant its usage in traditional and ayurveda medicinal system, its pharmacological properties and toxicity when taken in excessive amount. From the collected data, it is clear that the plant has great potential to cure various diseases and needs more research and development to explore its more pharmacological properties and socio-economic impact.
... Variation in the cell wall structure between Gram-negative and Gram-positive may have led to different inhibitory effects. Pharmacological properties that were described for the Plumbaginaceae family plants include anticancer, antiinflammatory, antioxidant, antimycobacterial, antimicrobial, antiatherogenic, cardiotonic, neuroprotective and insecticidal activities (Oyedapo, 1996;Kuo et al., 2002;Chaung et al., 2003;Mossa et al., 2004;Nguyen et al., 2004;SivaKumar et al., 2005;Yang et al., 2010;Dhale and Markandeya, 2011;Eren, 2016;Lashgari et al., 2016;Sundari et al., 2017). ...
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Objective: Acantholimon is a genus of perennial plant within the Plumbaginaceae family. Here, we aimed to investigate anticancer, antioxidant, and antibacterial potential of methanol extract of three Iranian endemic species of Acantholimon including A. austro-iranicum, A. serotinum and A. chlorostegium. Materials and methods: MTT assay was used to evaluate the in vitro cytotoxicity and apoptosis induction was examined by annexin V-PE apoptosis detection kit. Antioxidant activity was reported based on the DPPH-scavenging and DCF-DA assay. Antibacterial activity was measured by disc diffusion and micro-well dilution assay. Results: MTT assay showed less cytotoxicity of methanol extracts against the HUVEC normal cell line (IC50 values: 817-900 µg/ml) compared to cancer cell lines MCF-7, HT29, SH-SY5Y, NCCIT and A549 (IC50 values: 213 to 600 µg/ml) that show the specificity of extracts toward cancer cells. Plant extract showed apoptosis induction and cell cycle arrest at the G0/G1 phases documented by annexin V staining and flow cytometry. According to antioxidant tests, extracts exhibited significant DPPH scavenging potential (IC50 values: 30-37 µg/ml) and could protect against H2O2-induced oxidative stress. Antibacterial activities showed a stronger inhibitory effect on Escherichia coli and Pseudomonas aeruginosa as Gram- negative bacteria (diameter of inhibition zone: 11-13 mm and minimal inhibition concentration (MIC): 3.175 to 12.5 mg/ml) compared to Gram-positive bacteria including Enterococcus faecalis and Staphylococcus aureus (diameter of inhibition zone: 3-7 mm and MIC: 25 to 50 mg/ml). Conclusion: Our results suggested moderate cytotoxic and antibacterial potential and noteworthy antioxidant activity for the examined Acantholimon species.
... Salvia libanotica Boiss Labiatae) inhibit tumor promotio by DMBA/TPA [179] 40. Plumbago scandens Plumbaginaceae exhibit cytotoxic activity against breast cancer and melanoma cells, induces apoptosis and cell cycle arrest in a small cell [180] [181] 41. Citrus aurantifolia Rutaceae. ...
... A survey of literature revealed that some of the plants listed in the study possess antiproliferative and cytotoxic potencies. For instance, plumbagin isolated from Plumbago zeylanica has been shown to induce in vivo and potent in vitro antiproliferative and cytotoxic effect on a range of cancer cells such as Bowes cells, MCF-7, Hela cells, Raji, Calu-1 and glioma cells [24][25][26][27]. Similarly, methanol seed extract of Xylopia aethiopica induced potent antiproliferative and cytotoxic effect against drug sensitive and resistant human cancer cells (IC 50 3.28 μg/ml-33.43 ...
Article
Abstract Introduction The southwestern and northcentral parts of Nigeria are highly endowed with medicinal plants that have been used for decades to cancer. However, the herbal recipes and traditional medicinal practices used in treating cancer have been scarcely investigated and documented. New uninvestigated plants could serve as potential sources of novel cytotoxic agents. This study was aimed at documenting the traditional medicinal practices used for treating cancers in Ilorin and Lagos metropolis. Methods Information on herbal practices, medicinal plants and personal information of herbal practitioners was collected via questionnaire and oral interviews and analyzed. Plants cited were collected, identified and assigned voucher numbers. The names of plants were further authenticated using the plant list (www.theplantlist.org) and the world flora (www.worldfloraonline.org). Results A total of 41 plants were identified via oral interviews and questionnaires from 65 willing respondents within Ilorin and Lagos metropolis, respectively. Pistia stratiotes was the most frequently cited plant with a citation frequency of 57.1 % whereas, Mangifera indica Linn was the least cited plant with a citation frequency of 2.9%. Plants parts including leaf, bark, root, and seed were prepared as concoctions, decoctions or powders and administered topically or orally to treat breast, prostate, cervical, skin and ovarian cancer. Conclusion The study revealed that medicinal plants previously shown to have cytotoxicity in vitro are currently used for cancers in traditional medicine practice. Twenty six medicinal plants are mentioned here for the first time as anticancer plants and could serve as sources for novel cytotoxic agents against cancers.
... In addition, it has been reported that plumbagin exhibited as well an anti-proliferative, anti-invasive and apoptotic property both in human cancers cell line and in vivo. [28,29] The transition of melanoma cancer cells from a benign noninvasive stage to a metastatic, aggressive and invasive tumors is due to the accumulation of genetic and epigenetic alterations and the dysregulation of signal transduction pathways. [30,31] An early stage of melanoma is often characterized by a BRAF (V600E; 66%) mutation or an ectopic activation of neuroblastoma ras oncogene (NRAS), ...
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Melanoma is the most dangerous form of skin cancer with a very poor prognosis. Melanoma develops when unrepaired DNA damage causes to skin cells to multiply and form malignant tumors. The current therapy is limited by the highly ability of this disease to metastasize rapidly. Plumbagin is a naphtoquinone (5-hydroxy-2-methyl-1, 4-naphthoquinone), isolated from the roots of medicinal plant Plumbago zeylanica, and it is widely present in Lawsonia inermis L. It has been shown that plumbagin has anti-proliferative and anti-invasive activities in various cancer cell lines, however, the anticancer and anti-metastatic effects of plumbagin are largely unknown against melanoma cells. In this study, we evaluated the effect of plumbagin on B16F10 murine melanoma cell line. Plumbagin decreased B16F10 cell viability as well as the cell migration, adhesion, and invasion. The molecular mechanism was studied, and plumbagin downregulated genes relevant in MAPK pathway, matrix metalloproteinases (MMP's), and cell adhesion. Furthermore, plumbagin elevated the expression of apoptosis and tumors suppressor genes, and genes significant in reactive oxygen species (ROS) response. Taken together, our findings suggest that plumbagin has an anti-invasion and anti-metastasis effect on melanoma cancer cells by acting on MAPK pathway and its related genes.
... Plumbagin (5-hydroxy-2-methyl-1, 4-naphthoquinone), a yellow crystalline phytochemical isolated from the roots of plant Plumbago zeylanica L. ( Sandur et al., 2006) exhibited anti-proliferative, anti-angiogenic, anti-invasive, and apoptotic property in many human cancers in-vivo and in-vitro ( Kuete et al., 2016;Nguyen et al., 2004). Available data suggested that plumbagin induced toxicity against cancer at very less concentration compared with chemical chemotherapeutics and had an excellent impact on human health through the neuroprotective property ( Yuan et al., 2017). ...
Article
Plumbagin is a naturally-derived phytochemical which exhibits promising medicinal properties, including anticancer activities. In the present study, the anticancer potential of plumbagin has been demonstrated in lung cancer cells by targeting reactive oxygen species (ROS) and the intrinsic mitochondrial apoptotic pathway. Plumbagin showed impressive cytotoxic, anti-proliferative, and anti-migratory activities with IC50 3.10 ± 0.5 μM and 4.10 ± 0.5 μM in A549 and NCI-H522 cells, respectively. Plumbagin treatment significantly reduced the size of A549 tumor spheroids in a concentration-dependent manner. Plumbagin enhanced ROS production and arrested lung cancer cells in S and G2/M phase. Expression of antioxidant genes such as glutathione S-transferase P1 and superoxide dismutase-2 were found to be upregulated with plumbagin treatment in A549 cells. Plumbagin induced dissipation in mitochondrial membrane potential and affected the expression of intrinsic apoptotic pathway proteins. Increased expression of cytochrome c promotes the activation of pro-apoptotic protein Bax with decreased expression of anti-apoptotic protein Bcl-2. Further, plumbagin activated the mitochondrial downstream pathway protein caspase-9 and caspase-3 leading to apoptosis of A549 cells. Collectively, plumbagin could be a promising future phytotherapeutic candidate for lung cancer treatment via targeting intrinsic mitochondrial apoptotic pathway and ROS.
... Chemical content information from F. rukam very still limited. Ragasa et al. (2016) have been reported 5 compound from the dichloromethane extract the fruit of F. rukam that is monogalactosyl diacylglycerols, β-sitosteryl-3β-glucopyranoside-6β-O-fatty acid esters, β-sitosterol, triacylglycerols, and chlorophyll a. Compound monogalactosyl diacylglycerols is active as antiinflammatory agent (Imbs et al. 2013) and also reported to be cytotoxic (Nguyen et al. 2004;Tsai et al. 2012). Ikram et al. (2009) reported that the fruits contain phenolics and demonstrate the activation of antioxidants with an inhibitory value of 70.9%. ...
... It is used for treating diarrhea, dysentery, piles and peptic ulcers. The bioassay-guided fractionation of the dichloromethane extract of aerial parts of Plumbago zeylanica led to the isolation of β-sitosterol, β-sitosteryl-3β-glucopyranoside, β-sitosteryl-3β-glucopyranoside-6′-O-palmitate, lupenone, lupeol acetate, plumbagin and trilinolein (Nguyena et al., 2004). Plumbagin modulates cellular proliferation, carcinogenesis, and radioresistance, all known to be regulated by the activation of the transcription factor NF-κB, suggesting plumbagin might affect the NF-κB activation pathway (Santosh et al., 2006). ...
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This Reference e-Book contain 11 Chapters with an attempt to summarize the current knowledge of promising ethnomedicines and their phytophores, to compounds tested against diverse diseases. The therapeutic properties and structure activity relationship (SAR) of some important and potentially useful ethnomedicines is addressed with a focus on how these ethnic knowledge can led to the development of useful therapeutic lead for preclinical or clinical evaluation. In general it is a snapshot of different areas of research on the role of phytochemicals in health, comprehensively presented and is useful of tidbits of knowledge or ideas for research, covering the ethnomedicines uses in the management of several diseases, particularly, infectious diseases (like viral, bacterial and fungal) and lifestyle related disorders mostly validated by modern scientific methods. In depth information prepared by experts all over the globe traces the evolution of herbal drugs with civilization and their use as antiviral, antibacterial, antifungal, antiparasitic, antioxidants, anticancerous, chemopreventors, memory enhancers, neuroprotective, immunomodulator, laxatives, analgesic and anti-inflammatory disorders, along with safety issues and toxic effects.
... For example, β-sitosterol and βtrilinolein, two extracts of plumbago indica L 24 , exhibited cytotoxicity against breast cancer cell MCF7 and had an anti-inflammatory effect, respectively. 24,25 Plumbagin was also reported to show antibacterial activity against Staphylococcus aureus and Staphylococcus epidermidis. 26 Recently, some studies have shown that plumbagin exerted an anti-tumor effect on some tumors, including prostate cancer, esophageal cancer, and lung cancer. ...
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Purpose Plumbagin is thought to be a bioactive phytochemical drug and exerts an antitumor effect on various cancers. However, few studies focus on the antitumor activity of plumbagin on liver cancer. This study first investigated the antitumor activity of plumbagin on liver cancer and further investigated the molecular mechanism of its antitumor activity against hepatocellular carcinoma, both in vitro and in vivo. Methods The antiproliferative activity of plumbagin was evaluated through CCK-8, EdU, and colony forming test. The cell cycle and apoptosis were then analyzed by flow cytometer. Western blot was used to detect the expression of apoptosis related protein, SIVA, and mTOR pathway. RNA-seq was performed to determine the gene expression profiles and overexpressed or knocked down SIVA to validate its role in plumbagin’s antitumor activity. Regarding animal experiment, a xenograft model in BALB/c nude mice was built using LM3-Luci cells. Then bioluminescence imaging and further immunohistochemistry were performed to study the antitumor activity and the expression of SIVA and mTOR in the plumbagin-treated group. Results Plumbagin can inhibit proliferation and induce apoptosis of liver cancer cells in vitro. Further experiment demonstrated that plumbagin could inhibit the expression of SIVA and subsequently downregulate the mTOR signaling pathway, and upregulating the expression of SIVA will alleviate the antitumor activity of plumbagin on liver cancer, which confirmed the important role of the SIVA/mTOR signaling pathway in the antitumor activity of plumbagin. In vivo bioluminescence imaging showed a decreased signal in the plumbagin-treated group, and further immunohistochemistry demonstrated that plumbagin could inhibit the SIVA/mTOR signaling pathway in tumor tissues. Conclusion Our promising results showed that plumbagin could inhibit proliferation and induce apoptosis of hepatic cancer through inhibiting the SIVA/mTOR signaling pathway for the first time, which indicated that plumbagin might be a good candidate against liver cancer.
... 88 The dichloromethane extract of aerial parts contain beta-sitosterol, beta-sitosteryl-3betaglucopyranoside, beta-sitosteryl-3-betaglucopyranoside-6'-O-palmitate, lupenone, lupeol acetate, plumbagin and trilinolein. 59 In addition, the natural active compound Plumbagin isolated from different plant part of PZ by RP-HPLC 89 along with synthesis of the binaphthoquinone, 3, 3'-biplumbagin [90]. Plumbagin was quantified by reverse phase HPLC and UV detection, 91 liquid chromatography coupled with tandem mass spectrometric. ...
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Plumbago zeylanica L. (Plumbaginaceae) (PZ) commonly called as Doctorbush is a semi climbing sub shrub used to effective against anaemia, rheumatic pain, dysmenorrhoea, leprosy, ulcers and elimination of intestinal parasites. In Ayurvedic system of medicine, the roots of the plant and its constituents are credited with potential therapeutic properties including cardiotonic, neuroprotective and CNS stimulating properties. The aim of this review is to provide comprehensive information on the traditional uses, phytochemistry, pharmacological actions and toxicity study of Plumbago zeylanica L to explore their therapeutic potential and future research opportunities. All the relevant information of PZ was collected through MEDLINE/PUBMED. The evidence presented in this review has showed that PZ has great potential to be integrated into conventional medical practice for the treatment of various metabolic diseases, hepatotoxic, diabetes, inflammation, cancer and other disease complications. Future research on PZ would provide much knowledge about pharmacological uses and socioeconomic impact.
... Plumbagin (5-hydroxy-2-methyl-1, 4-naphthoquinone), a yellow crystalline phytochemical isolated from the roots of plant Plumbago zeylanica L. (Sandur et al., 2006) exhibited anti-proliferative, anti-angiogenic, anti-invasive, and apoptotic property in many human cancers in-vivo and in-vitro (Kuete et al., 2016;Nguyen et al., 2004). Available data suggested that plumbagin induced toxicity against cancer at very less concentration compared with chemical chemotherapeutics and had an excellent impact on human health through the neuroprotective property (Yuan et al., 2017). ...
... We have recently reported the isolation of some anti-inflammatory steroid glycosides with new skeletons from the stems of this plant (Seeka et al., 2017). Further investigation of the hexanes leave extract, which inhibited NO production in RAW264.7 cells with an IC 50 value of 93.6 μg/mL and showed several fluorescent spots on TLC chromatograms, has led to the isolation of two new triterpenoid cinnamates (1 and 2) in addition to 13 known compounds identified as 3β-O-D-friedoolean-11α,12α-epoxy-14-enyl cinnamate (3) (Lai et al., 1987), β-sitosteryl-3β-glucopyranoside 6'-palmitate (Nguyen et al., 2004;Kuo et al., 1998), phytol, 3β-O-D-friedoolean-11α,12α-epoxy-14-enyl palmitate (Barreiros et al., 2002;Huang et al., 1990), 3β-O-D-friedoolean-11α,12α-epoxy-14-enyl acetate (marsformoxide B) Lai, 1979, 1978), lupeol cinnamate (Wood et al., 2001;Akihisa et al., 2010), αamyrin cinnamate (Wood et al., 2001;AKihisa et al., 2010), β-amyrin cinnamate (Akihisa et al., 2010), a mixture of β-sitosterol and stigmasterol, citrostadienol (Rao and Suseela, 1982;Yan et al., 2015;Zhang et al., 2006), a ceramide [(2S,3S,4R)-2-[(2R)-2-hydroxytetracosanoylamino]-1,3,4-octadecanetriol] (Zeng et al., 2012), lupeol and 1,2-di-hexadecanoyl-3-(9Z-octadecenoyl)-sn-glycerol. Herein, we report the spectroscopic identification of 1 and 2. Because there was no available physical data or 1 H and 13 C NMR spectroscopic data for 3, although this compound was documented to be isolated from Gymnema alternifolium (Lai et al., 1987), that data was also included in this report. ...
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Two new triterpenoid cinnamates, namely, 3β-O-D-friedours-11α,12α-epoxy-14-enyl cinnamate and 3β-O-29-nor-20-oxolupanyl cinnamate, as well as thirteen known compounds were isolated from hexanes extract of the leaves of Hoya kerrii. The structural elucidation of the compounds was performed using spectroscopic methods. Among several isolated triterpenoid cinnamates, lupeol cinnamate is known to possess strong anti-inflammatory properties. The presence of 3β-O-D-friedours-11α,12α-epoxy-14-enyl and 3β-O-D-friedoolean-11α,12α-epoxy-14-enyl esters has only been reported in a few species of Apocynaceae.
... Plumbagin, a cytotoxic element extracted from Plumbago species [4] has the potential to serve this purpose. Plumbagin's effective chemosuppressive action has been demonstrated in breast cancer, [5] ovarian cancer, [6,7] pancreatic cancer, [8] lung cancer, [9,10] and prostate cancer. ...
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Background: Plumbagin (5-hydroxy-2-methyl-1,4-napthoquinone) derived from Plumbago species is a potential anti-tumour agent. Plumbagin has been tested for anti-cancer activity in vitro and in vivo using mice model. Aim: To study the tumour suppressing efficacy of plumbagin using zebrafish model. Materials and methods: Human Non-small lung cancer cell line were cultured in vitro and transplanted in to zebrafish. The development of tumour was confirmed by performing histology. The tumour was then allowed to progress in vivo and the fishes were administered with plumbagin orally for three continuous days. The tumour suppression capacity was monitored subsequently using transcriptosome analysis. Statistical methods: The pixel integrated density obtained was converted into relative gene expression using IBM SPSS. Results: The administration of plumbagin had an ability to suppress tumour and the size of the tumour were relatively lesser when compared with the control sample; it has also increased p53 gene expression. Conclusion: The study helps to conclude that plumbagin is an effective anti-tumour agent against human cancer cells based on the study in vivo in zebrafish.
... Plumbago rosea with red flowers, Plumbago zeylanica with white flowers and Plumbago auriculata with blue flowers. Their major ingredients are napthoquinones such as plumbagin (5-hydroxy-2methyl-1, 4-naphthoquinone), 3, 3'-biplumbagin and elliptinone, 4-hydroxybenzaldehyde (V), trans-cinnamic acid (VI), vanillic acid (VII), lupenone and trilinolein (Nguyen, 2004;Zhang et al., 2007;Kaewbumrung and Panichayupakaranant, 2011). Plumbago indica is more commonly used in Thai traditional medicine. ...
... Plumbago indica also known as Plumbago rosea common plants used in Ayurveda system of medicine. Its root extract is widely used due to its medicinal property such as antibacterial[9], antifungal[10], antiparasitic[11,12], antifertility[13]and antitumor activities[14]. Our previous studies revealed the protective efficacy of P. indica root extract against thioacetamideinduced oxidative stress[15]. However no comprehensive evidence has yet been documented for the hepatocurative activity of P. indica experimentally. ...
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The root parts of The study was designed to evaluate the hepato curative activity Plumb methanolic root extracts at different doses (100 and 200 mg/kg bw) against thioacetamide induced liver damag Thioacetamide (100 mg/kg bw) and was assessed by evaluating the activity of liver marker enzymes, antioxidant enzymes and lipid peroxidation. The liver sections were evaluated serum liver enzymes and hepatic levels of antioxidant markers. Histopathological findings also confirmed the curative effect of scientifically rationale the use of liver disorders
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Plumbago zeylanica is a member of the Plubaginaceae family and well known for its pharmacological properties attributed to secondary metabolites such as phenolics, alkaloids, and saponins. Notably, the root extracts of this plant contain a compound called "plumbagin (PLB)," which has been responsible for its anti-cancer activity. PLB is a naturally forming naphthoquinone found in plant roots. Numerous researchers have stated the anti-cancer activity of PLB against various cell lines of cancer that include squamous cell carcinoma, gastric cancer, cholangiocarcinoma, adenocarcinoma, prostate cancer, oral squamous cell carcinoma, melanoma, brain tumor, lung cancer, breast cancer, kidney lymphocyte carcinoma, osteosarcoma, canine cancer, tongue leukemia, esophageal cancer, and hepatoma. In this chapter, we comprehend a review of the studies published till now related to the anticancer properties of Plumbago zeylanica, examining both recent advances and existing limitations in understanding of its potential in cancer treatment.
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Plants have long been recognized as valuable sources of medicine, with numerous herbal drugs derived from plant compounds. Plumbago zeylanica Linn., a member of the Plumbaginaceae family, is a perennial sub scandent shrub widely used in traditional Indian medicine. The study aims to explore the potential of various parts of Plumbago zeylanica in the treatment of diabetic nephropathy by investigating in-vitro experiments and conducting molecular docking studies with proteins associated with the disease. The in-vitro findings exhibited that the extract of roots have greater inhibition activity than stem extract, followed by the leaf extracts of Plumbago zeylanica. The glucose uptake assay showed that the enhancement of glucose transport was different for all three concentrations of glucose solution. In molecular docking, the highest binding affinities of Plumbago zeylanica bioactive compounds and target proteins were ranging from-7.196 to-9.447. Additionally, the lowest binding affinities of Plumbago zeylanica bioactive compounds and target proteins were ranging from-3.779 to-7.196, which were also higher than reference compound for different active constituents. ADMET prediction was performed to assess the pharmacokinetic properties of the active constituents. The findings of this study will shed light on the phytochemical composition of Plumbago zeylanica and its potential as a therapeutic agent for diabetic nephropathy.
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Plumbago zeylanica Linn. (Plumbaginaceae), a plant utilised as a widespread folk remedy and antifertility agent, was examined for its antifertility activity in the current study. The effects of 200 and 400 mg/kg of five sequential solvent extracts, including petroleum ether, chloroform, acetone, ethanol, and water, on the estrous cycle were investigated. Only the acetone extract was shown to be the most successful at stopping the rats' typical estrous cycle (p0.05, p0.01, and p0.00). The rats' diestrous portion of the estrous cycle was lengthened, which temporarily inhibited ovulation. When the extract was removed, the anovulatory activity was reversible. The functioning of oestrogen in rats was further investigated using the efficient acetone extract. In comparison to the control, the extract demonstrated strong estrogenic and antiestrogenic action (p0.05), (p0.01), and (p0.001). Studies on the uteri's histology were done to verify the estrogenic activity. The findings showed that Plumbago zeylanica stem extract had an antifertility effect on albino rats.
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The present review summarizes the studies regarding the isolation and characterization of phytoconstituents and the biological activity of Plumbago zeylanica. Biological activity like: cytotoxic activity, antifertility, antifungal, anti-inflammatory, antibacterial, antioxidant, anticancer and CNS activity of this plant have been reviewed in this paper.
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Sustainability entails addressing our demands without jeopardizing future generations' ability to meet their own needs. In September 2015, 193 United Nations Member States adopted the 17 Sustainable Development Goals (SDGs), also known as the Global Goals, as a universal call for action to eradicate poverty, safeguard the environment, and ensure that all people experience peace and prosperity by 2030. These 17 interconnected global goals and 169 targets will be tracked and reviewed using a set of global indicators that will serve as a "blueprint for achieving a better and more sustainable future for everybody." Sustainability is all about the effective management of natural resources. These resources are limited and critical to maintaining ecological balance. There is a range of ways that can be used to attain these goals, including climate-smart agriculture, various means for achieving food security for zero hunger, adoption of local food diversity and education for zero poverty, and the removal of environmental toxins from land. A collective effort is required to balance our socio-economic needs with environmental needs. As a result, the effort to generate work that covers all aspects of sustainability, as is the case here, must come from a diverse set of experts. This permits each discipline of study to provide its unique perspective to a very complex and vital subject that could otherwise be intractable. In the prologue, the writers remind readers that the text does not always convey a self-contained set of ideas. Rather, within the broader documentation of Sustainability and Science, a degree of variability is accepted. This is unusual for an academic text, yet it is required in this case. The reason for this is that contemporary environmental issues are both time-sensitive and dynamic, and a perfect understanding does not exist and may never exist. However, the difficulties must be handled in good faith, on time, and with the best science available. As humanity fights to understand and tackle the great environmental concerns of our day, it is my sincerest hope that this effort, which is freely and extensively shared, will serve as an educational milestone. Furthermore, the text Strategies to Achieve Sustainable Development Goals (SDGs): A Road Map for Global Development contributes to the intellectual foundation that will enable students to become the engines that will propel and maintain society on the path of sustainability and sustainable development through the difficult process of change alluded in “Our Common Future’’. A brief chapter-by-chapter description is as follows: In Chapter 1, Thakur Prasad Yadav, Rajani Srivastava and Kalpana Awasthi have presented an innovative and sustainable approach for E-waste management through mechanical milling. E-waste is something that contains harmful compounds that, if not properly controlled, could harm human health and the environment. They also discussed various methods for recovering metals from e-waste. Manish Mathur and Preet Mathur in Chapter 2 discussed land restoration as key to sustainable prosperity and provide holistic information on different aspects of halophytes, specifically regarding the genus Haloxylon. Chapter 3 discusses cyanobacteria, a third-generation renewable energy resource that does not conflict with our food supply. It helps attain UN-SDGs especially goal 7 i.e., access to affordable, reliable, sustainable and modern energy for all. Chapter 4, written by Sonam Gupta and Pradeep Kumar, describes the current state of biodiversity, the reasons for the decline and the interconnections between biodiversity and food security. It also discusses the importance of soil biodiversity as well as how the agricultural system contributes to biodiversity loss. Chapter 5 deals with microbial biomass and suggests it as a sustainable approach to restoring degraded soil. Microorganisms present in soil can bio-mineralize or bio-transform the contaminants into simpler, less toxic, or immobile forms. This chapter is written by Gitanjali. Anupriya Singh and others have given their research output in Chapter 6. Their study provides comprehensive information about Arbuda (cancer) and its probable remedy through Ayurveda and fulfilling the SDG 3. Chapter 7 describes combating the menace of indoor air pollution for sustainable life. The authors emphasized the replacement of conventional stoves and fuel with much more efficient ones. Chapter 8 represents the development of natural farming systems as eco-tourism, a newly emerging concept in tourism, fusing environmental protection, cultural awareness, and low impact travel with the provisioning of employment generation. Mishra and coauthors in their chapter presented agro-eco-tourism models to improve the farm income and the socio-economic status of the farmers of rural areas is required while preserving the biodiversity and ensuring sustainable growth. Chapter 9 covers the wide area of the impact of crop residue/stubble burning on human, environment and soil health along with its possible management. According to Siddique and Sai Mentada in their chapter, crop residue can be utilized efficiently as a source of biofuel, biochar, bio-oil and cattle feed. In Chapter 10, Dwivedi, Srivastava and Vijai Krishna give an overview of sustainable plant nutrition and soil carbon sequestration. They reviewed the basic mechanism leading to carbon stabilization in soils and new practices and technological developments in agricultural and cropland sciences for carbon sequestration. Chapter 11 intends to offer insight into the underpinnings of ‘place making’ through exploring diverse perspectives related to the concept. This chapter also seeks to identify the nexus between placemaking and urban tourism and attempt to recognize major ways in which it can contribute to achieving the goals of sustainability. Ranjana Tiwari in Chapter 12 emphasized that a healthy and long life is the first requirement of humans. She stresses the outlook of health from a psychological perspective and according to her, good mental health and well-being are strategies to attain sustainability. Chapter 13 gives an overview of the potentiality of cyanobacteria and its application in wastewater management. According to Tripti Kanda and coauthors, cyanobacteria can be used as an innovative solution for a sustainable ecosystem. Gender equality is an important goal among 17 SDGs; Chapter 14 discussed this in the Indian context. Chapter 15 is presented by Rekha Srivastava, where she discussed challenges of mental health and prevention, the importance of healthy life and achieving SDGs. Chapter 16 explores the field of biofortification, innovative technology and strategies to remove malnutrition and achieve different UN-SDGs like Goal 2 (Zero hunger), Goal 3 (good health and well-being), Goal 12 (responsible consumption and production) and Goal 13 (Climate Action). This strategy will not only reduce the number of severely malnourished people who require complementary interventions but will also assist them in maintaining their improved nutritional status. Chapter 17 discussed the efficiency of ecotourism. According to the author, it should promote sustainable development by establishing a long-term productive base that benefits both residents and ecotourism providers. Srishti, Alok and Gopal Nath in Chapter 18 presented phage therapy, a new way for the treatment of multidrug-resistant bacteria. According to them, phage therapy might be a good alternative to antimicrobial chemotherapy and helpful in achieving good health and well-being which is goal 3 of UN-SDGs.
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Cancer is one of the most dreaded diseases of the 20th century and spreading further with continuance and increasing incidence in 21st century and additionally is set to become a major cause of morbidity and mortality in the coming decades in every region of the world. Moreover, cancer is a complex disease involving numerous tempospatial changes in cell physiology, which ultimately lead to malignant tumors. Abnormal cell growth (neoplasia) invasion of surrounding tissues and distant organs is the primary cause of morbidity and mortality for most cancer patients. It is a fatal disease caused mainly by environmental factors that mutate genes encoding critical cell-regulatory proteins. The resultant aberrant cell behavior leads to expansive masses of abnormal cells that destroy surrounding normal tissue and can spread to vital organs resulting in disseminated disease. The cancer-causing agents (carcinogens) can be present in food and water, in the air, and in chemicals and sunlight that people are exposed to. In this chapter we summarize the basic knowledge's in cancer definition, history, etiology, diagnosis, classifications and epidemiology.
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Plumbago zeylanica L. (Fam. – Plumbaginaceae) is an annual herb or perennial shrub, height up to 0.5–2 m, leaves are dark green, alternate, simple, and stipulated, raceme type inflorescence, flowers are white with diameter of 1/2–3/4 in., and arranged in clusters. The root decoction used for treatment of dysentery, abdominal problems, peptic ulcers, diarrhea, disorders of spleen, fevers, and piles. The methanolic extract of this plant species demonstrated antiviral effect against Coxsackie virus B3, influenza A virus, herpes simplex virus, type 1 Kupka, and antifungal activity against Candida albicans, Epidermophyton floccosum, Microsporum gypseum, and Trichophyton rubrum. Plumbago zeylanica L. is considered as therapeutically important plant and possesses various types of pharmacological activities. The in vitro cultures were established on Murashige and Skoog culture medium with addition of 6‐benzylaminopurine.
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Chemical investigation of the dichloromethane extracts of Kosteletzkya batacensis (Blanco) Fern.-Vill., an endemic Philippine plant, has led to the isolation of β-sitosteryl-3β-glucopyranoside-6'-O-fatty acid esters (1), phytyl fatty acid esters (2), squalene (3) and chlorophyll-a (4) from the leaves; squalene (3), chlorophyll-a (4), a mixture of β-sitosterol (5a) and stigmasterol (5b) in a 2:1 ratio and long chain hydrocarbons (6) from the stems. The structures of compounds 1-6 were identified by comparison of their NMR data with literature data.
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Background: Gastrin and cholecystokinin (CCK) mediate their effects through at least two types of receptors (CCK receptors A and B). While it has been hypothesized that gastrin, a stimulator of gastric acid secretion, is also a neurotransmitter and a stimulator of cell proliferation in various normal and neoplastic tissues, its effect on astrocytic brain tumors has not been actively investigated. Purpose: Our goal was to determine the effects of gastrin and gastin and/or CCK antagonists on the proliferation in vitro of astrocytic tumor cells by use of both established cell lines and primary cell cultures of tumor tissue. Methods: Ten established astrocytic tumor cell lines, SW1088, SW1783, Hs683, H4, U87, U118, U138, U373, T98G, and A172, were studied. The effects of added gastrin (at 0.01, 0.1, and microM) and the gastrin/CCK antagonists L-365,260, CI-988, L-364,718, and JMV 234 (each at 0.01, 0.1, and 1 microM) on the cellular proliferation rates of the 10 cell lines were indirectly measured by use of the colorimetric tetrazolium assay. The influence of gastrin (at 0.01 microM) on the cellular proliferation of primary cultures from nine freshly explanted astrocytic tumors was assessed by means of tritiated thymidine uptake and autoradiography. Results: At specific concentrations, added gastrin increased the cellular proliferation of three established astrocytic cell lines (A172, Hs683, and SW1088), decreased it in two (U373 and T98G), and was without effect on the remaining five. Gastrin decreased cellular proliferation in one primary astrocytic tumor cell culture, stimulated it in five, and had no apparent effect in the remaining three. L-365,260, a CCK receptor B antagonist used at 0.01 microM, increased cellular proliferation in seven cell lines (A172, H4, Hs683, SW1783, T98G, U118, and U138), decreased it in one (U87), and had no effect in the remaining two. CI-988, another CCK receptor B antagonist used at 0.01 microM, inhibited cellular proliferation in five cell lines (A172, H4, SW1783, U373, and U87), stimulated it in two (T98G and U138), and had no effect in three. The CCK receptor A antagonists L-364,718 and JMV 234, both used at 0.01 microM, affected the cellular proliferation of only three of the 10 cell lines. Conclusions: These results suggest that gastrin (and perhaps CCK that belongs to the same peptide family) may play a role in the growth of a substantial proportion of human astrocytic tumors.
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Two new triterpenoids, 1-keto-3β, 19α-dihydroxyurs-12-ene-24,28-dioic acid dimethyl ester (1) and its 3-O-β-D-arabinopyranosyl derivative 2, were isolated from P. zeylanica.
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A new steroid, 22, 23-dihydrospinasterol plamitate was isolated from the whole plants of Arenaria kansuensis (Caryophyllaceae) and its structure was determined by chemical and spectroscopic means. 22, 23-Dihydrospinasterol, 22, 23-dihydrospinasterone, ergosterol-5, 8-peroxide, 24-methylene-22, 23-dihydrolanosterol, zeorin, fernenone, β-sitosterol 3β-O-β-D-glucopyranoside, tricin, (+)-isoscoparin and (-)-isoscoparin were also isolated.
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Epi-isoshinanolone, a diastereoisomer of isoshinanolone, has been isolated from Plumbago scandens and characterized with the aid of NMR spectroscopy.
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The13C NMR spectra of a series of steroids used to synthesize ecdy- and brassinosteroids are studied.
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A new steroid derivative, sitosteryl 3β-glucoside 6′-O-palmitate, together with sitosterol, sitosteryl 3β-glucoside, lupeol, taraxasterol, crysoeriol, vitexin, luteolin 3′-glucoside, p-hydroxybenzoic acid, vanillic acid, p-hydroxyacetophenone and a lignan, (−)-arctigenin, were isolated from the aerial parts of Centaurea regia.
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The 13C NMR spectra of lupeol and related triterpenes were recorded and all carbon shifts assigned. Their analysis aided in the shift assignment of the structurally related hopane-like triterpenes.
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beta-Sitosterol (SI-0), beta-sitosterol glucoside (SI-1), dioscin (SI-2), methyl protoprosapogenin A of dioscin (SI-3), methyl protodioscin (SI-4) and protodioscin (SI-5) were isolated and characterized from the whole plant of Solanum indicum L. (Solanaceae). Except for beta-sitosterol, these compounds have not been previously isolated from Solanum indicum L. Both CHCl3 soluble (SI-IV) and insoluble (SI-V) fractions of the ethanolic extract (SI-I) showed cytotoxicity on seven cancer cell lines: Colo-205 (colon), KB (nasopharynx), HeLa (uterine cervix), HA22T (hepatoma), Hep-2 (laryngeal epidermoid), GBM8401/TSGH (glioma) and H1477 (melanoma). The purified constituents, SI-2 and SI-4 showed more potent effects by DEA and MTT assay. SI-2,3,4 and 5 also demonstrated cytotoxicity on cultured C6 glioma cells by PRE assay, ans SI-3,4 and 5 showed a tumor inhibitory effect in vivo in C6 glioma cells. In addition, SI-2 had an inhibitory effect on the DNA synthesis of C6 glioma cells at 10 micrograms/ml.
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Dose-effect curves were fitted in optimizing a non-linear cost function by the simplex method. Two kinds of mathematical functions (Gompertz and Von Bertalanffy) and some weighting processes were studied. In each case a statistical analysis was carried out to choose the curve which is best fitted to experimental data. From the best curve, the efficient doses were calculated. This work was illustrated by cytotoxicity studies concerning melphalan and pyrrolidin.
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Epidemiological and experimental studies have suggested a protective role of phytosterols (PS) in the development of some types of cancer such as colon and prostate cancer. No work has been reported on the role of PS in the development of breast cancer, the second leading cancer in woman. The present study was designed to examine the effect of the two most common dietary PS, beta-sitosterol (SIT) and campesterol, as compared to cholesterol, the main sterol in the Western diet, on growth, apoptosis and cytotoxicity of MDA-MB-231 human breast cancer cells in culture. In addition, we investigated the possible role of protein phosphatase 2A (PP2A), an enzyme that has been shown to regulate growth and apoptosis in tumor parameters studied. Breast cancer cell growth was found to be inhibited by 66% after 3 days and 80% after 5 days with 16 microM SIT. Both campesterol and cholesterol sustained tumor growth at levels comparable to that of the vehicle control. None of the sterols tested at this level (16 microM) induced cytotoxicity as measured by lactic dehydrogenase release. SIT supplementation for 3 days at 16 microM resulted in a 6-fold increase in apoptosis in cells when compared to cholesterol treated cells. SIT treatment was found to have no effect on the level and content of tumor cell PP2A. It is concluded that SIT, by a still unknown mechanism, may offer protection from breast cancer by inhibiting growth and stimulating apoptosis.
Article
Two simple experiments measuring the 13C linewidths nu(1/2) and spin-lattice relaxation times T(1) of each of the signals in the spectrum of trilinolein indicate that the nu(1/2) and T(1) values are consistent with the different degrees of motional freedom expected for the various 13C nuclei. However, for each chain, the nu(1/2) and T(1) measurements indicate a small reversal in mobility at C-10 relative to C-9 before motional freedom again steadily increases on each chain starting at C-11. The T(1) experiment allows unambiguous assignments of the C-8 signal and C-14 signal, which differ by only 0.010 ppm. Measurements of 13C nu(1/2) and T(1) values on tripalmitin provide secure assignments for the C-5 and C-6 signals, for which conflicting assignments have been reported. The T(1) measurements also show that among the tightly clustered C-8 through C-12 signals, the C-11 signals are the most downfield, while the C-12 signals are the most upfield, again contrary to a previous report. Similar measurements of 13C nu(1/2) and T(1) values on other triacylglycerols or related compounds may prove equally useful in making chemical shift assignments and detecting any discontinuities in motional freedom along a chain. The benefits and possible limitations of ultrahigh field NMR for studying triacylglycerols and related compounds are discussed.
Vietnamese medicinal plant dictionary
  • Vc Vo
  • V Veluri
  • Vd Diwan
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  • Ir Siddiqui
  • J Singh
  • S Oksuz
  • Ah Mericli
  • R Vicente
  • Rd Carvalho
  • Gv Baddeley
  • Ir Burfitt
  • Ln Moreno
w2x Vo VC. Vietnamese medicinal plant dictionary. Hanoi: Y Hoc Press, 1997. w3x Veluri V, Diwan VD. Indian Drugs 1999;36:724. w4x Gupta A, Rai R, Siddiqui IR, Singh J. Fitoterapia 1998;5:420. w5x Ulubelen A, Oksuz S, Mericli AH. Phytochemistry 1988;27:3964. w6x Bhattacharyya J, Vicente R, Carvalho RD. Phytochemistry 1986;25:764. w7x Wenkert E, Baddeley GV, Burfitt IR, Moreno LN. Org Mag Res 1978;11:337. w8x Alemany LB. Chem Phys Lipids 2002;120:33.
Medicinal plants and drugs from Vietnam
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Vietnamese medicinal plant dictionary
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Veluri V, Diwan VD. Indian Drugs 1999;36:724.
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  • J Bhattacharyya
  • R Vicente
  • R D Carvalho
Bhattacharyya J, Vicente R, Carvalho RD. Phytochemistry 1986;25:764.
  • E Wenkert
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  • I Camby
  • I Salmon
  • A Danguy
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  • J Martinez
  • R Kiss
Camby I, Salmon I, Danguy A, Pasteels JL, Brotchi J, Martinez J, Kiss R. J Natl Cancer Inst 1996;88:594.
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  • H C Chiang
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Chiang HC, Tseng TH, Wang CJ, Chen CF, Kan WS. Anticancer Res 1991;11:1911.