白花丹地上部分的化学成分

研究白花丹Plumbago zeylanica L．地上部分的化学成分。应用各种色谱方法分离；用波谱学方法特别是二维核磁共振波谱的方法确定结构。从白花丹地上部分分离鉴定了7个化合物，分别是：1β，3β，11α-trihydroxy-urs-12-ene（1），androsta-1，4-diene-3，17-dione（2），异信浓柿醇酮（3），neoechinulin A（4），harman（5），ergostadiene-3β，5α,6β—triol（6），N-（N-benzoyl-S-phenylalaninyl）-S-phenylalaninol（7）。化合物1为新化合物，化合物2，4-7均为首次从该属植物中分离得到。     

白花丹中微量元素的测定

目的:建立白花丹中微量元素的测定方法。方法:采用电感耦合等离子体发射光谱(ICP-AES)法同时测定白花丹中Cu、Zn、Fe、Ca、Mg、Mn、Sr等7种微量元素,原子荧光(AFS)法测定Se元素。结果:2种方法的RSD在0.78%～3.01%之间(n=5),元素回收率在91.9%～105.8%之间,测定结果较理想。白花丹中含有非常丰富的Se元素,Cu、Zn、Fe、Ca、Mg、Mn、Sr等元素也较为丰富。结论:本方法简便、快速、准确,适于分析测定白花丹中的微量元素,测定结果对研究白花丹的药理作用具有参考意义。     

白花丹不同提取部位体外抗肿瘤及急毒研究

白花丹为蓝雪科植物白花丹Plumbago zeylanicaL.的干燥根、根茎和全草。为东南亚许多国家及中国多民族常用药材[1]。在民间有良好地治疗某些恶性疾病(癌症)的临床应用基础,本文拟对白花丹不同溶媒提取物进行体外抗肿瘤活性筛选,以期为进一步开发利用提供科学依据。1材料与方法1.1材料1.1.1供试品白花丹石油醚部位(A)、三氯甲烷(B)、乙酸乙酯(C)、水饱和的正丁醇(D)、水部位(E)均自备。1.1.2试剂RPMI1640、DMEM(低糖),购自Gibco;小牛血清,购自成都哈里;胰蛋白酶,购自Gibco;MTT、DMSO,购自Sigma公司。1.1.3癌细胞株乳腺癌细胞株(mda…     

HPLC法测定云南不同产地白花丹的不同部位中白花丹醌的含量

目的:建立白花丹药材中白花丹醌的反相高效液相色谱测定方法,以分别考察云南不同产地白花丹药材的不同部位中白花丹醌的含量。方法:色谱柱为 Kromasil C_(18)柱(250 mm×4.6 mm,5μm),流动相为甲醇-水(70:30),流速为1.0mL·min~(-1),检测波长为254 nm,柱温为25℃。结果:白花丹醌在25.3～253μg·mL~(-1)范围内,具有良好的线性关系,r=0.9998;平均回收率为99.0%,RSD=1.4%(n=6)。不同产地白花丹药材地上部分的白花丹醌含量分别为0.046%(嘎洒),0.079%(勐养),0.134%(嘎东),0.032%(曼东),0.047%(曼阁),0.057%(曼老);根部的白花丹醌含量分别为0.842%(嘎洒),1.04%(勐养),1.44%(嘎东),0.763%(曼东),0.639%(曼阁),1.97%(曼老)。结论:本法简便、准确,灵敏度高,重复性好,可用于控制白花丹药材质量。     

Antimicrobial activities of neo- and 1-epineo-isoshinanolones from Plumbago zeylanica roots

Context: The roots of Plumbago zeylanica Linn. (Plumbaginaceae) are reputed to have a wide spectrum of therapeutic properties in the Ayurvedic system of medicine. They are useful in curing many ailments such as skin diseases, diarrhea, plague and leprosy.

Objective: The study was aimed at isolating, separating and evaluating the antimicrobial properties of compounds such as neoisoshinanolone and 1-epineo-isoshinanolone from the roots of P. zeylanica.

Materials and methods: The crude petroleum ether extract of roots of P. zeylanica was subjected to repeated chromatographic techniques to separate compounds 2 and 3 along with plumbagin. Structure elucidation was carried out using nuclear magnetic resonance (NMR), infra red (IR) and mass spectroscopy. The serial dilution method was used to test antimicrobial activities and their minimum inhibitory concentration (MIC) expressed in µg/mL.

Results: 1-Epineo-isoshinanolone is more active with a MIC of 12.5-25 µg/mL whereas neoisoshinanolone has recorded a MIC of 50-100 µg/mL. The activities are compared with plumbagin (0.78-3.13 µg/mL) and standards streptomycin for bacteria and nystatin for fungi.

Discussion: Earlier researchers have established the presence of plumbagin in the roots of P. zeylanica and its antimicrobial activities. The structure elucidation of two more biologically active biogenetic precursors along with their activities in the root extracts has been established for the first time in the present study.

Conclusion: The root extract of P. zeylanica possesses good antimicrobial activity, which suggests its therapeutic use in the Ayurvedic system of medicine to cure skin diseases.     

Bioassay-guided isolation of anti-inflammatory and antinociceptive compound from Plumbago zeylanica leaf

Plumbago zeylanica Linn. (Plumbaginaceae) is used in the treatment of various inflammatory ailments in traditional medicines. In order to validate these ethnobotanical practices, the anti-inflammatory and antinociceptive activities of various leaf extracts (petroleum ether (60–80°), chloroform, acetone, ethanol, and aqueous) were studied using in vivo experimental models at two dose levels (200 and 400?mg/kg, p.o.). Anti-inflammatory activity was tested using the carrageenan induced rat hind paw edema method while analgesic activity was studied using the hot plate and formalin induced models. Diclofenac (100?mg/ kg) was used as the reference standard in both anti-inflammatory and analgesic models and morphine (10?mg/ kg, i.p.) was used as the reference standard in the formalin induced analgesic model. The acetone extract significantly (p?<?0.01) reduced inflammation in the rats when compared to the control group. As for the analgesia effect, the acetone and petroleum ether extracts significantly (p?<?0.01) decreased the pain stimulus only in the later phase of the formalin test, suggesting that the drug could be peripherally acting. Bioassay-guided fractionation of the acetone extract led to the isolation and identification of plumbagin. Structure elucidation of plumbagin confirmed it as 5-hydroxy-2-methyl-1,4-naphthoquinone, a naphthaquinone derivative, through spectral techniques.     

Oral Glutamine Attenuates Cyclophosphamide-Induced Oxidative Stress in the Bladder but Does Not Prevent Hemorrhagic Cystitis in Rats

Cyclophosphamide (CP) is widely used in the treatment of cancer and non-malignant disease states such as rheumatoid arthritis. Hemorrhagic cystitis is a major dose-limiting side effect of CP. The incidence of this side effect is related to the dosage and can be as high as 75%. Elimination of the side effects of CP can lead to better tolerance of the drug, and a more efficient therapy can be achieved for patients in need of CP treatment. Several studies have demonstrated that oxidative stress and neutrophil infiltration play important roles in CP-induced bladder damage. Glutamine is utilized under clinical conditions for preventing chemotherapeutic drug-induced side effects, based on its ability to attenuate oxidative stress. The aim of the study is to verify whether glutamine prevents CP-induced oxidative stress and bladder damage using a rat model. Adult male rats were administered 150 mg/kg body weight of CP intraperitoneally. Glutamine pretreated rats were administered 1 g/kg body weight of glutamine orally 2 h before the administration of CP. Vehicle/glutamine-treated rats served as controls. All the rats were killed 16 h after the dose of CP/vehicle. The urinary bladders were removed and used for light microscopic and biochemical studies. The markers of oxidative stress including malondialdehyde content, protein carbonyl content, protein thiol, and myeloperoxidase activity, a marker of neutrophil infiltration, were measured in bladder homogenates. CP treatment induced hemorrhagic cystitis in the rats. Pretreatment with glutamine significantly reduced CP-induced lipid peroxidation (p < 0.01), protein oxidation (p < 0.01), and increase in myeloperoxidase activity (p < 0.05). However, it did not prevent CP-induced bladder damage. The results of the present study show that glutamine pretreatment does not attenuate CP-induced hemorrhagic cystitis, although it prevents CP-induced oxidative stress and neutrophil infiltration significantly. It is therefore necessary to clarify the utility of glutamine as a chemoprotective agent before it is recommended in the market as a nutrient supplement.     

Antihyperlipidemic effect of aqueous extract of Plumbago zeylanica roots in diet-induced hyperlipidemic rat

This study examined the antihyperlipidemic effect of the aqueous extract of Plumbago zeylanica Linn. (Plumbaginaceae) roots in diet-induced hyperlipidemic rats. The oral administration of the aqueous extract at the dose of 20, 40, and 80?mg kg^?1 were found to ameliorate the hyperlipidemic condition as evidenced by a reduction of cholesterol and triglyceride levels. The standards fenofibrate (20?mg kg^?1) and atorvastatin (8?mg kg^?1) were also found to exhibit significant (p?<?0.05) cholesterol and triglyceride lowering effect. Further, the aqueous extract at all doses demonstrated a significant (p?<?0.05) increase in fecal cholesterol excretion indicating a reduction in intestinal cholesterol absorption. Additionally, the activity of lipogenic enzymes like HMGCoA reductase in the liver remained significantly (p?<?0.05) low on treatment of aqueous extract (80?mg kg^?1), thus decreasing the cholesterogenesis. The aqueous extract (20, 40 and 80?mg kg^?1) also significantly (p?<?0.05) reduced the total lipid content in the liver. Moreover, the aqueous extract demonstrated a potential antioxidant capacity in DPPH and TBARS in vitro antioxidant assay. Thus the results suggest a beneficial role of aqueous extract of Plumbago zeylanica roots in ameliorating the hyperlipidemic condition leading to atherosclerosis.     

In Vivo Micronucleus Assay and GST Activity in Assessing Genotoxicity of Plumbagin in Swiss Albino Mice

Information available on the mutagenicity of a large number of indigenous drugs commonly employed in the Siddha and Ayurveda systems of medicine is scanty. In this context, the current investigation on plumbagin, 5-hydroxy-2methyl-1,4-napthoquinone, an active principle in the roots of Plumbago zeylanica used in Siddha and Ayurveda for various ailments, was carried out; 16 mg/kg b.w. (LD₅₀) was fixed as the maximum dose. Subsequent dose levels were fixed as 50% and 25% of LD₅₀ amounting to 8 mg and 4 mg/kg b.w., respectively, and given orally for 5 consecutive days in 1% Carboxyl Methyl Cellulose (CMC) to Swiss albino mice weighing 25–30 g. The micronucleus assay was done in mouse bone marrow. Plumbagin was found to induce micronuclei at all the doses studied (4 mg/kg, 8 mg/kg, 16 mg/kg b.w.), and it proves to be toxic to bone marrow cells of Swiss albino mice. Animal treated with cyclophosphamide (40 mg/kg b.w.) served as positive control. In addition, glutathione S-transferase (GST) activity was observed in control, plumbagin (4 mg, 8 mg, 16 mg/kg b.w., respectively), and genotoxin-treated experimental group of animals. No significant change in GST activity was observed with plumbagin dose of 4 mg/kg b.w., whereas GST activity was significantly inhibited by higher doses of plumbagin (8 mg and 16 mg/kg b.w.) and cyclophosphamide.     

Protective Effect of Nardostachys jatamansi Against Radiation-induced Damage at Biochemical and Chromosomal Levels in Swiss Albino Mice

The effect of 100 mg of ethanol extract of Nardostachys jatamansi was studied on the mice exposed to 6 Gy electron beam radiation. Treatment of mice with 100 mg of Nardostachys jatamansi extract for 15 days before irradiation reduced the symptoms of radiation sickness when compared with the nondrug treated irradiated groups. The irradiation of animals resulted in an elevation in lipid peroxidation and reduction in glutathione, total antioxidants and antioxidant enzymes such as glutathione peroxidase and catalase activities. Irradiated group had shown micronucleus in the bone marrow cells. Treatment of mice with Nardostachys jatamansi extract before irradiation caused a significant depletion in lipid peroxidation followed by significant elevation in reduced glutathione, total antioxidants, glutathione peroxidase and catalase activity. It also showed a reduction in the micronucleus formation in the bone marrow cells. Our results indicate that the radioprotective activity of Nardostachys jatamansi extract may be due to free radical scavenging and increased antioxidant level in mice.     

ICP-OES法测定不同栽培条件下白花丹茎中的无机元素

目的 测定不同栽培条件下白花丹茎样品中无机元素的含量.方法 采用微波肖解和电感耦合等离子体发射光谱法(ICP-OES)同时测定白花丹茎中的无机元素.结果 栽培条件对白花丹茎中无机元素的含量影响较大,且大都降低其无机元素的含量;栽培能大幅降低白花丹茎中As、Pb、Cd、Cr等重金属元素的总含量.结论 从减少重金属元素含量的角度分析,白花丹的栽培条件为:繁殖选用种子苗或扦插苗、植被条件选用全光照、施肥选用钾肥、土壤条件选择黏土.     

Induction of Anti-inflammatory and Altered T-Cell Proliferative Responses by the Ethanol Root Extract of Plumbago zeylanica. in Adjuvant-Induced Arthritic Rats

ABSTRACT

The ethanol root extract of Plumbago zeylanica. L. (PZE) was investigated for anti-inflammatory activity in adjuvant-induced arthritic (AIA) rats. The AIA rats were treated with PZE (20 mg/kg body weight) daily from day 0 to day 13. The PZE reduced the paw thickness and paw volume of AIA rats. The effect of PZE treatment was assessed in cutaneous delayed type hypersensitivity (DTH) response to Mycobacterium. tuberculin (MT) in development of AIA. The results demonstrated that PZE inhibited the development of cutaneous DTH response in AIA rats. The T-cell proliferation induced by concanavalin A (Con A), a mitogen, was depressed in three different strains of AIA rats (Wistar, Lewis, and Fischer) when compared with that of normal; however, the PZE treatment of AIA rats reversed the decrease of T-cell proliferation to the normal levels. The treatment of AIA rats with PZE on splenic T-cell proliferation was also compared with T-cell proliferation of rats that were treated with the known anti-inflammatory compounds such as cyclophosphamide and indomethacin.     

Protection by Black Tea Extract Against Chromosome Damage Induced by Two Heavy Metals in Mice

The efficacy of infusion of black tea leaf, Camellia sinensis (Linn.) O.Kuntze (Theaceae), in reducing the cytotoxic effects of two heavy metal salts, chromium and arsenic, was tested in bone marrow cells of mice following dietary administration. Mice were given black tea infusion by gavage twice daily, in concentrations simulating human consumption, for 6 days. On day 7 after treatment with tea, separate sets of mice were given single doses of potassium dichromate and sodium arsenite, and then killed after 24 h. Control sets were treated with potassium dichromate or sodium arsenite separately and also observed after 24 hours. The concentration of each salt corresponded to 1/10th of its LD 50 value. Chromosomes were studied from bone marrow cells following the usual colchicine-hypotonic-fixation-air-drying Giemsa schedule. Both metallic salts were highly clastogenic when given alone, inducing a high frequency of chromosomal aberrations as compared with d istilled water. Tea alone, given twice daily for 6 days, was not clastogenic. When mice, given tea twice daily for previous 6 days, were treated with either of the two salts on day 7, the degree of chromosome damage induced was reduced significantly as compared with the salts given alone. This reduction was more significant for sodium arsenite as compared with potassium dichromate. Such protection against arsenic cytotoxicity by prolonged dietary administration of black tea infusion is of importance in view of the widespread exposure of human populations to arsenic damage through drinking water from tubewells in West Bengal, India and adjoining Bangladesh.     

Antigenotoxic effect of the Plumbago zeylanica extract against the genotoxic damage induced by potassium canrenoate in cultured human peripheral blood lymphocytes

In India, natural preparations derived from the plants are widely use for the treatments of various diseases. Hence, it becomes necessary to assess the modulating action of the plant extract when associated with other substances. Potassium canrenoate (PC) is a synthetic steroid and is used in the treatment of hypertension. It is not only a genotoxic agent, but also a tumor-initiating agent. In the present study, the effect of various doses (i.e., 5, 10, 20, and 30 µM) of PC were studied for their genotoxic effects in the presence of S9 mix in cultured human lymphocytes, using mitotic index, chromosomal aberrations, sister chromatid exchanges, and replication index as parameters. PC was found to be genotoxic at 20 and 30 µM. Treatment of 30 µM of PC was given along with different doses of Plumbago zeylanica extract (i.e., 107.5, 212.5, 315, and 417 µg/mL) of the culture medium. A dose-dependent decrease in the genotoxic effects of PC was observed. The result suggested that the plant extract per se does not have genotoxic potential, but can modulate the genotoxicity of PC in cultured human lymphocytes.     

Protective effect of Plumbago zeylanica against cyclophosphamide-induced genotoxicity and oxidative stress in Swiss albino mice

Plumbago zeylanica, commonly known as white leadwort, found abundantly in the plains of Bengal and southern India, was tested for its possible in vivo protective effect against cyclophosphamide-induced genotoxicity and oxidative stress in Swiss albino mice. Pretreatment with the alcoholic root extract of Plumbago zeylanica (250 and 500 mg/kg body weight orally for 5 days) significantly reduced the frequency of micronucleated polychromatic erythrocytes (MnPCEs), increased the PCE/NCE (normochromatic erythrocyte) ratio in the bone marrow, and decreased the levels of lipid peroxidation products with concomitant changes in the status of antioxidants. Both doses of Plumbago zeylanica were effective in exerting a protective effect against cyclophosphamide-induced genotoxicity and oxidative stress.     

N-乙酰半胱氨酸对糖尿病模型小鼠氧化应激的影响研究

目的:探讨N-乙酰半胱氨酸(NAC)对糖尿病模型小鼠氧化应激的影响。方法:取小鼠腹腔注射链脲佐菌素建立糖尿病模型,建模成功8周后随机分为非治疗组和NAC治疗组(200mg·kg-1.d-1),每组6只,腹腔注射相应药物,每日1次,连续4周,另设正常对照组进行比较。检测各组小鼠给药前后体重、血糖水平及给药后尿液中脂质过氧化标志物8-异前列腺素(8-Isoprostane)浓度。结果:与正常对照组比较,非治疗组和NAC治疗组小鼠给药前后体重均明显降低,血糖均明显升高(P<0.001),但2组间比较无显著性差异;与非治疗组比较,NAC治疗组小鼠尿液中8-Isoprostane浓度明显降低(P<0.01),且与正常对照组比较无显著性差异。结论:NAC可有效改善糖尿病模型小鼠的氧化应激状态。     

Antifertility Activity of Stems of Plumbago rosea in Female Albino Rats

In the present study, Plumbago rosea Linn. (Plumbaginaceae), one of the folk medicinal plants commonly used as an antifertility agent, was evaluated for its antifertility effect. Five successive solvent extracts, petroleum ether, chloroform, acetone, ethanol, and water extracts, of the stems of P. rosea were studied on estrous cycle at two dose levels, 200 and 400 mg/kg respectively. Of these, the acetone extract was found to be most effective in interrupting the normal estrous cycle of rats (p < 0.05) (p < 0.01). The rats exhibited prolonged diestrous stage of the estrous cycle with consequent temporary inhibition of ovulation. The antiovulatory activity was reversible on withdrawal of the extract. The effective acetone extract was further studied on estrogenic functionality in rats. The acetone extract showed significant estrogenic and antiestrogenic activity (p < 0.05) (p < 0.001). Histological studies of the uteri further confirmed the estrogenic activity of acetone extract. The results indicated the antifertility activity of stems of Plumbago rosea in female Wistar rats.     

Myrica nagi Attenuates Cumene Hydroperoxide‐Induced Cutaneous Oxidative Stress and Toxicity in Swiss Albino Mice

In recent years, considerable efforts have been made to identify new chemopreventive agents which could be useful for man. Myrica nagi, a subtropical shrub, has been shown to possess significant activity against hepatotoxicity and other pharmacological and physiological disorders. We have shown a chemopreventive effect of Myrica nagi on cumene hydroperoxide‐induced cutaneous oxidative stress and toxicity in mice. Cumene hydroperoxide treatment at a dose level of 30 mg/animal/0.2 ml acetone enhances susceptibility of cutaneous microsomal membrane for iron‐ascorbate‐induced lipid peroxidation and induction of xanthine oxidase activity which are accompanied by decrease in the activities of cutaneous antioxidant enzymes such as catalase, glutathione peroxidase, glutathione reductase, glucose‐6‐phosphate dehydrogenase and depletion in the level of cutaneous glutathione. Parallel to these changes a sharp decrease in the activities of phase II metabolizing enzymes such as glutathione S‐transferase and quinone reductase has been observed. Application of Myrica nagi at doses of 2.0 mg and 4.0 mg/kg body weight in acetone prior to that of cumene hydroperoxide (30 mg/animal/0.2 ml acetone) treatment resulted in significant inhibition of cumene hydroperoxide‐induced cutaneous oxidative stress and toxicity in a dose‐dependent manner. Enhanced susceptibility of cutaneous microsomal membrane for lipid peroxidation induced by iron ascorbate and xanthine oxidase activities were significantly reduced (P<0.05). In addition the depleted level of glutathione, the inhibited activities of antioxidants, and phase II metabolizing enzymes were recovered to a significant level (P<0.05). The protective effect of Myrica nagi was dose‐dependent. In summary our data suggest that Myrica nagi is an effective chemopreventive agent in skin and capable of ameliorating cumene hydroperoxide‐induced cutaneous oxidative stress and toxicity.     

槲皮素对糖尿病视网膜病变小鼠氧化应激损伤和炎症反应的影响

目的：探讨槲皮素对糖尿病视网膜病变（DR）的保护作用及其抗氧化和抗炎机制。方法： 腹腔注射链脲佐菌素（STZ）建立小鼠糖尿病模型,随机分为正常对照组、造模组、槲皮素治疗组（n = 10）。治疗后定期监测小鼠精神状态、血糖、体重;检测小鼠视网膜结构变化、超氧化物歧化酶（SOD）活性、8-羟基脱氧鸟苷（8-OHdG）、丙二醛（MDA）、肿瘤坏死因子-α（TNF-α）、白介素-6（IL-6）、白介素-β（IL-β）的mRNA等水平。结果：与造模组相比,槲皮素降低小鼠血糖（P ＜ 0.05）,小鼠体重无明显差异（P ＞ 0.05）,视网膜细胞排列整齐,厚度增加;视网膜组织中8-OHdG、MDA、TNF-α mRNA、IL-6 mRNA、IL-β mRNA、Bax及p-p38 MAPK蛋白表达指数显著降低（P ＜ 0.05）,T-SOD活力和Bcl-2蛋白表达水平明显升高（P ＜ 0.05）,但各组p38 MAPK蛋白表达水平无明显差异（P ＞ 0.05）。结论： 槲皮素改善2型糖尿病小鼠视网膜组织氧化应激损伤和炎症反应,其机制可能与p38 MAPK信号通路有关。     

白花丹不同有机溶剂提取物和白花丹醌对移植性乳腺癌和S180肉瘤的作用

目的初步了解白花丹不同有机溶剂提取物和白花丹醌对BALB/C小鼠移植性EMT-6乳腺癌及KM小鼠移植性S180的作用。方法用动物移植性肿瘤在体实验法。结果①氯仿1g·kg-1剂量组、白花丹醌0.02g·kg-1组可抑制EMT-6乳腺癌在BALB/C小鼠体内生长,与生理盐水组比较,瘤重明显减轻(P<0.05),其抑制率分别为34.2%和41.2%。②氯仿1g·kg-1、0.5g·kg-1剂量组,石油醚1g.kg-1、0.5g·kg-1剂量组,乙酸乙酯1g·kg-1、0.5g·kg-1剂量组均可抑制S180肉瘤在KM小鼠体内生长,与生理盐水组比较,瘤重明显减轻(P<0.05或<0.01),其中以氯仿1g·kg-1剂量组抑制率最高(P<0.01),达55.6%。结论白花丹氯仿提取物、石油醚提取物、乙酸乙酯提取物和白花丹醌有一定抑制移植性EMT-6乳腺癌和S180肉瘤的作用,值得进一步深入研究。