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A new chalcone glucoside, androechin, and a known flavone glucoside, echioidinin 5-O-glucoside, were isolated from the whole plant of Andrographis echioides. Androechin was characterized as 2,2',6'-trihydroxy-4'-methoxychalcone 2'-O-beta-D-glucopyranoside by spectral and chemical studies.
A new flavone glucoside, 5,2',6'-trihydroxy-7-methoxyflavone 2'-O-beta-D-glucopyranoside has been isolated from the whole plant of Andrographis alata. The structure was elucidated on the basis of spectral and chemical evidence.
1. The hypotensive activity of an aqueous extract of Andrographis paniculata was studied using chronic intraperitoneal (i.p.) infusions by osmotic pumps. The extract exhibited a dose-dependent hypotensive effect on the systolic blood pressure (SBP) of spontaneously hypertensive rats (SHR). 2. The optimum hypotensive dose determined was repeated in a study in SHR and their normotensive controls, Wistar-Kyoto (WKY) rats, to demonstrate its comparative effects on the SBP, plasma and lung angiotensin-converting enzyme (ACE) activities, as well as on lipid peroxidation in the kidneys, as measured by the thiobarbituric acid (TBA) assay. 3. The extract significantly lowered the SBP of both SHR and WKY rats. 4. Plasma, but not lung, ACE activity and kidney TBA level were significantly lower in extract-treated SHR when compared with vehicle-treated SHR controls. 5. Plasma and lung ACE activities as well as kidney TBA levels were not significantly different between extract- and vehicle-treated WKY rats. 6. This study indicates that the aqueous extract of A. paniculata lowers SBP in the SHR possibly by reducing circulating ACE in the plasma as well as by reducing free radical levels in the kidneys. The mechanism(s) of hypotensive action seems to be different in WKY rats.
The methanol extract of the aerial part of Andrographis paniculata Nees showed potent cell differentiation-inducing activity on mouse myeloid leukemia (M1) cells. From the ethyl acetate-soluble fraction of the methanol extract, six new diterpenoids of ent-labdane type, 14-epi-andrographolide (3), isoandrographolide (4), 14-deoxy-12-methoxyandrographolide (7), 12-epi-14-deoxy-12-methoxyandrographolide (8), 14-deoxy-12-hydroxyandrographolide (9) and 14-deoxy-11-hydroxyandrographolide (10) as well as two new diterpene glucosides, 14-deoxy-11,12-didehydroandrographi-side (12) and 6'-acetylneoandrographolide (14), and four new diterpene dimers, bis-andrograpolides A (15), B (16), C (17) and D (18), were isolated along with six known compounds. The structures of the diterpenoids were determined by means of spectral methods. Some of these compounds showed potent cell differentiation-inducing activity towards M1 cells.
Two new 2'-oxygenated flavones, 5,2',6'-trihydroxy-7-methoxyflavone (3) and skullcapflavone I 2'-O-beta-D-(4"-E-cinnamyl) glucopyranoside (5), together with three known flavones, 7-O-methylwogonin (1), skullcapflavone I (2) and skullcapflavone I 2'-O-beta-D-glucopyranoside (4) were isolated from the whole plant of Andrographis elongata, and the structures were elucidated by FAB-MS and one- and two-dimensional (1D- and 2D)-NMR spectral studies including 1H-1H correlation spectroscopy (COSY), heteronuclear single quantum coherence (HSQC), heteronuclear multiple bond connectivity (HMBC) and rotating frame Overhauser enhancement spectroscopy (ROESY) experiments, and chemical studies.
OBJECTIVE: To observe the effects of Andrographis Paniculata component (API0134) on nitric oxide (NO), endothelin (ET), cyclic guanosine monophosphate (cGMP), lipid peroxide (LPO) and superoxide dismutase (SOD) in experimental atherosclerotic rabbit. METHODS: An atherosclerotic rabbit model was established by feeding high cholesterol diet supplemented by bovine serum albumin injection bolus. The rabbits were randomly divided into the control, model, and API0134 treated group. Blood samples were collected before 4 weeks and 8 weeks after relevent treatment. RESULTS: Before 4 and after 8 weeks API0134 administration, compared with model group, the NO, cGMP and activity of SOD increased (P < 0.01), while LPO and ET decreased (P < 0.01). CONCLUSIONS: API0134 possesses the effects of antioxidation, preserving endothelial function, and maintaining the balance of NO/ET.
Andrographis paniculata (AP) treatment prevents BHC induced increase in the activities of enzymes y-Glutamyl transpeptidase, glutathione-S-transferase and lipid peroxidation. The activities of antioxidant enzymes like superoxide dismutase, catalase, glutathione peroxidase and the levels of glutathione were decreased following BHC effect. Administration of AP showed protective effects in the activity of superoxide dismutase, catalase, glutathione peroxidase, glutathione reductase as well the level of glutathione. The activity of lipid peroxidase was also decreased. The result indicate antioxidant and hepatoprotective action of A. paniculata.
AIM: To investigate the anti-diabetic effect of a crude ethanolic extract of Andrographis paniculata in normal and streptozotocin (STZ)-induced diabetic rats. METHODS & RESULTS: Oral administration of the extract at different doses (0.1, 0.2, and 0.4 g/body weight) significantly reduced the fasting serum glucose level in STZ-diabetic rats compared to the vehicle (distilled water), but not in normal rats. This effect was dose-dependent. A similar result was seen with metformin (0.5 g/body weight). In the glucose tolerance test, an oral administration of the extract at the same doses suppressed the elevated glucose level in normal and diabetic rats, as did metformin. The effects were also dose-respondent. In the long-term experiment, the extract (0.4 g/body weight), metformin (0.5 g/body weight), and vehicle were given twice daily to diabetic rats for 14 d. On d 15, fasting serum glucose levels were found to be significantly lower in the extract- and metformin-treated groups (P < 0.001) than in the vehicle-treated group. The mean food and water intakes over 14 days were significantly lower in the extract-treated group (P < 0.05, P < 0.01, respectively) and also in the metformin-treated group (both P < 0.001) when compared to the vehicle-treated group. No significant change in insulin level was observed among the 3 groups of diabetic rats. The extract, like metformin, maintained the leptin levels after 14-d treatment, whereas this level was significantly decreased (P < 0.05) in the vehicle-treated group. The activity of hepatic glucose-6-phosphatase (G-6-Pase) was significantly reduced by the extract as well as by metformin (both P < 0.05). No significant difference in hepatic glycogen stores was noted among the 3 groups. The extract caused 49.8% reduction of fasting serum triglyceride levels, compared to 27.7% with metformin. However, neither the extract nor metformin significantly affected serum cholesterol level. CONCLUSION: The ethanolic extract of A paniculata possesses antidiabetic property. Its antidiabetic effect may be attributed at least in part to increased glucose metabolism. Its hypotriglyceridemic effect is also beneficial in the diabetic state.
In 16 dogs the endothelium of the left anterior descending coronary artery was injured mechanically. Then a copper wire was inserted into the lumen as a choke of flow and the vessel was slightly compressed from outside by a constrictor. Eight dogs had been treated beforehand with a preparation of flavone extracted from the root of the Chinese medicinal herb Andrographis paniculata (TFAP). In the control group, saline solution was given, the epicardially recorded ST segment started to elevate within 15 minutes, the platelet aggregation rate and the plasma levels of TXB2 increased rapidly, whereas the level of 6-k-PGF1 alpha remained stable. Platelet cGMP rose continuously; however, platelet cAMP rose only at 60 minutes. Histological findings confirmed the occurrence of arterial thrombus and myocardial necrosis. Contrariwise, in the pretreated group there was no elevation of the ST segment, plasma 6-k-PGF1 alpha and platelet cAMP were increased, the production of TXB2 and aggregation of platelets were inhibited, and no thrombus or myocardial infarction was induced. All data suggest that TFAP might promote the synthesis of PGI2, inhibit the production of TXA2, stimulate the synthesis of cAMP in platelets, impede aggregation of platelets, and thereby prevent the formation of thrombi as well as the development of myocardial infarction.
Andrographis paniculata (Burma) Wall. ex Ness (AP) is a herbal medicine and has been used for therapy of upper respiratory tract infection (URI) as well as acute diarrhea with reported efficacy of 75-100 per cent. To investigate whether anti-bacterial activity was responsible for the reported therapeutic success of AP, we carried out a number of studies. The first study was a direct assay of anti-bacterial activity of AP suspended in water. The tested pathogens included Salmonella, Shigella, E.coli, gr. A Streptococci and S.aureus. Anti-bacterial activity was not demonstrable even in a solution containing 25,000 mg per litre of crude powder. The second was designed to detect serum bactericidal activity after oral intake of stem and leaves of AP. Ten healthy volunteers were enrolled in the study. They received a single oral dose of AP (1, 2, 3 and 6 g) in a randomized, cross-over manner. The washout period was one week. Blood samples were taken at 0, 1, 2, 4, 8 and 24 hours after ingestion. Serum bactericidal activity was assayed by agar diffusion technique using Bacillus spores and five strains of each pathogen (Shigella, Salmonella typhi, S.aureus and gr. A Streptococci) incubated for 24 hours. Again serum bactericidal activity was not detected in any of the sera tested. In a third study, ninety-six rats were daily fed with high doses of AP ranging 0.12-24 g per kg body wt. for six months before sacrifice. Antibacterial activity was still undetectable when lung parenchyma and liver tissue was placed on culture media containing bacteria tested. In conclusion, anti-bacterial activity of AP is undetectable in our study.
Antifertility effect of Andrographis Paniculata (AP) was observed in mice under different experimental conditions. When sun-dried powder of AP was mixed with animal's food (Rats Pelletts) in a dose of 2G per Kg. B.W. per day and was allowed to consume by the female mice daily for a period of six weeks, none of the animal (100%) were pregnant when mated with the male of proven fertility who did not receive the drug. On the other hand, the majority of the control female mice (95.2%) who did not receive the drug were pregnant when mated with the similar type of male as in the experimental group, and they continued to give birth to litters of usual size and number (average 5-6) for subsequent six matings.
So far known Andrographis paniculata Nees (AP) is a hepatoprotective, antiplatelet and antithrombotic drug. In this experiment its hypoglycaemic effect has been tried in various way. Water extract of AP 10 mg/kg body weight can prevent induction of hyperglycaemia significantly (P < 0.001) induced by oral administration of glucose 2 mg/kg body weight. But any how failed to do so in adrenaline induced hyperglycaemia. It also failed to demonstrate any "fasting blood sugar lowering effect" upon chronic administration (6 weeks) of AP. So probably AP prevents glucose absorption from gut. Whole experiment was done on rabbits.
Restenosis rate after coronary angioplasty has been up to 30%-40%. To solve this problem, we studied the effects of Andrographis Paniculata Nees (APN) and fish oil (FO, omega 3 polyunsaturated fatty acids over 70%) on atherosclerotic stenosis and restenosis after experimental angioplasty and the relevant mechanisms of APN and FO. Preliminary results showed that APN can significantly alleviate atherosclerotic iliac artery stenosis induced by both deendothelialization and high cholesterol diet (HCD) and restenosis following angioplasty in rabbits. FO showed the same but milder effects than APN did. Both APN and FO significantly inhibited blood monocytes to secrete growth factors in vivo. Ca(++)-ATPase activity of cell membrane of atherosclerotic rabbits was significantly decreased, while APN or FO, especially the former alleviated this reduction. Refined extract of APN significantly decreased in vitro resting platelet [Ca++]i and in vivo the resting and thrombin-stimulated platelet [Ca++]i after oral administration of APN for 2 weeks. APN significantly inhibited cell growth or DNA synthesis in dose-dependent manner. In conclusion because of the mechanisms described above, APN can alleviate atherosclerotic artery stenosis induced by both deendothelialization and HCD as well as lower restenosis rate after experimental angioplasty. The effects of APN are evidently superior to those of FO.
63 patients of cardiac and cerebral vascular diseases were observed at 3 hours and/or one week after taking Andrographis paniculata (AP) extracts. Results showed that both 1 min. and 5 min. platelet aggregation induced by ADP were significantly inhibited (P < 0.001), 33 cases of them were observed for one week. The aggregation rate was even significantly lower than that of 3 hours. Serotonin (5-HT) release reaction from platelet was observed in 20 volunteers taking AP. Result showed 5-HT released from platelet decreased (P < 0.01), but plasma 5-HT level remained unchanged. The ultrastructural observation showed that AP could inhibit the releasing of dense and alpha agranules from platelet and dilating of canalicular system. It suggested that a raise of platelet cAMP level might be the mechanism of antiplatelet effect of AP.
Studies were performed to investigate the prohormone/proprotein convertase (PC)-inhibitory properties of chemical constituents of the medicinally active plant Andrographis paniculata (AP; from the family Acanthaceae), also known as 'King of Bitters'. Among the individual components tested against the clinically important convertases, furin and PC1, neoandrographolide (a C3 O-glucoside derivative of the major constituent andrographolide) exhibited the highest inhibitory action with an IC50 of 53.5 microM against furin. The data further revealed that although andrographolide, the major bitter principle of AP, exhibited a relatively small enzyme inhibition (IC50=1.0 mM and Ki=200 microM against furin), upon succinoylation, its inhibitory action against the above convertases was enhanced significantly with a Ki in the low micromolar range (<30 microM), suggesting that a specific structural modification of the andrographolide skeleton may be exploited to develop a new class of non-peptide inhibitors of PCs. When tested against PC7, these succinoylated derivatives of andrographolide also displayed strong inhibitory action, with Ki values again in the low micromolar range. This potentially interesting observation may be attributed to the reported anti-HIV property of 14-dehydroandrographolide succinic acid monoester (DASM). It is suggested here that DASM, by virtue of this protease inhibitory property, possibly acts by suppressing the proteolytic cleavage of envelope glycoprotein gp160 of HIV, which is known to be PC-mediated, particularly by furin and PC7.
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The present paper describes the development of a microemulsion electrokinetic chromatographic (MEEKC) method for simultaneous determination of andrographolide and dehydroandrographolide in traditional Chinese medicines and Chinese medicinal preparations. The MEEKC method involved the use of sodium dodecyl sulfate (SDS) as surfactant, heptane as organic solvent and butan-1-ol as co-solvent. The effect of temperature and pH of running buffers on separation were examined. The optimized conditions (heptane 0.81% (w/w), SDS 3.31% (w/w), butan-1-ol 6.61% (w/w) and 10mM sodium tetraborate buffer, pH 9.2) allowed a useful and good reproducible separation of the studied analytes to be achieved.
The protective effect of Andrograhis paniculata and andrographolide (ANDLE) against cyclophosphamide (CTX)-induced urothelial toxicity was investigated in this study. Pretreatment of Swiss albino mice with A paniculata extract (10 mg/dose/animal intraperitoneally [ip]) and ANDLE (500 microg/dose/animal ip) could significantly reduce CTX (1.5 nmol/kg body weight)-induced urothelial toxicity. Morphological and histopathological analysis of urinary bladder of CTX-treated mice showed severe inflammation and dark coloration, whereas A paniculata and ANDLE-treated mice showed almost normal bladder morphology. Elevation of urinary protein level (7.33 +/- 0.3 g/L) by CTX administration was reduced by A paniculata (3.78 +/- 0.4 g/L) and ANDLE treatment (4.19 +/- 0.1 g/L). Urinary urea N2 level, which was elevated after 48 hours of CTX administration (24.25 +/- 0.2 g/L) was found to be reduced by the treatment with A paniculata (14.19 +/- 0.5 g/L) and ANDLE (15.79 +/- 0.4 g/L). A decreased level of reduced glutahione (GSH) content in liver (2.81 +/- 0.1 nmol/mg protein) and bladder (1.20 +/- 0.2 nmol/mg protein) after CTX administration was also increased by the treatment with A paniculata (liver: 5.78 +/- 0.3 nmol/mg protein; bladder: 2.96 +/- 0.2 nmol/mg protein) and ANDLE (liver: 5.14 +/- 0.3 nmol/mg protein; bladder: 2.84 +/- 0.2 nmol/mg protein). Production of the proinflammatory cytokine, tumor necrosis factor-alpha, which was elevated during CTX administration, was found to be inhibited by A paniculata and ANDLE treatment. The lowered level of interleukin-2 and interferon-gamma during CTX treatment was elevated by the administration of A paniculata and ANDLE.