Kustha (Saussurea Lappa)

Recent Research on Kustha

• This study was performed to investigate the potential use of Saussurea lappa C.B. Clarke as a source of antioxidant agents. Various solvent fractionates from S. lappa C.B. Clarke roots were investigated for their antioxidative effectiveness. Study shows that the S. lappa C.B. Clarke plant may help prevent antioxidative stress. Chang KM, Choi SI, Kim GH. Antioxidant Activity of Saussurea lappa C.B. Clarke Roots. Prev Nutr Food Sci. 2012 Dec; 17 (4): 306- 9. doi: 10. 3746/ pf. 2012. 17. 4. 306.
• The cardiac activity of Saussurea lappa roots was evaluated in isolated perfused rabbit hearts by Langendorff’s technique. Heart rate, contractility, and coronary flow were determined in the presence of different concentrations of methanolic extract of Saussurea lappa, digoxin, and diltiazem. Saussurea lappa roots contain certain pharmacologically active compounds that could be involved in the cardiotonic activity of the extract. Akhtar MS’, Bashir S, Malik MN, Manzoor R. Cardiotonic activity of methanolic extract of Saussurea lappa Linn roots. Pak J Pharm Sci. 2013 Nov. 26 (6): 1197- 201.
•  The antimicrobial activity of the ethanol extract of the Auklandia (Saussurea lappa) root plant was investigated to verify its medicinal use in the treatment of microbial infections. The results demonstrated that the crude ethanolic extract of the Auklandia (Saussure lappa) root plant has a wide spectrum of activity suggesting that it may be useful in the treatment of infections caused by the above clinical isolates (human pathogens). Hasson SS’, AI-Balushi MS, Alharthy K, Al-Busaidi JZ, Aldaihani MS, Othman MS, Said EA, Habal O, Sallam TA, Aljabri AA, Ahmedidris M. Evaluation of anti-re resistant activity of Auklandia (Saussurea lappa) root against some human pathogens. Asian Pac J Trop Biomed, 2013 Jul; 3 (7): 557- 62. doi 10. 1016/ S2221-1691 (13) 60113- 6.
• To explore potential chemotherapeutic effects and mechanism of cell growth inhibition of Saussurea lappa on human oral cancer cells. The results suggested that S. lappa extract inhibited cell proliferation through the apoptosis pathway in KB human oral cancer cells. Moon SM’, Yun SJ, Kook JK, Kim HJ, Choi MS, Park BR, Kim SG, Kim BO, Lee SY, Ahn H, Chun HS, Kim Does K, Kim CS. Anticancer activity of Saussurea lappa extract by an apoptotic pathway in KB human oral cancer cells. Pharm Biol. 2013 Nov; 51 (11): 1372- 7. doi: 10. 3109/ 13880209. 2013. 792847. Epub 2013 Jul 16.
• Five sesquiterpenes, dehydrocostus lactone (1), santamarine (5), betacyclocostunolide (6), 4- alpha- hydroxy- 4- beta- methyl- dihydrocostol (7), and 10-  alpha- hydroxyl-artemisinic acid (9), along with four other com-pounds, beta-sitosterol (2), daucosterol (3), 5-  hydroxy- methyl- furaldehyde (4), and transsyingin (8), were isolated and identified from the roots of Saussurea lappa (Compositae). Duan JA’, Hou P, Tang Y, Liu P, Su S, Liu H. A new sesquiterpene and other constituents from Saussure lappa root. Nat Prod Commun. 2010. Oct; S (10): 1531- 4.
• The essential oil of kuth roots has strong antiseptic and disinfectant properties, especially against Strep. and Staphyl. It has marked carminative properties. It inhibits peristaltic movements of the gut and produces relations. Injection of the essential oil produces vasodilatation in the splanchnic area and prosorbed from the G.I.T. and partly excreted by the lungs producing an expectorant action; partly by the kidneys producing a diuretic action (Chopra, 1958).
• Delactonized oil and some lactone fractions of the oil exhibit hypotensive, spasmolytic, and broncho dilatory effects (Chopra, 1958, Dutta, 1960).
• The effect of different fractions was studied with very minimum doses i.e.; Img (Solvent ether, petroleum ether, and chloroform extract) and 1 mg (water soluble and alcoholic extract) on frog’s heart. There was no appreciable response to the heart rate, contractility, and tone up to the dose of 2mg. The dose was gradually increased to Sm (solvent ether, P.E., and Chloroform) and 100mg (water-soluble alcoholic extract) and a better response was observed, which showed a decrease in heart rate, contractility, and tone. These observations suggest that the drug has got -ve iconography, geography, and choreography. While comparing the effect with standard drugs, it was found that the drug has got direct depressant action as the action was not blocked by atropine and also suggest that it was acting through the Muscranic receptor (Upadhyay, 1986).
• Anthelmintic activity of S. lappa was established by Kokate, in 1986.
• In a study on the pharmacological and therapeutic evaluation of S. lappa, it was found to be effective in cardiovascular diseases (Dwivedi, et al; 1987).
• Its powder enhanced the aortic prostaglandin E, (PGEz) like- activity in experimental rabbits (Dwivedi et al., 1987).
• Patel, Ayyub & Mohammed, Amanullah & Elsaid, Fahmy & Eissa, Mohamed & Alothaid, Hani. (2021). In-Vitro evaluation of the anti-cancer and genotoxic potential of medicinal herb Saussurea lappa extract in human cancer cell lines. For centuries, plants have been known to play part in the daily routine from providing food to the management of human health. During the last few decades, diverse phytochemicals have been characterized as agents that possess the potential to execute cancer cells. The oil extracted from the root of Saussurea costus has been used in traditional medicine for a long time. Purpose: This study was carried out to assess the effect of Saussurea lappa aqueous extract on five different cell lines; Human Lung Fibroblast cells (MRC5), Human Dermal Fibroblast adult (HDFa), Madin-Darby Canine Kidney cells (MDCK), breast cancer cells (MCF7) and human colonic cancer (Caco2). Results: On normal cell lines; the extract showed cytotoxic activities with the half maximal inhibitory concentration; IC50 values, ranging from 0.85 to 2.5 mg/ml whereas MRC5 was the most sensitive cell line (IC50 values: 0.85). On malignant cell lines, MCF7 cells showed inhibition in cell proliferation with activity from 67.17% to 91.01% by the extract treatment concentration of 0.50 to 2.0 mg/dl. However, Caco2 cells exhibited inhibition in proliferation ranging from 37.10% to 69.45% by the same treatment dose. Thus, breast cancer cells were more sensitive than colon cancer cells to Saussurea costus extract. The genotoxic potentialities of the crude extract showed an increase in the expression of proapoptotic genes; P53, IκBα, BAX, and TNF, and a decrease in the expression of antiapoptotic genes; Bcl2, Survivin, and MMP-7. Conclusion: Our work pointed out that Saussurea lappa extract could be a potential candidate that can fight cancer.
• Alotaibi, Amal & Bepari, Asmatanzeem & Assiri, Rasha & Niazi, Shaik K. & Nayaka, Sreenivasa & R, Muthuraj & K N, Shashiraj & Bhat, Meghashyama. (2021). Saussurea lappa Exhibits Anti-Oncogenic Effect in Hepatocellular Carcinoma, HepG2 Cancer Cell Line by Bcl-2 Mediated Apoptotic Pathway and Mitochondrial Cytochrome C Release. Current Issues in Molecular Biology. 43. 1114- 1132. 10. 3390/ cimb  43020079. Background and Objectives: Saussurea lappa (S. lappa) is an important species of the Asteraceae family with several purposes in traditional medicine. This study intended to explore the cytotoxic effect of S. lappa on HepG2 cancer cell proliferation. Materials and Methods: The effects of an S. lappa n-butanol extract on the induction of apoptosis were investigated by flow cytometry and mitochondrial cytochrome C-releasing apoptosis assay. Additionally, real-time PCR was employed to confirm apoptosis initiation. Further, qualitative estimation of the active constituent of S. lappa was done by gas chromatography-mass spectroscopy (GC–  MS). Results: The cell viability study revealed that the n-butanol extract of S. lappa demonstrated potent cytotoxicity against HepG2 cancer cells, with an IC50 value of 56.76 μg/mL. Cell morphology with dual staining of acridine orange (AO)- ethidium bromide (EB) showed an increase in orange/red nuclei due to cell death by S. lappa n-butanol extract compared to control cells. Apoptosis, as the mode of cell death, was also confirmed by the higher release of cytochrome C from mitochondria, the increased expression of caspase-3 and bax, along with down-regulation of Bcl-2. Conclusion: These findings conclude that S. lappa is a cause of hepatic cancer cell death through apoptosis and a potential natural source suggesting furthermore investigation of its active compounds that are responsible for these observed activities.
• The effect of its root (S. radix in China) on gastrointestinal motility was tested by its ability to enhance charcoal meal transport in mice. The 25 mg/kg of acetone extract on oral administration, significantly enhanced gastrointestinal motility. Dehydro costus was purified from the acetone extract as an active principle (Yamahara, 1990)
• Five new amino acid- sesquiterpene adducts, sausurea-mines A, B, C, D, E, F, were isolated from the root, together with a new lignan glycoside, (-) massoni- resinol 4- 0- beta – D- ghecopyvanoside. Among these, A, B, and C fractions showed an anti-ulcer effect on Hcl/ethanol-induced lesions in roots, and Saussure amine A also exhibited inhibitory activity on stress-induced ulcer formation in mice, (Yoshikawa et al., 1993).
• Lim, Hye-Sun & Jin, Sung-Eun & Kim, Ohn-Soon & Shin, Hyeun-Kyoo & Jeong, Soo-Jin. (2015). Alantolactone from Saussurea lappa Exerts Anti-inflammatory Effects by Inhibiting Chemokine Production and STAT1 Phosphorylation in TNF- and IFN- induced in Haacht cells. Phytotherapy research: PTR. 29. 10. 1002/ ptr. 5354. Skin inflammation is the most common condition seen in dermatology practice and can be caused by various allergic reactions and certain toxins or chemicals. In the present study, we investigated the anti-inflammatory effects of Saussurea lappa, a medicinal herb, and its marker compounds alantolactone, caryophyllene, costic acid, costunolide, and dehydrocostuslactone in the HaCaT human keratinocyte cell line. HaCaT cells were stimulated with tumor necrosis factor-alpha (TNF-α) and interferon-gamma (IFN-γ), and treated with S. lappa or each of five marker compounds. Chemokine production and expression were analyzed by enzyme-linked immunosorbent assay and reverse transcription-polymerase chain reaction, respectively. Phosphorylation of signal transducer and activator of transcription (STAT) 1 was determined by immunoblotting. Stimulation with TNF-α and IFN-γ significantly increased the production of the following chemokines: thymus-regulated and activation-regulated chemokine (TARC): regulated on activation, normal T-cell expressed and secreted (RANTES): macrophage-derived chemokine (MDC): and interleukin-8 (IL- 8). By contrast, S. lappa and the five marker compounds significantly reduced the production of these chemokines by TNF-α and IFN-γ-treated cells. S. lappa and alantolactone suppressed the TNF-α and IFN-γ-stimulated increase in the phosphorylation of STAT1. Our results demonstrate that alantolactone from S. lappa suppresses TNF-α and IFN-γ-induced production of RANTES and IL-8 by blocking STAT1 phosphorylation in HaCaT cells.
• The aqueous extract was administered orally, and the effect was compared to clofibrate. The lipid-lowering property was highly significant (P> 0.001) (Upadhyay, 1994). (10). It contains essential oil which is partly excreted from the urine. During the passage of urine through the urethra, the presence of the oil causes considerable irritation, which can give rise to a somewhat painful erection. Hence it is claimed to be an aphrodisiac agent (Johan, 1997).
• Effect of S. lappa on smooth muscle alkaloids from Muxiang (S. Radix) has a strong inhibitory effect on histamine-induced bronchospasm and intestinal spasm in guinea pigs. Chemical extracts from this herb have anti-spasmodic, bronch0- dilatory and blood pressure lowering effects similar to, but weaker than papaverine (Internet, 1997).
• Sutar, Niranjan & Garai, Ranju & Singh, Nrendra & Deb Roy, Saumendu. (2011). The antiulcerogenic activity of Saussurea lappa root. INTERNATIONAL JOURNAL OF PHARMACY & LIFE SCIENCES. 2. 516- 520. The study was designed to investigate the antiulcer activity of ethyl acetate extract of the Saussurea lappa root using different models of gastric and duodenal ulceration in rats. Gastric ulcers were induced by oral administration of ethanol, aspirin, and by pyloric ligation, and duodenal ulcers were induced by oral administration of cysteamine HCl. The extract was administered at a dose of 200 and 400 mg/kg orally 30 min before ulcer induction. Ranitidine (50 mg/kg) was used as a reference standard. The antiulcer activity was accessed by determining and comparing the ulcer index in the test group with that of the standard drug-treated group. Gastric volume, total acid, and free acid were estimated in the pylorus-ligated rats. Saussurea lappa root (400 mg/ kg) showed maximum inhibition of gastric acid, free acid, and total acid to 53.54%, 52.55%, and 30.30%, respectively. The ulcer index in the Saussurea lappa root-treated animals was found to be significantly less in all the models compared to standard drug-treated cases. The antiulcer activity of Saussurea lappa root was, however, less than that of ranitidine. The results suggest that Saussurea lappa root possesses a significant antiulcer property which could be due to the cytoprotective action of the drug or the strengthening of gastric and duodenal mucosa with the enhancement of mucosal defense.
• Molecular analysis of cross-reactions in cost- sensitive patients revealed that the most active sesquiterpene lactones are the ones with the lesser no. of oxygenated subtitles. It has been suggested that a mixture of lactones with different skeletons be used to screen sesquiterpene lactone sensitivity in patients with contact dermatitis (Benezra, C. Cu Epstein, W.L., 1986).
• Kushta Cuozijasara was administered separately for two groups of patients 500 mg and 100 ml (decoction) each for 30 days. It was found that both are effective in the management of Madhumeha (D.M.) No. side-effects were observed (Singh, D. C. & Sharma, B. P., 1990).
• A preliminary clinical trial on IHD suggests significant improvement in clinical and biochemical parameters after 4 months of treatment. The results were compared to these of the section group. The combination of Kushta and segontin is more effective and suitable without the occurrence of any major side effects. The dose of segontin could be reduced in combined drug therapy in comparison to the segontin group. The side effects were also less in the combined group (Udadhyay, 1993).
• Chandur, Uma & Shashidhar, Shrusti & Chandrasek, S.B. & Bhanumathy, M. & Midhun, T. (2011). Phytochemical Evaluation and Anti-Arthritic Activity of Root of Saussurea lappa. Pharmacologia. 2. 265- 267. 10. 5567/pharmacology. 2011. 265. 267. Background: Saussurea lappa is a well-known Indian medicinal plant used in the indigenous systems of medicine for the treatment of inflammatory conditions. Materials and Methods: The petroleum ether, chloroform, and alcoholic extracts of the Saussurea lappa roots in the presence of chemically active compounds by standard methods and evaluated for their antiarthritic activity by using Complete Freund’s Adjuvant (CFA) induced rat model. Results: The results revealed the presence of alkaloids, carbohydrates, flavonoids, glycosides, phenolic compounds, saponins, and tannins. Application of all three extracts exhibited significant (p<0.01) edema inhibition when compared with the arthritic control group. Conclusion: The results obtained suggest that Saussurea lappa root extracts are endowed with effective antiarthritic activity. These findings seem to justify the use of the plant in traditional Indian medicine in the treatment of inflammation, including arthritic conditions.
• Chang, Kyung-Mi & Choi, Soo-Im & Chung, Sophia & Kim, Gun-Hee. (2011). Antimicrobial Activity of Saussurea lappa C.B. Clarke Roots. Preventive Nutrition and Food Science. 16. 10. 3746/ jfn. 2011. 16. 4. 376. We investigated the total phenolic and flavonoid contents and the antimicrobial activity of ethanol extracts obtained from Saussurea lappa C.B. Clarke. The ethanol extracts of S. lappa C.B. Clarke was fractionated with various solvents (n-hexane, chloroform, and n-butanol). The antimicrobial activity of S. lappa C.B. Clarke was examined by disc-diffusion and micro-dilution susceptibility assays with six food-borne pathogens, and compared to that of the synthetic antibiotics. It is found that the S. lappa C.B. Clarke ethanol extract and n-hexane fraction have strong activity against B. cereus and V. parahaemolyticus strains compared to ampicillin. The inhibitory concentration () values of hexane fraction against L. monocytogenes, B. cereus, and B. subtilis were 62.5, 250, and 500 ppm, respectively. Therefore, these data suggest that S. lappa C.B. Clarke may be useful as an antimicrobial agent against food-borne pathogens.
• Deabes, Mohamed & Aboulthana, Wael & El-Din, Emad & Marzouk, M & Ibrahim, Mohamed & Ahmed, Kawkab. (2021). Evaluation of Hepato-and Neuroprotective Effect of Chemical Constituents in Saussurea costus Extracts against the Toxicity Induced by Chlorpyrifos Ethyl in Rats. Egyptian Journal of Chemistry. 64. 631-647. 10.21608/EJCHEM.2021.55840.3199. The health hazards occurring in both humans and animals as a result of the continuous misuse of pesticides drives researchers to look for a solution. Natural plant extracts contain active Phyto-constituents with antioxidant potency enabling them to inhibit the production of the free radicals that induce damage to the cells. The present study aimed to reveal the efficiency of Saussurea costus (S. costus extract) against the hepato-and neurotoxicity induced by Chlorpyrifos ethyl (CPF) in experimental animals (rats). The gas chromatography/mass spectrometer (GC/MS) used for analyzing the active constituents in S. costus extract showed that the extract contains 11 potent active compounds and Dehydrocostuslactone represents about 77.37% and is considered the most dominant compound in the extract. Both CPF and S. costus extract were studied on the rats that were divided into 6 groups as the following: Group 1 (control) received distilled water orally. Group 2&3 (S. costus extract treated groups) received S. costus extract orally at a dose of 0.25 and 0.50 ml, respectively. Group 4 (CPF injected group) was injected with CPF at a dose of 3 mg/ kg. bw. Groups 5& 6 (CPF + S. costus extract group) were injected with CPF and then treated with S. costus extract at two tested doses respectively. Most hematological and biochemical measurements declined significantly (P≤0.05) in the CPF injected group. S. costus extract restored all tested parameters toward the control values. Moreover, the electrophoretic isoenzyme showed that the physiological alterations that occurred in the esterases (ESTs) as a result of CPF injection were represented by hiding normal EST types associated with the existence of abnormal ones. Therefore, the similarity index (SI%) and genetic distance (GD%) values were altered with α-EST (SI= 80.00%; GD= 20.00%) and β-EST (SI= 50.00%; GD= 50.00%) patterns in CPF injected group. The S. costus extract at a dose of 0.5 ml restored the integrity of these isoenzyme patterns by restoring the absent types while hiding the abnormal ones. Therefore, this group became physiologically similar to the control group (SI=  100.00%; GD= 0.00%). These results were supported by histopathological examination for the target organs (brain, liver, and kidney) that were affected by CPF, and the S. costus extract improved the architecture of these organs and restored their histopathological integrity to the normal structure.
• Chang, Kyung-Mi & Choi, Soo-Im & Kim, Gun-Hee. (2012). Antioxidant Activity of Saussurea lappa C.B. Clarke Roots. Preventive nutrition and food science. 17. 306- 9. 10. 3746/ pnf. 2012. 17. 4. 306. This study was performed to investigate the potential use of Saussurea lappa C.B. Clarke as a source of antioxidant agents. Various solvent fractionates from S. lappa C.B. Clarke roots were investigated for their anti-oxidative effectiveness. The contents of total phenolics and flavonoids were determined by the Folin- Ciocalteu’s colorimetric and the aluminum nitrate method, respectively. Total phenolic and flavonoid contents of n-butanol soluble fractionate from S. lappa C.B. Clarke, 44.43 μg gallic acid equilibrium (GAE)/g extract and 92.15 μg quercetin equilibrium (QE)/g extract, respectively, were higher than those of other solvent fractionates. The n-butanol soluble fractionates of S. lappa C.B. Clarke (1,000 ppm) showed the strongest inhibitory potential on 2,2- diphenyl- 1- picrylhydrazyl (DPPH) radicals and reducing power at 92.98% and 0.38, respectively. Thus, our data show that the S. lappa C.B. Clarke plants may help prevent antioxidative stress.
• Trikushta guggulu containing C. mukul and S. lappa is given to 30 patients of osteoarthritis (Sandhigata vata) at a 2 gm TDS dose for 60 days. Clinical improvement was noticed in stiffness, pain, swelling, and tenderness within 2-3 weeks of treatment. Joint movements became less painful. A marked reduction in average body weight was observed after 60 days of treatment. Totally 10% of cases got complete relief, 13.4% marked relief, 50% moderate relief, and 6.7% cases no relief (Sand, B.N. & Kumari, K., 1994).
• It has shown a significant effect in reducing the blood sugar levels of obese diabetics (Upadhyay O.P. et al., 1996).
• Yeesh, Sheikh & Jamal, Qamar & Shah, Abdul & Gilani, Anwar-ul. (2010). Antihepatotoxic Activity of Saussurea lappa Extract on D-galactosamine and Lipopolysaccharide-Induced Hepatitis in Mice. Phytotherapy research: PTR. 24 Suppl 2. S229- 32. 10. 1002/ ptr. 3089. The effects of aqueous-methanol extract of Saussurea lappa Clarke root (Sl. Cr) were investigated against D-galactosamine (D- GalN) and lipopolysaccharide (LPS)-induced hepatitis in mice. Co-administration of D- GalN (700 mg/kg) and LPS (1 micron/kg) significantly raised the plasma transaminase levels (ALT/AST) as compared to the control group (p < 0.05). Pretreatment of mice with different doses of Sl. Cr (150, 300, and 600 mg/kg) significantly prevented the D- GalN and LPS-induced rise in plasma levels of ALT and AST in a dose-dependent manner (p < 0.05). Post-treatment with Sl. Cr (600 mg/kg) significantly restricted the progression of hepatic damage induced by D- GalN and LPS (p < 0.05). The improvement in plasma enzyme levels was further verified by histopathology of the liver, which showed improved architecture, absence of parenchyma congestion, decreased cellular swelling, and apoptotic cells in treatment groups as compared to the toxin group of animals. These data indicate that the Sl. Cr exhibits hepatoprotective effects in mice and this study rationalizes the traditional use of this plant in liver disorders.
• Krishna Dutta Tejaswi, Juluri & Rajan, Govinda & Sara, Picq. (2018). BIOLOGICAL EVALUATION OF SAUSSUREA LAPPA ROOT EXTRACT FOR ANALGESIC AND ANTI- INFLAMMATORY ACTIVITY. Asian Journal of Pharmaceutical Research and Development. 6. 35- 38. 10. 22270/award. v6i4. 378. The present study was designed to evaluate the Phytochemical Screening for Analgesic and Anti-inflammatory activities of the Ethonolic extract of Saussurea lappa. The collected plant root material was washed, shade dried, and size reduced into small pieces. Dried materials were coarsely powdered and macerated with petroleum ether for 72 hrs. The plant material was extracted by using ethanol by the cold maceration method. The study concluded that the root extract has potential bioactive substances that may be used to formulate new drugs. The Flavo-Glycosides content in the Ethonolic extract of Saussurea lappa root was extracted and results were compared with the standard for Analgesic and Anti-inflammatory activities. The results were compared with the standard using statistical methods. However further investigation was required for structural elucidation and pharmacological properties. Keywords: Saussurea lappa, Ethonolic, Glycosides, Analgesic, Anti-inflammatory.
• Two active components costunolide and hydro costus lactone, show a strong suppressive effect on the expression of Hepatitis B Surface Antigen (HBSAg) in human hepatoma Hep 3 B cells, but have little effect on the viability of the cells. Both fractions suppress HBsAg production by Hep 3 B cells in a dose-dependent manner with IC 50s of 1.0 and 2.0 micro-H, respectively. (Chen, H.C. et al., 1995).