 Gen info
• Crassocephalum is a genus in the family Asteraceae, with common names of members include ragleaf, thickhead, and bologi. The genus is typically thistle-like in appearance, but all parts are soft and not spiny.
(41)
• Crassocephalum crepidioides use is widespread in many tropical and subtropical regions. The safety for internal use needs further study due to presence of plant toxins. (see studies below)
Botany
• Borbotak is an erect annual slightly succulent little-branched herb growing up to 1 meter tall. Leaves are fleshy and mucilaginous. and many parts of the plant have medical uses. Flower heads are cylindrical, green, with red florets visible on top. Seeds are floating balls of numerous silky white hairs.
• Plants erect, 20-120 cm tall. Stems striate, glabrous. Leaf petiole 2-2.5 cm; blade elliptic or oblong-elliptic, 7-12 × 4-5 cm, membranous, both surfaces glabrous or subglabrous, base cuneate, margin irregularly serrate or double-serrate, sometimes pinnately lobed at base, apex acuminate. Capitula several to numerous in terminal corymbiform cymes, shortly pedunculate, 3-5 mm in diam. Involucres cylindric, 1-1.2 cm, basally truncate, with few unequal linear bracteoles; bracts of calyculus 6-21, 2-6 mm; phyllaries uniseriate, linear-lanceolate, equal, ca. 1.5 mm wide, margin narrowly scarious, apically puberulent. Florets tubular, bisexual; corolla red-brownish or orange, rarely yellow, 8-10 mm; lobes 5, ca. 1 mm. Style branches acute, papillose. Achenes brownish, narrowly oblong, 1.8-2.3 mm, ribbed, hairy. Pappus 7-13 mm, early deciduous. (Flora of China)
Distribution
- Introduced to the Philippines.
- Naturalized.
- Throughout the Philippines, generally at low to medium elevation. Common roadside weed, in waste places, abandoned cultivation, forest clearings, etc., at 800-1400 m. (28)
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Native to much of Africa.
- In tropical Asia, found in the Indian subcontinent (Bhutan, India, Nepal, Pakistan, Sri Lanka), Indo-China (Cambodia, Laos, Myanmar, Thailand, Vietnam) and Malesia (Indonesia, Malaysia, Papua New Guinea, and the Philippines).
 Constituents
- Phytochemical screening yielded tannins, coumarins, combined anthracene derivatives, C-heterosides, flavonoids, mucilage, reducing compounds and steroids. (5)
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Study of essential oil of roots yielded 47 compounds, representing 93.2 % of the total oil. The main constituents were were (E)-β-farnesene (30.6%), α-humulene (10.3%), β-caryophyllene (7.2%), cis-β-guaiene (6.1%) and α-bulnesene (5.3%). The oil was constituted mainly of sesquiterpene hydrocarbons (77.6%), followed by oxygenated sesquiterpenes (8.7%), oxygenated monoterpenes (3.5%), monoterpene hydrocarbons (2.8%) and phenyl derivatives (0.6%). (4)
- Essential oil of flowers and aerial parts yielded monoterpene hydrocarbons (82.0%; 70.8%) with myrcene (45.3%; 46.1%), β-phellandrene (20.2%; 31.0%) as major constituents. Flower oil also yielded dauca-5,8-diene (6.9%), trans-β-farnesene (4.8%) and daucene 3.6%), while the aerial parts yielded allo-aromadendrene (4.9%), α-muurolene (2.6%) and β-panasinsene (2.4%). (8)
- Essential oil of leaves yielded α-caryophyllene (10.29 %), β-cubebene (13.77 %) and α-farnesene (13.27 %) as major constituents, while stem oil yielded thymol (43.93 %), α-caryophyllene (15.16 %) and 4-cyclohexybutyramide (20.94 %) as dominant constituents. (7)
 - Leaves yield per 100 g of edible portion: water 79.9%, energy 268 kJ (64 kcal), protein 3.2 g, fat 0.7 g, carbohydrate 14.0 g, fiber 1.9 g, calcium 250 mg, phosphorus 52 mg.
(Leung, W.-T.W., Busson, F. & Jardin, C., 1968). (10)
- Study of leaves for secondary metabolites yielded gallic tannins, cathetic tannins, flavonoids, steroids,mucilage, coumarins, reducing compounds, and combined anthracene derivatives C-heterosides. (12)
- Water extract of C. crepidioides yielded isochlorogenic acids, quercetin and kaempferal glycoside as active components. (see study below) (15)
- Phytochemical screening of leaves yielded polyphenol compounds (gallic tannins, cathetic tannins, flavonoids), steroids, mucilage, coumarins, reducing compounds, and combined anthracene derivatives C-heterosides. (see study below) (5)
- Nutrient and proximate analysis of powdered stems and leaves revealed: moisture 10.16%, crude protein 15.09%, lipid 2.48%, ash
13.15%, crude fiber 13.27%, carbohydrate 56.01%, and food energy value 306.72 Kcal/100g. Mineral composition yielded: calcium 105.09 mg/kg, sodium 64.86 mg/kg, potassium 791.40 mg/kg, magnesium 20.34 mg/kg, iron 1.92 mg/kg, manganese 2.16 mg/kg,, with zinc, lead, copper, and selenium in range between 0.09 to 0.14 mg/kg. The powdered sample contained flavonoid, phenol, oxalate, tannin, saponin, phytate, and ascorbic acid, with absence of alkaloid. (37)
Toxicity concern
- Crassocephalum crepidioides contains hepatotoxic and tumorigenic pyrrolizidine alkaloid, jacobin.
- See studies below (29) (30)
Properties
- Wound healing, anti-diarrheal.
- Studies have shown anti-tumor, antioxidant, antidiabetic, hepatoprotective, radical scavenging, wound healing, nephroprotective, anti-inflammatory, immunomodulatory, non-genotoxic, anti-dyslipidemic, anti-atherogenic, anticoagulant, anti-anemic properties.
Parts used
Leaves, stems, flowers, essential oil.
 Uses
Edibility
- Fleshy, mucilaginous leaves and stems are eaten raw or cooked. Leaves have a nutty flavor.
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In Africa, fleshy mucilaginous leaves and stems are eaten as vegetable.
- A highly consumed leafy vegetable in Benin.
- In Nigeria, lightly blanched leaves are cooked with pepper, onions, tomatoes, melon, and fish or meat to makes soups and stews. In Sierra Leone, leaves are grounded into paste to make a sauce.
- In Thailand, roots eaten with chili sauce. (13)\
Folkloric
- In India, Nepal and China, plant used for wound healing and to treat diarrhea.
- In Gbolo used as antimicrobial, anti-diabetic and anti-inflammatory.
- In Nigeria, leaf decoction used for headache, indigestion, stomach aches.
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In Tanzania, a mixture of leaf sap of C. crepidioides and Cympogon giganteus used orally and externally for treatment of epilepsy. Also, leaf powder used as snuff to stop nose bleeds and smoked to treat sleeping sickness. (3)
- In southern Nigeria, leaves used to treat indigestion. In the Congo, leaf sap used to treat stomach upsets. In Uganda, leaf sap used to treat fresh wounds. In Tanzania, dried leaf powder used as snuff to stop nose bleeding and smoked to treat sleeping sickness. Roots used to treat swollen lips. (10)
- In Bangladesh, plant decoction used as lotion for headache and stomach pains. Juice taken to treat constipation and other stomach disorders. (21)
- In Cóte d'Ivoire, leaf preparation by anal enema used to facilitate childbirth. (23)
Others
- Fodder: Plants used by livestock; also useful green fodder for poultry. (10)
- Plant trap: Used as plant trap to collect adult corm weevils in banana plantations. (13)
Studies
• Anti-Tumor: Study evaluated the in vitro and in-vivo antitumor activities of C. crepidioides on murine Sarcoma 180 (S-180) and related mechanisms. Results showed oncolytic and immunopotentiation properties mediated through NF-kB-induced release of NO from macrophages. (2)
• Renal Histo-Toxic Effects: Study evaluated the effects of oral consumption of aqueous leaf extract of Crassocephalum crepidioides on the frontal cortex, kidney, liver and testes of Sprague Dawley rats. Results showed no deleterious effect on the cytoarchitecture of the frontal cortex, liver and testes. Histopathological alterations were observed characterized by histological damage to kidneys of the rats which may be the result of direct toxicity, effect of released of toxic substances from other organs, or deleterious effects of a plant phytochemical. Results suggest further studies to isolate the specific component responsible for the kidney toxicity. (3)
• Cytotoxicity Testing: Cytotoxicity testing was done using the brine shrimp lethality bioassay. LC50 value of leaf extract showed to be 0.901 mg/ml indicating non-toxicity. (see constituents above) (5)
• Hepatoprotective / Free Radical Scavenging: Study showed C. crepidioides to be a potent antioxidant and protective against galactosamine (GaIN) plus liposaccharide (LPS)- or CCl4-induced hepatotoxicity. Isochlorogenic acids, quercetin and kaempferol glycosides were identified as active components. (6)
• Antibacterial: Study evaluated the antibacterial activity of hot aqueous extract of C. crepidioides and C. odorata against three bacterial isolates i.e., S. aureus, K. pneunonia, and E. coli. All three were sensitive to both, however K. pneumonia was most sensitive to C. crepidioides with MIC of 15 mg/ml while S. aureus was most resistant. (11)
- Toxicity Study as Leafy Vegetable: Study based on LC50 and toxicity table showed non of the species of vegetable Gboli investigated was toxic to shrimp larvae as their LC50 are greater than 0.1 mg/ml. Taking in account established correlation between toxicity of shrimp larvae and that of human cells, study suggests the two species of Gbolo can be considered as leafy vegetable with no risk of toxicity. (12)
• Renal Effects: Study evaluated the effects of oral consumption of aqueous leaf extract of Crassocephalum crepidioides on frontal cortex, kidney, liver and testes of Sprague Dawley rats using anatomical studies. Results showed no deleterious effects on the cytoarchitecture of the frontal cortex, kidney, liver, and testes of rats. It showed histophathological changes in the kidneys of treated rats suggesting it may affect the functional activities of the kidney. Authors suggest isolation of specific components responsible for renal toxicity to standardize plant preparations for maximum culinary and therapeutic benefits. (14)
• Antioxidant / Hepatoprotective: Study evaluated the free radical scavenging and protective actions of Crassocephalum crepidioides against chemically induced hepatotoxicity. Results showed C. crepidioides is a potent antioxidant and hepatoprotective against GaIN plus LPS- or CCl4-induced hepatotoxicity. (see constituents above) (15)
• Anti-Diabetic / B-Cell Protection: Study in Wistar albino mice evaluated the B-cell protection and anti-diabetic activities of Crassocephalum crepidioides by pancreatic B-cell culture and α-amylase inhibition technique. Results showed significant (p<0.05, p<0.01) effect on hyperglycemia compared to standard (Gliclazide) in OGTT. Plant showed efficient protection of pancreatic B-cell death in INS-1 cell line by significantly reducing levels of alloxan-induced apoptosis and intracellular ROS accumulation. (16)
• Cadmium Accumulation / Phytoremediation Potential: C. crepidioides has been identified as a cadmium accumulator plant in heavy-metal polluted environment. Study showed the plant has strong potential for use in phytoremediation in farm fields contaminated with Cd. (17)
• Anthelmintic / Leaves: Study evaluated the in vitro anthelmintic activity of aqueous leaf extract of C. crepidioides against Haemonchus contortus on three development stages. Results showed concentration-dependent anthelmintic activity. Levamisole (500 µg/ml) killed 100% worms while the plant exhibited only 16.67% inhibition at highest concentration (2400 µg/ml). Activity may be due to secondary metabolites i.e., saponins, flavonoids, and tannins in the extract. (18)
• Antioxidant / Antihyperlipidemic / Aerial Parts: Study evaluated the antioxidant and antihyperlipidemic activities of methanol extract of aerial parts of C. crepidioides. Results showed significant dose-dependent antioxidant activity. In high-fat diet induced hyperlipidemic rats, the extract significantly reduced (p<0.01 or 0.001) serum TC, TG, LDL-c and VLDL-c, and significantly (p<0.05) serum HDL-c level. (19)
• Antibacterial / Brine Shrimp Lethality / Essential Oil: Study evaluated essential oil of C. crepidioides for antibacterial activity and brine shrimp lethality. Brine shrimp lethality assay showed the essential oil of stem (LC50 9.10 µg/ml) was as toxic as the EO of leaves (LC50 9.2 µg/ml). The EOs were active against all test bacterial strains, although of lower activity compared to standard gentamicin. Main constituents of leaf essential oil were α-caryophyllene (10.29%) and ß-cubebene (13.77%) while stem EO were mainly thymol (43.93%) and 4-cyclohexybutyramide (20.94%). (22)
• Local Anesthetic Effect
/ Leaves: Study of a methanol extract using different experimental animal models showed significant local anesthetic property in intracutaneous wheal method in guinea pigs and in lumbar plexus anesthesia method in frogs. (24)
• Effect of Blanching on Antioxidant and Anticholinesterase Properties: Study investigated the effect of blanching on phenolic distribution and in vitro antioxidant and anticholinesterase properties of HCl-methanolic extract. Blanching decreased the antioxidant and anticholinesterase properties, as evidenced by a reduction/loss of polyphenolic content from the blanched fireweed. (25)
• Anthelmintic / Leaves: Study evaluated the in vitro anthelmintic activity of an aqueous leaf extract of Crassocephalum crepidioides against Haemonchus contortus. EHA (egg hatch assay) showed significant reduction reduction (p<0.05) on H. contortus egg hatch. Inhibition was concentration dependent. The anthelmintic activity may be due to secondary metabolites such as saponins, flavonoids, and tannins. (26)
• Acetylcholinesterase Inhibitory Property / Antioxidant: Study characterized the phenolic constituents and evaluated the acetylcholinesterase inhibitory effect and antioxidant properties of hydrophilic extract of redflower ragleaf. The extract was found rich in phenolic acids (chlorogenic acid and caffeic acid) and flavonoids (rutin and quercetin). The extract inhibited acetylcholinesterase activity in a dose-dependent manner and exhibited high antioxidant properties as evidenced by radical scavenging abilities, reducing property, Fe2+ chelating ability and inhibition of lipid peroxidation. Results suggest a source of phenolic phytochemicals with antioxidant and acetylcholinesterase inhibitory properties with potential for the treatment of Alzheimer's disease. (27)
• Acute and Subacute Toxicity Studies / Leaves: Study evaluated the acute and subacute toxicity of aqueous leaves extract of Cc using OECD guidelines for oral toxicity study. Lethal dose (LD50) was greater than 5,000 mg/kbw in rats. In subacute toxicity using doses of 250, 500, and 1,000 mg/kbw for 28 days, there was significant increase in body weight, food and water consumption with maximums of 15.14, 24.52, and 28.86% respectively at 1,000 mg/kbw. While there was no significant change in hematological parameters, significant changes were observed in biochemical parameters, along with structural changes in liver and kidneys of treated animals. Data suggest Cc could be safe in single administration, but has toxic effects in repeated treatment. (29)
• Toxic Pyrrolizidine Alkaloid Jacobine: Although the plant has beneficial properties, C. crepidioides can accumulate highly toxic pyrrolizidine alkaloid (PA) jacobine. Study investigated how jacobine production is controlled. Tetraploid C. crepidioides forms jacobine, an ability its diploid close relative C. rubens appears to lack. Nitrogen (N) deficiency or starvation strongly increases jacobine in the shoots and leaves of Cc. -- the consumed plant parts -- a capacity that depends more strongly on the shoot than root system, and homospermidine synthase (HSS) activity is not rate-limiting the reaction. Avoiding N shortage is one strategy to produce low-PA Cc plants; however, this may be difficult, if not impossible, to consistently implement in agricultural systems. Jacobine concentrations should be monitored to ensure safe use, a major challenge to producers. (30)
• Wound Healing / Leaves: Study evaluated the wound healing activity of C. crepidioides hydroethanolic leaf extract (CCLE) via its antioxidant and anti-inflammatory activities and healing capability on a mouse excision wound model. CCLE at dose of 50 mg/k/day reduced wound closure time and showed a 2.8-fold decrease in density of inflammatory cells, 1.9-fold increase in fibroblast density, and higher number of blood vessels. mRNA expression level of NF-kB1 and TNF-α mRNA in CCLE-treated wounds decreased 4.6 and 3.3 times, respectively, while TGF-ß1 and VEGF increased by 3.3 and 2.4 times, respectively. The wound healing activity was attributed to antioxidant, anti-inflammation, fibroblast proliferation, wound contraction, and angiogenesis effects. (31)
• Nephroprotective / Paracetamol-Induced Toxicity / Leaves: Study evaluated the protective effect of C. crepidioides methanol leaves extract against paracetamol (PCM)-induced oxidative stress in Wistar rats. PCM had no significant effect on serum creatinine and BUN levels, but significantly decreased glutathione levels, SOD, and catalase activities, with significantly increased activity of glutathione-S-transferase and malondialdehyde (MDA) level. Co-administration of the extract and acetylcysteine (NAC) reversed the effects. Study suggest Cc protects against PCM-induced oxidative stress in the kidneys of Wistar rats. (32)
• Anti-Inflammatory / Immunomodulatory / Antigenotoxic: Study evaluated Cc methanolic extract (CcME) for invitro anti-inflammatory, immunomodulatory, and invivo antigenotoxic properties. The CcME showed potent invitro anti-inflammatory activity by inhibition of NO, PGE-2, TNF-α, IL-1ß and IL-6 production in LPS treated murine RAW264.7 macrophage cell line. Immunomodulatory properties were evidenced by increase splenocyte proliferation index, elevated IgA and IgM, a delayed-type hyper-
sensitivity responses in footpad swelling test and lower level of cytokines (TNFα and IL-6) in systemic candidiasis challenged animal model. CcME exhibited no genotoxic effects. Instead CcME showed protection of DNA damage induced by cyclophosphamide. (33)
• Antioxidant / Lipoxygenase Inhibitory / Leaves: Study evaluated the anti-inflammatory and antioxidant effects of leaves of Cc through ABTS and anti-lypoxygenase activities. Extract showed good antioxidant effect with IC50 of 45.78 µg/mL with ascorbic acid as positive control at 41.56 µg/mL and anti-inflammatory activity with IC50 39.59 µg/mL. with indomethacin as positive control at 31.06 µg/mL. (34)
• Attenuation of Dyslipidemia and Atherogenic Indices / Leaves: Study evaluated the effects of aqueous (CAF) and hexane (CHF) fractions of C. crepidioides leaves on lipid profile and atherogenic indices of diabetic rats. The tested concentrations of CAF and CHF significantly (p<0.05) reduced plasma glucose (51.3-62.2%), plasma and liver triglycerides (up to 50,5% in plasma, 66.1% in liver), total cholesterol (up to 49.0% in plasma, 35.3% in liver), LDL-cholesterol (up to 96.0 and 91.0% in plasma and liver), VLDL (50.5% and 55.0%), and atherogenic indices elevated by diabetes induction. HDL levels were significantly increase. Histological exam showed improved tissue architecture in pancreas of diabetic-treated rats compared to control. Results showed hypolipidemic and anti-atherogenic activities with potential usefulness in management of diabetes, dyslipidemia, and cardiovascular conditions. (35)
• Modulation of Blood Coagulation and Hematological Parameters / Leaves: Study evaluated the effects of Cc leaf methanol extract and fractions on blood coagulation profile of diabetic Wistar rats. The ME and fractions of Cc at concentrations of 50, 100, and 200 mg/kg significantly prolonged bleeding (58-200%), clotting (65-133%), prothrombin (176-441%), and activated partial thromboplastin time (209-518%) in diabetic rats compared to control (LD50≥5000mg/kg). Plasma calcium concentration and platelet counts were significantly reduced (p<0.05). while RBC, Hb concentration, and PCV were significantly increased. Results showed anticoagulant and anti-anemic activities, with potential source of novel anticoagulant and nutraceutical for thrombotic disorders in diabetes. (36)
• Silver Nanoparticles / Antimicrobial / Leaves: Study reports on the green synthesis of silver nanoparticles using aqueous leaf extract of C. crepidioides. S1(1:50) AgNPs showed highest antibacterial activity against E. coli, S. aureus, and B. subtilis and less for antifungal activity towards C. albicans. (38)• Neuroprotective / Diazepam-Induced Amnesia / Leaves: Study evaluated the neuroprotective effects of ethanolic extract of C. crepidioides on diazepam-induced amnesia in mice. Memory effects were evaluated using RAM (Radial Arm Maze) and NOR (Novel Object Recognition) tests, while anti-depressive effects were evaluated using tail suspension test. The extract significantly (p<0.001) decreased the number of working and reference memory errors in the RAM test and significant (p<0.01) increase in time spent exploring the novel object in the NOR test. Extract also significantly (p<0.001) increase the mobility time in tail suspension. Histopathological analysis of hippocampi showed increased cell density. Results suggest neuroprotective properties attributed to its antioxidant properties. (39)
• Mosquito Larvicidal / Essential Oils: Study evaluated leaf, stem, and floral essential oils of C. crepidioides by hydrodistillation and GC-MS spectrometry for larvicidal activities against Aedes aegypti, Ae. albopictus, and Culex quinquefasciatus. The major component in all 3 oils was myrcene (59.3%, 26.1%, and 43.3% respectively). The 24-hour mosquito larvicidal activities of EO of aerial parts (stems and leaves) against Ae. albopictus showed IC50 of 14.3 µg/mL, Ae. aegypti IC50 4.95 µg/mL, and Cx. quinquefasciatus IC50 18.4 µg/mL. Mosquito larvicidal activity was attributed to the high concentration of myrcene in the EO. (40)
Availability
Wild-crafted.
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