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| Andrographis — Andrographis (typically Andrographis paniculata, “King of Bitters”) is a bitter medicinal plant whose principal bioactive diterpenoid lactone is andrographolide (with related diterpenoids such as neoandrographolide). It is best classified as a botanical drug / phytochemical mixture (plant extract) with a dominant small-molecule active. Common abbreviation(s): AP (plant), AND (andrographolide). The best-supported pharmacology in humans is anti-inflammatory/immunomodulatory use (e.g., URTI symptom reduction), while oncology relevance is predominantly preclinical, with frequent reporting of NF-κB/STAT3/PI3K-AKT pathway suppression and downstream effects on proliferation, apoptosis, invasion, and angiogenesis. Primary mechanisms (ranked):
Bioavailability / PK relevance: Oral exposure of andrographolide from extracts is highly formulation-dependent and often low; even at high oral regimens used clinically (e.g., extract equivalents targeting ~180–360 mg/day andrographolide), measured plasma concentrations can remain in the low ng/mL range and may show non-linear dose proportionality. This creates a translation gap for many oncology in-vitro concentrations unless delivery is optimized (e.g., solubility enhancement, lipid/polymer carriers, prodrugs). In-vitro vs systemic exposure relevance: Many reported anticancer effects occur at micromolar in-vitro levels that commonly exceed achievable free systemic concentrations after standard oral supplementation; therefore, “direct cytotoxic” interpretations are frequently exposure-limited, while anti-inflammatory signaling modulation may be more plausibly aligned with in-vivo exposures depending on tissue distribution and formulation. Clinical evidence status: Human clinical evidence is strongest for infectious/inflammatory indications (URTI symptom reduction; studied in COVID-19-era settings with mixed outcomes and safety monitoring). For oncology, evidence is primarily preclinical, with limited registered/early clinical exploration and no established standard anticancer indication. "used traditionally for the treatment of array of diseases such as cancer, diabetes, high blood pressure, ulcer, leprosy, bronchitis, skin diseases, flatulence, colic, influenza, dysentery, dyspepsia and malaria for centuries in Asia, America and Africa continents." Andrographolide: – Is a specific diterpenoid lactone and the major active constituent extracted from Andrographis paniculata. – It is responsible for many of the therapeutic effects attributed to the plant, including anti-inflammatory and antioxidant properties. A. Anti-Inflammatory Effects. • Andrographolide has been shown to inhibit the NF-κB pathway, leading to a reduction in the transcription of inflammatory cytokines (e.g., TNF-α, IL-6). • Andrographolide has been reported to cause cell cycle arrest at critical checkpoints (such as G0/G1 or G2/M phase) in some cancer cell models. Andrographis, primarily through its active constituent andrographolide, offers compelling anti-inflammatory, immunomodulatory, pro-apoptotic, and antiproliferative properties. While not a standard anticancer agent, its capacity to modulate key pathways in cellular stress response and inflammation makes it an attractive candidate for complementary research in oncology. Andrographis paniculata, also known as the "King of Bitters," is a plant native to India and Southeast Asia. Its aqueous extract, Andrographis paniculata aqueous extract (APAE), has been studied for its potential anti-cancer properties. • Inhibition of cancer cell growth: APAE has been shown to inhibit the growth of various cancer cell lines, including breast, lung, colon, and prostate cancer cells. • Induction of apoptosis: APAE has been found to induce apoptosis (programmed cell death) in cancer cells, which may help to prevent tumor growth and progression. • Anti-inflammatory effects: APAE has anti-inflammatory properties, which may help to reduce the risk of cancer development and progression. • Antioxidant activity: APAE has antioxidant activity, which may help to protect against oxidative stress and DNA damage. Key compounds:Andrographolide, Neoandrographolide APAE may interact with certain medications, including blood thinners and diabetes medications, and may not be suitable for individuals with certain medical conditions, such as autoimmune disorders. Andrographis (A. paniculata / andrographolide) — ranked mechanistic axes in oncology context
TSF legend: P: 0–30 min; R: 30 min–3 hr; G: >3 hr |
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| Also known as CP32. Cysteinyl aspartate specific proteinase-3 (Caspase-3) is a common key protein in the apoptosis and pyroptosis pathways, and when activated, the expression level of tumor suppressor gene Gasdermin E (GSDME) determines the mechanism of tumor cell death. As a key protein of apoptosis, caspase-3 can also cleave GSDME and induce pyroptosis. Loss of caspase activity is an important cause of tumor progression. Many anticancer strategies rely on the promotion of apoptosis in cancer cells as a means to shrink tumors. Crucial for apoptotic function are executioner caspases, most notably caspase-3, that proteolyze a variety of proteins, inducing cell death. Paradoxically, overexpression of procaspase-3 (PC-3), the low-activity zymogen precursor to caspase-3, has been reported in a variety of cancer types. Until recently, this counterintuitive overexpression of a pro-apoptotic protein in cancer has been puzzling. Recent studies suggest subapoptotic caspase-3 activity may promote oncogenic transformation, a possible explanation for the enigmatic overexpression of PC-3. Herein, the overexpression of PC-3 in cancer and its mechanistic basis is reviewed; collectively, the data suggest the potential for exploitation of PC-3 overexpression with PC-3 activators as a targeted anticancer strategy. Caspase 3 is the main effector caspase and has a key role in apoptosis. In many types of cancer, including breast, lung, and colon cancer, caspase-3 expression is reduced or absent. On the other hand, some studies have shown that high levels of caspase-3 expression can be associated with a better prognosis in certain types of cancer, such as breast cancer. This suggests that caspase-3 may play a role in the elimination of cancer cells, and that therapies aimed at activating caspase-3 may be effective in treating certain types of cancer. Procaspase-3 is a apoptotic marker protein. Prognostic significance: • High Cas3 expression: Associated with good prognosis and increased sensitivity to chemotherapy in breast, gastric, lung, and pancreatic cancers. • Low Cas3 expression: Linked to poor prognosis and increased risk of recurrence in colorectal, hepatocellular carcinoma, ovarian, and prostate cancers. |
| 1351- | And, | MEL, | Impact of Andrographolide and Melatonin Combinatorial Drug Therapy on Metastatic Colon Cancer Cells and Organoids |
| - | in-vitro, | CRC, | T84 | - | in-vitro, | CRC, | COLO205 | - | in-vitro, | CRC, | HT-29 | - | in-vitro, | CRC, | DLD1 |
| 1078- | And, | Andrographolide inhibits breast cancer through suppressing COX-2 expression and angiogenesis via inactivation of p300 signaling and VEGF pathway |
| - | in-vitro, | BC, | MDA-MB-231 | - | in-vitro, | Nor, | HUVECs | - | in-vivo, | BC, | MCF-7 | - | in-vitro, | BC, | T47D | - | in-vitro, | BC, | BT549 | - | in-vitro, | BC, | MDA-MB-361 |
Query results interpretion may depend on "conditions" listed in the research papers. Such Conditions may include : -low or high Dose -format for product, such as nano of lipid formations -different cell line effects -synergies with other products -if effect was for normal or cancerous cells
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